Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameliorated by inhibition of phosphatidylinositol 3-kinase.
Type:
Grant
Filed:
July 2, 2010
Date of Patent:
January 22, 2013
Assignee:
Novartis AG
Inventors:
Robin Alec Fairhurst, Marc Gerspacher, Robert Mah
Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
Type:
Grant
Filed:
November 15, 2010
Date of Patent:
January 22, 2013
Assignee:
Receptos, Inc.
Inventors:
Esther Martinborough, Marcus F. Boehm, Adam Richard Yeager, Junko Tamiya, Liming Huang, Enugurthi Brahmachary, Manisha Moorjani
Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.
Type:
Grant
Filed:
June 17, 2009
Date of Patent:
January 15, 2013
Assignee:
Concert Pharmaceuticals, Inc.
Inventors:
Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof.
Abstract: A pharmaceutical composition comprising a pharmaceutically acceptable excipient or carrier and a compound Formula I: or a pharmaceutically acceptable salt or prodrug thereof.
Type:
Grant
Filed:
March 19, 2009
Date of Patent:
January 8, 2013
Assignee:
New Mexico Technical Research Foundation
Inventors:
Alexander Kornienko, Igov V. Magedov, Snezna Rogelj
Abstract: The efficiency of catalyzed batch esterification reactions is improved by the use of a particular temperature and pressure profile during the reaction cycle. In particular elevated pressure is maintained to prevent alcohol boil off during initial mixing and reaction of the reactants prior to any catalyst addition, and preferably the pressure is reduced rapidly after the desired reaction temperature has been reached.
Type:
Grant
Filed:
March 7, 2008
Date of Patent:
January 1, 2013
Assignee:
ExxonMobil Chemical Patents Inc.
Inventors:
Nicolaas Anthony De Munck, Klaas Bandstra, Raphael Frans Caers, Brady Compton, John Lyford, IV, Aad Gerrit Oskam, Berend Jan Van Der Veen
Abstract: The present invention relates to compounds selected from the group consisting of 14-0-[((Mono- or dialkylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[((Cycloalkyl- or heterocyclylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioaceyl or -imino-oxy]-mutilins, 14-O-[((Heterocyc-N-yl-cycloalkyl)-sulfanyl- or -oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Mono- or dialkylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Cycloalkyl- or heterocyclylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and 14-O-[((Heterocyc-N-yl-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and their use as pharmaceuticals.
Abstract: Disclosed herein are compounds of formula (I) wherein R1, R2, R3, R25a, R26a, X, and n are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions are also described.
Type:
Grant
Filed:
September 26, 2011
Date of Patent:
December 25, 2012
Assignee:
AbbVie Inc.
Inventors:
Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez-Medrano, Xueqing Wang, Karin Rose Marie Tietje, Sridhar Peddi, William A. Carroll
Abstract: The present invention relates to a compound according to formula I, wherein X, A, G, E, R1, R2, R3 are as shown herein; and pharmaceutically acceptable salts, hydrates, N-oxides or solvates hereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
Type:
Grant
Filed:
February 26, 2008
Date of Patent:
December 25, 2012
Assignee:
Leo Pharma A/S
Inventors:
Ravindra Babu Bollu, Jakob Felding, Simon Feldbæk Nielsen, Jens Christian Højland Larsen
Abstract: The present invention relates to thiadiazolyloxyphenylamidines of the general formula (I), to a process for the preparation thereof, to the use of the amidines according to the invention in combating undesirable microorganisms and to a composition for this purpose comprising the thiadiazolyloxyphenylamidines according to the invention. The invention furthermore relates to a method for combating undesirable microorganisms by application of the compounds according to the invention to the microorganisms and/or to the habitat thereof.
Type:
Grant
Filed:
June 19, 2009
Date of Patent:
December 18, 2012
Assignee:
Bayer Cropscience AG
Inventors:
Pierre Cristau, Jörg Nico Greul, Ulrich Heinemann, Klaus Kunz, Oswald Ort, Thomas Seitz, Arnd Voerste, Peter Dahmen, Ulrike Wachendorff-Neumann, Klaus-Günther Tietjen, Hiroyuki Hadano
Abstract: An organic compound represented by the following general formula (I) and characterized by the conjugation of thieno[3,2-b]thiophene, thiophene and phenylene units in the conjugated compound.
