Abstract: The present invention relates to a method of preparing a material formed from arborescent-branched molecules comprising associative groups that includes the following successive steps: (a) the reaction of at least one at least trifunctional compound (A) bearing first and second functional groups with at least one bifunctional compound (B), the functional groups of which are capable of reacting with the first functional groups of the compound (A); and (b) the reaction of the compound(s) obtained in step (a) with at least one compound (C) bearing, on the one hand, at least one reactive group capable of reacting with the second functional groups of (A) and, on the other hand, at least one given associative group.
Type:
Grant
Filed:
December 19, 2008
Date of Patent:
September 10, 2013
Assignees:
Arkema France, Centre National de la Recherche Scientifique CNRS
Inventors:
François-Genes Tournilhac, Manuel Hidalgo, Ludwik Leibler
Abstract: The present invention is a compound having the general formula (I), (II), or (III) or a pharmacologically acceptable salt, solvate, or hydrate thereof, and a pharmaceutical composition containing such a compound, or its pharmacologically acceptable ester, or other pharmacologically acceptable derivative thereof as an active ingredient. The compound has an excellent ACAT 2-inhibiting activity by a mechanism different from that of a statin drug and is useful as a therapeutic or prophylactic agent for obesity, adiposis, hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, and arteriosclerosis, as well as obesity-derived hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, arteriosclerosis, and hypertension.
Abstract: ABT-263 free base and crystalline forms thereof are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
Type:
Grant
Filed:
July 28, 2011
Date of Patent:
August 20, 2013
Assignee:
AbbVie Inc.
Inventors:
Geoff G. Z. Zhang, Paul J. Brackemeyer, Nathaniel D. Catron, Thomas B. Borchardt
Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.
Abstract: This invention is directed to compounds of the formula (I) and salts therefore that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds of this invention, pharmaceutical compositions and kits comprising the compounds of this invention, uses of the compounds of this invention to make medicaments, and treatments comprising the administration of the compounds of this invention to animals in need of the treatments.
Type:
Grant
Filed:
June 16, 2010
Date of Patent:
August 13, 2013
Assignee:
Intervet International B.V.
Inventors:
Christophe Pierre Alain Chassaing, Thorsten Meyer
Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, —SO.sub.
Type:
Grant
Filed:
February 19, 2010
Date of Patent:
August 13, 2013
Assignees:
Vernalis (R&D) Limited, Cancer Research Technology Limited, The Institute of Cancer Research
Inventors:
Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
Type:
Grant
Filed:
June 17, 2011
Date of Patent:
August 13, 2013
Assignee:
Threshold Pharmaceuticals, Inc.
Inventors:
Mark Matteucci, Jian-Xin Duan, Hailong Jiao, Jacob Kaizerman
Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.
Type:
Grant
Filed:
August 4, 2009
Date of Patent:
July 23, 2013
Assignee:
Virginia Commonwealth University
Inventors:
Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
Abstract: The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
Type:
Grant
Filed:
February 18, 2009
Date of Patent:
July 23, 2013
Assignee:
Merck, Sharp & Dohme, Corp.
Inventors:
Ivory D. Hills, Craig A. Coburn, Samuel L. Graham, Keith P. Moore, Philippe G. Nantermet, Hemaka A. Rajapakse, Shawn J. Stachel, Hong Zhu
Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
Type:
Grant
Filed:
December 3, 2008
Date of Patent:
July 2, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
Abstract: There is provided an electroactive material having Formula I wherein: Q is the same or different at each occurrence and can be O, S, Se, Te, NR, SO, SO2, or SiR3; R is the same or different at each occurrence and can be hydrogen, alkyl, aryl, alkenyl, or alkynyl; R1 through R8 are the same or different and can be hydrogen, alkyl, aryl, halogen, hydroxyl, aryloxy, alkoxy, alkenyl, alkynyl, amino, alkylthio, phosphino, silyl, —COR, —COOR, —PO3R2, —OPO3R2, or CN.
Abstract: Disclosed is an ionic liquid which is stable over a wide potential range and exhibits a high ionic conductivity. The ionic liquid comprises a cyclic guanidine salt represented by the following formula (1): wherein R1 and R2 each is independently an alkyl group or an alkoxyalkyl group, X is a methylene group, an oxygen atom, a sulfur atom, or R3N; R3 is an alkyl group, an alkoxyalkyl group, or an acyl group; l, m, and n each is an integer in the range of 1-6; Y? is a monovalent anion such as (R4SO2)2N?, R4SO3?, R4COO?, BF4?, PF6?, NO3?, (CN)2N?, (CHO)2N?, NCS?, R4OSO3?, R4SO2S?, and a halogen ion. The ionic liquid is useful for a variety of electrolytes, particularly for electrolytes of electrochemical cells.
Type:
Grant
Filed:
January 25, 2012
Date of Patent:
May 28, 2013
Assignee:
Nippon Steel & Sumikin Chemical Co., Ltd.
Inventors:
Atsushi Kawada, Aya Tashiro, Toshihiro Kumagai
Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.
Type:
Grant
Filed:
June 18, 2012
Date of Patent:
May 28, 2013
Assignees:
Vernalis (R&D) Limited, Cancer Research Technology Ltd., The Institute of Cancer Research
Inventors:
Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
Abstract: Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.
Type:
Grant
Filed:
September 16, 2011
Date of Patent:
April 30, 2013
Assignee:
Zealand Pharma A/S
Inventors:
Bjarne Due Larsen, Jørgen Søberg Petersen, Ketil Jørgen Haugan, John A. Butera, James K. Hennan, Edward H. Kerns, Evgueni Lvovich Piatnitski
Abstract: The invention provides derivatives of azabicyclo alkane having formula (ID), and the method for making them, wherein each substitute in formula (ID) is same as defined in the description.
Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38?, and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
Type:
Grant
Filed:
June 22, 2012
Date of Patent:
April 2, 2013
Assignee:
Novartis AG
Inventors:
Olga M. Fryszman, Hengyuan Lang, Jiong Lan, Edcon Chang, Yunfeng Fang
Abstract: The present invention relates to a method for regioselectively reducing the maleimide compounds of formula (I). The invention also relates to C7 hydroxy lactam regioisomers of formula (II) obtainable by this method and their use for the preparation of lactams of formula (III) which are particularly useful as intermediate for the synthesis of fused pyrrolocarbazoles.
Abstract: This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast.
Abstract: The present invention relates to a process for preparing azabicyclic compounds that are useful intermediates for synthesizing pharmaceutical compounds or salts thereof.
Type:
Grant
Filed:
September 17, 2010
Date of Patent:
March 26, 2013
Assignee:
Vertex Pharmaceuticals
Inventors:
Narendra Bhalchandra Ambhaikar, Brian Richard Bear, Lev T. D. Fanning, Robert Hughes, Benjamin Littler