Acyclic Carbon Bonded Directly To The -c(=x)- (e.g., N-oleoylpyrrolidine, Etc.) Patents (Class 548/540)
  • Patent number: 9249096
    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. The disclosure also provides a novel method of treating diseases or conditions related to the activity of endothelial lipase by use of compounds according to Formula (II): as defined in the specification and compositions comprising any of the compounds.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: February 2, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Patent number: 9115082
    Abstract: The invention comprises novel inhibitors of dipeptidyl peptidase IV (DPP-IV) with beta blocker activity, pharmaceutical compositions comprising therapeutically effective amounts of novel inhibitors of DPP-IV, and novel methods of treating medical conditions are provided. The novel inhibitors of DPP-IV described herein are useful in the treatment of neurological disorders, diabetes, inflammatory disorders such as arthritis, obesity, osteoporosis, hypertension, and glaucoma of such other enumerated conditions as can be treated with inhibitors of DPP-IV and beta blockers.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: August 25, 2015
    Inventors: Catherine Yang, Weixing Li
  • Publication number: 20150141646
    Abstract: In certain aspects, compounds and uses thereof are provided. In certain aspects, compound-conjugates and uses thereof are provided.
    Type: Application
    Filed: May 14, 2013
    Publication date: May 21, 2015
    Applicant: Concortis Biosystems, Corp., a wholly owned subsidary of Sorrento Therapeutics, Inc,
    Inventors: Zhenwei Miao, Yufeng Hong, Tong Zhu
  • Publication number: 20150141624
    Abstract: This invention relates to anti-CD70 antibodies and antibody drug conjugates comprising at least one non-naturally-encoded amino acid. Disclosed herein are ?CD70 antibodies with one or more non-naturally encoded amino acids and further disclosed are antibody drug conjugates wherein the ?CD70 antibodies of the invention are conjugated to one or more toxins. Further disclosed are methods for using such non-natural amino acid antibody drug conjugates, including therapeutic, diagnostic, and other biotechnology uses.
    Type: Application
    Filed: June 19, 2013
    Publication date: May 21, 2015
    Applicant: AMBRX, INC.
    Inventors: Richard S. Barnett, Nick Knudsen, Ying Sun, Sandra Biroc, Timothy Buss, Tsotne Javahishvili, Damien Bresson, Shailaja Srinagesh, Amha Hewet, Jason K. Pinkstaff
  • Patent number: 9029406
    Abstract: The present application relates to new derivatives, substituted on the N terminus by a carboxyalkyl group, of monomethylauristatin E and monomethylauristatin F, to processes for preparing these derivatives, to the use of these derivatives for treating and/or preventing diseases, and to the use of these derivatives for producing medicaments for treating and/or preventing diseases, more particularly hyperproliferative and/or angiogenic disorders such as cancer disorders, for example. Such treatments may be applied as a monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: May 12, 2015
    Assignee: Seattle Genetics, Inc
    Inventors: Hans-Georg Lerchen, Sherif El Sheikh, Beatrix Stelte-Ludwig, Joachim Schuhmacher, Mark Gnoth
  • Publication number: 20150087823
    Abstract: The present invention relates to a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical agent containing the compound as an active ingredient. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt, which is the compound of the present invention, is specifically represented by the general formula (I): wherein X is a substituent such as a 1-pyrrolidyl, a 3-thiazolizyl, or a piperidino, and the compound is highly useful as a pharmaceutical agent, such as a prophylactic or therapeutic agent for a peripheral nerve disorder induced by administration of an anticancer agent, a prophylactic or therapeutic agent for neurodegenerative diseases or mental diseases such as dementia, Alzheimer's disease, Parkinson's disease, diabetic neuropathy, depression, glaucoma, or autistic disorder spectrum, a therapeutic or repairing agent for spinal cord injury, analgesics against various pain diseases, or the like.
    Type: Application
    Filed: April 26, 2013
    Publication date: March 26, 2015
    Inventors: Munekazu Iinuma, Shoei Furukawa, Mitsuru Naiki, Tomonori Matsumoto, Kunihiko Higashiura
  • Publication number: 20150080559
    Abstract: Disclosed herein are non-natural amino acids and dolastatin analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The dolastatin analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid dolastatin analogs and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology uses.