Type:
Grant
Filed:
February 19, 2009
Date of Patent:
December 11, 2012
Assignees:
Nanyang Technological University, Agency for Science, Technology and Research
Inventors:
Omer E. Ahmed Moawia, Ashok Mishra, Andrew Grimsdale, Siu Choon Ng, Subodh G. Mhaisalkar, Beng Ong, Zhikuan Chen
Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds of general formula (A) wherein A1 is sulfur, A3 is CH, A2 is CH, D is heterocycle, Z is oxygen, SO0-2 or NR, Ar is phenyl and G is not a ring, and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
Type:
Grant
Filed:
December 8, 2011
Date of Patent:
December 11, 2012
Assignee:
MethylGene Inc.
Inventors:
Oscar Mario Saavedra, Stephen William Claridge, Lijie Zhan, Franck Raeppel, Arkadii Vaisburg, Stephane Raeppel, Michael Mannion, Frederic Gaudette, Ljubomir Isakovic, Marie-Claude Granger, Naomy Bernstein
Abstract: The present invention provides a novel class of azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
Type:
Grant
Filed:
January 21, 2010
Date of Patent:
December 4, 2012
Assignee:
Corcept Therapeutics, Inc.
Inventors:
Robin D. Clark, Nicholas C. Ray, Paul Blaney, Christopher Hurley, Hazel Hunt, David Clark, Karen Williams
Abstract: Substituted 3-(4-((1H-imidazol-1-yl)methyl)phenyl)-5-phenyl-1,2,4-oxadiazole derivatives which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
Abstract: Invention is related to novel compounds -5-aryl-4-(5-substituted 2,4-dihydroxyphenyl)-1,2,3-thiadiazoles with general formula (I). The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit Hsp90 chaperone which participate in cancer progression. This invention is also related to new intermediate compounds which are used for the synthesis of thiadiazoles of general formula (I).
Type:
Grant
Filed:
June 18, 2008
Date of Patent:
November 20, 2012
Assignee:
Biotechnologijos Institutas
Inventors:
Daumantas Matulis, Inga Cikotiene, Egidijus Kazlauskas, Jurgita Matuliene
Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.
Type:
Grant
Filed:
February 9, 2010
Date of Patent:
November 20, 2012
Assignee:
Laboratorios del Dr. Esteve, S.A.
Inventors:
Christian Laggner, Maria Rosa Cuberes-Altisent, Joerg Holenz, Juana Maria Berrocal-Romero, Maria Montserrat Contijoch-Llobet
Abstract: The present invention relates to piperidine and piperazine phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.
Type:
Grant
Filed:
March 14, 2012
Date of Patent:
November 13, 2012
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Esther Ann Martinborough, Lev Tyler Dewey Fanning, Urvi Jagdishbhai Sheth, Dean Mitchell Wilson, Andreas P. Termin, Timothy Donald Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
Abstract: There is provided a fluorine-containing organosulfur compound having an excellent controlling effect on arthropod pests represented by the formula (I): wherein m represents 0 or 1; n represents 0, 1 or 2; A represents an optionally substituted 5-membered aromatic heterocyclic group; R1 and R3 are independently represent an optionally substituted C1-C4 chain hydrocarbon group, —C(?G)R5, cyano, halogen or hydrogen; R2 and R4 independently represent an optionally substituted C1-C4 chain hydrocarbon group, halogen or hydrogen; Q represents a C1-C5 haloalkyl group containing at least one fluorine, or fluorine; G represents oxygen or sulfur; and R5 represents optionally substituted C1-C4 alkyl, hydroxyl, optionally substituted C1-C4 alkoxy, optionally substituted C3-C6 alkenyloxy, optionally substituted C3-C6 alkynyloxy, amino, optionally substituted C1-C4 alkylamino, optionally substituted di(C1-C4 alkyl)amino, C2-C5 cyclic amino or hydrogen.
Abstract: The use of a compound of formula I wherein X is (i), (ii) or (iii) Y is O, S(O)m, NR3, CR5R6, CR5R6—CR7R8, O—CR7R8, S(O)m—CR7R8, NR3—CR7R8, CR5R6—O, CR5R6—S(O)m, CR5R6—NR3, SO2—NR3, NR3—SO2, NR3—O or O—NR3; m is 0, 1, or 2; the ring (T) is a 5- or 6-membered aromatic or heteroaromatic ring; R1 to R10 are specified organic groups and n and is 0, 1, 2, 3 or 4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.
Type:
Grant
Filed:
May 11, 2011
Date of Patent:
November 13, 2012
Assignee:
Syngenta Limited
Inventors:
Anthony Cornelius O'Sullivan, Juergen Harry Schaetzer, Christoph Luethy, Allison Clare Elliott, Christopher John Mathews