    Type: Application
    Filed: May 24, 2012
    Publication date: March 19, 2015
    Applicant: AMBRX, INC.
    Inventors: Zhenwei Miao, Kyle Atkinson, Sandra Biroc, Timothy Buss, Melissa Neal, Vadim Kraynov, Robin Mardsen, Jason Pinkstaff, Lillian Skidmore, Ying Sun, Agnieszka Szydlik, Ianina Valenta
  • Patent number: 8980936
    Abstract: The present invention is directed to the compound 2-(4-(hydroxymethyl)phenoxy)-1-(3-(2-(trifluoromethyl)phenoxy)pyrrolidin-1-yl)ethanone, its use as an inhibitor of stearoyl CoA desaturase and to pharmaceutical compositions containing this compound.
    Type: Grant
    Filed: July 18, 2013
    Date of Patent: March 17, 2015
    Assignee: Thesan Pharmaceuticals, Inc.
    Inventors: Jin Li, Nicole Lee Kolosko
  • Publication number: 20150057451
    Abstract: The present invention provides organic molecules and methods thereof for reactions between organoboron reagents and double bonds, such as imines or carbonyls, to stereoselectively provide chiral products including amines and alcohols, entities useful for the preparation of biologically active molecules.
    Type: Application
    Filed: March 1, 2013
    Publication date: February 26, 2015
    Inventors: Amir H. Hoveyda, Daniel L. Silverio, Tatiana Pilyugina, Sebastian Torker, Daniel Robbins
  • Patent number: 8952180
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) 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: Grant
    Filed: September 25, 2012
    Date of Patent: February 10, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20150038493
    Abstract: The present invention relates to a series of molecules derived from 2,3-diaminopropionic acid (DAP), comprising or not comprising an 8-hydroxyquinoline (8-HQ) motif, and to the use of said molecules for trapping an alpha-oxoaldehyde resulting particularly from the degradation of the glucose or for trapping an alpha-beta-unsaturated aldehyde, resulting particularly from the oxidative degradation of fatty acids. These molecules can have a further application in the fields of cosmetics, food processing, and pharmaceuticals.
    Type: Application
    Filed: October 5, 2012
    Publication date: February 5, 2015
    Inventors: Guy Potier, André Nobumichi Sasaki, Nicolas Audic
  • Patent number: 8946432
    Abstract: Disclosed is a compound of formula (I): wherein ‘D’, ‘E’, ‘m’, ‘n’ and R1-R4 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
    Type: Grant
    Filed: July 2, 2012
    Date of Patent: February 3, 2015
    Assignee: Lupin Limited
    Inventors: Neelima Sinha, Navnath Popat Karche, Girish Dhanraj Hatnapure, Anil Kashiram Hajare, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 8912329
    Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: December 16, 2014
    Assignee: Bioversys AG
    Inventors: Ronald Schoenmakers, Wilfried Weber, Marc Gitzinger, Martin Fussenegger, Marcel Tigges, Peter Schneider
  • Patent number: 8853393
    Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: October 7, 2014
    Assignee: Anhui New Star Pharmaceutical Development Co., Ltd.
    Inventors: Ziao Xu, Yuanhai Zhao, Degang Li, Xiaoxiang Li
  • Publication number: 20140296527
    Abstract: The present invention relates to processes for the enantio-selective preparation of spyrrolidine derivatives useful in the manufacture of pesticidally active compounds, as well as to intermediates in the processes. The processes include those comprising (a-i) reacting a compound of formula Ia wherein P is alkyl, aryl or heteroaryl, each optionally substituted, wherein the heteroaryl is connected at P via a ring carbon atom; R1 is chlorodifluoromethyl or trifluoromethyl; R2 is aryl or heteroaryl, each optionally substituted; with a source of cyanide in the presence a chiral catalyst to give a compound of formula IIa wherein P, R1 and R2 are as defined for the compound of formula Ia; and (a-ii) oxidising the compound of formula IIa with a peroxy acid, or peroxide in the presence of an acid to give a compound of formula VI wherein R1 and R2 are as defined for the compound of formula Ia.
    Type: Application
    Filed: September 28, 2012
    Publication date: October 2, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Tomas Smejkal, Helmars Smits, Sebastian Volker Wendeborn, Guillaume Berthon, Jerome Yves Cassayre, Myriem El Qacemi
  • Publication number: 20140275543
    Abstract: A method for stabilization of potent alkanone-heterocyclic flavorants in dry powder form is provided. Coordination of alkanone-heterocyclic flavorants to transition metal salts results in the formation of stable crystalline complexes, which upon hydration release the free flavorant. Food and topping products containing the stabilized alkanone-heterocyclic flavorant are provided as are methods for stabilizing the alkanone-heterocyclic flavorant.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Keith R. Cadwallader, Ming-Chih Fang
  • Publication number: 20140256702
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: March 4, 2014
    Publication date: September 11, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Erik Fenster, Melissa Fleury, Adam D. Hughes
  • Publication number: 20140249320
    Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
    Type: Application
    Filed: March 25, 2014
    Publication date: September 4, 2014
    Inventors: David Hook, Thomas Ruch, Bernard Riss, Bernhard Wietfeld, Gottfried Sedelmeier, Matthias Napp, Markus Bänziger, Steven Hawker, Lech Ciszewski, Liladhar Murlidhar Waykole
  • Publication number: 20140179925
    Abstract: Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas 1 and 2 wherein the variables have the meaning disclosed in the specification
    Type: Application
    Filed: December 18, 2013
    Publication date: June 26, 2014
    Applicant: Allergan, Inc.
    Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
  • Publication number: 20140171641
    Abstract: Disclosed is a process for making diastereomeric N-sulfinyl ?-amino amides by reaction of chiral sulfinimines with formamides and lithium diisopropylamide. The process of the invention provides the N-sulfinyl ?-amino amides in high yields and with high diastereoselectivity.
    Type: Application
    Filed: November 5, 2013
    Publication date: June 19, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Jonathan Timothy REEVES, Chris H. SENANAYAKE
  • Publication number: 20140155433
    Abstract: Disclosed is a compound of formula (I): wherein ‘D’, ‘E’, ‘m’, ‘n’ and R1-R4 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
    Type: Application
    Filed: July 2, 2012
    Publication date: June 5, 2014
    Applicant: LUPIN LIMITED
    Inventors: Neelima Sinha, Navnath Popat Karche, Girish Dhanraj Hatnapure, Anil Kashiram Hajare, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20140142322
    Abstract: The present application provides methods and catalysts for activation of carboxylic acids for organic reactions.
    Type: Application
    Filed: February 14, 2012
    Publication date: May 22, 2014
    Inventors: Dennis Hall, Nicolas Gernigon, Raed Al-Zoubi, Paul D. Thornton
  • Publication number: 20140127240
    Abstract: The present patent application relates to novel binder-drug conjugates (ADCs) of N,N-dialkylauristatins directed against the target epidermal growth factor receptor (EGFR, gene ID 1956), effective metabolites of these ADCs, methods for producing these ADCs, use of these ADCs for treatment and or prevention of diseases as well as the use of these ADCs to produce pharmaceutical drugs for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic diseases such as cancer, for example. Such treatments may be administered as monotherapy or in combination with other pharmaceutical drugs or other therapeutic measures.
    Type: Application
    Filed: April 20, 2012
    Publication date: May 8, 2014
    Applicants: Bayer Pharma Aktiengesellschaft, Bayer Intellectual Property GmbH
    Inventors: Hans-Georg Lerchen, Lars Linden, Sherif El Sheikh, Jörg Willuda, Charlotte C. Kopitz, Joachim Schuhmacher, Simone Greven, Christoph Mahlert, Beatrix Stelte-Ludwig, Sven Golfier, Rudolf Beier, Iring Heisler, Axel Harrenga, Karl-Heinz Thierauch, Sandra Bruder, Heike Petrul, Hannah Jörißen, Sandra Brokowski
  • Patent number: 8710241
    Abstract: The present invention relates to a novel anhydrous crystalline form of zofenopril calcium of formula (I), chemically known as (4S)-1-[(2S)-3-(benzoylthio)-2-methylpropionyl]-4-(phenylthio)-L-proline calcium salt or hemi-calcium salt. The present invention further relates to a process for the preparation of the new crystalline form of zofenopril calcium, its use in pharmaceutical compositions and the use of the new crystalline form and compositions in the treatment of hypertension and various other diseases.
    Type: Grant
    Filed: August 8, 2008
    Date of Patent: April 29, 2014
    Assignee: Generics [UK]Limited
    Inventor: Axel Becker
  • Publication number: 20140100227
    Abstract: Disclosed herein are novel C17-alkanediyl and alkenediyl derivatives of oleanolic acid, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.
    Type: Application
    Filed: September 10, 2013
    Publication date: April 10, 2014
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventors: Christopher F. BENDER, Xin JIANG, Eric ANDERSON, Melean VISNICK
  • Publication number: 20140093513
    Abstract: The invention relates to new methods of modulating cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) with fatty acid derivatives; and new methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid derivative. The present invention is also directed to fatty acid bioative derivatives and their use in the treatment of metabolic diseases.
    Type: Application
    Filed: May 24, 2013
    Publication date: April 3, 2014
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Chi B. Vu
  • Publication number: 20140088074
    Abstract: Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
    Type: Application
    Filed: May 29, 2012
    Publication date: March 27, 2014
    Applicant: NEWRON PHARMACEUTICALS S.P.A.
    Inventor: Paolo Pevarello
  • Publication number: 20140066420
    Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
    Type: Application
    Filed: October 16, 2013
    Publication date: March 6, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Shizuo KASAI, Tomohiro KAKU, Masahiro KAMAURA
  • Publication number: 20140051697
    Abstract: The present invention relates to compounds of formula (I) its salts, isomers or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation.
    Type: Application
    Filed: October 23, 2013
    Publication date: February 20, 2014
    Applicant: Biota Scientific Management Pty Ltd.
    Inventors: Jeffrey Peter Mitchell, Gary Pitt, Alistair George Draffan, Penelope Anne Mayes, Laura Andrau, Kelly Helen Anderson
  • Publication number: 20140018327
    Abstract: Disclosed is a compound of formula (I) wherein ‘a’ and R1-R5 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereofs, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
    Type: Application
    Filed: March 27, 2012
    Publication date: January 16, 2014
    Applicant: LUPIN LIMITED
    Inventors: Neelima Sinha, Gourhari Jana, Ajay Ramchandra Tilekar, Navnath Popat Karche, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 8624022
    Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: January 7, 2014
    Assignee: UCB Pharma, S.A.
    Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
  • Publication number: 20130331387
    Abstract: Disclosed is a compound of formula (I), wherein Z, m and R1-R6 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
    Type: Application
    Filed: February 22, 2012
    Publication date: December 12, 2013
    Applicant: Lupin Limited
    Inventors: Neelima Sinha, Gourhari Jana, Sachchidanand Sachchidanand, Sanjay Pralhad Kurhade, Navnath Popat Karche, Anil Kashiram Hajare, Ajay Ramchandra Tilekar, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20130324539
    Abstract: Improved methods of treating multiple sclerosis and/or psoriasis using prodrugs of methyl hydrogen fumarate are disclosed. The methods comprise administering certain prodrugs of methyl hydrogen fumarate. The methods are able to achieve high blood plasma concentrations of the active metabolite, methyl hydrogen fumarate, without causing significant gastrointestinal irritation. New prodrugs of methyl hydrogen fumarate are also disclosed.
    Type: Application
    Filed: May 30, 2013
    Publication date: December 5, 2013
    Inventors: Peter A. Virsik, David J. Wustrow, Thamil Annamalai
  • Patent number: 8597706
    Abstract: The present invention relates to a method for synthetizing a compound of the following formula (I): wherein R is a methyl or ethyl group, n is 1 or 2, and X is a CH2 or CD2 group, from a compound of the following formula (II): wherein R and n are as defined above, and also relates to a method for assaying the compounds of the formula (I) using a corresponding deuterated derivative as an internal reference, as well as to the use of ketal derivatives of compounds of the formula (I) as a stable precursor, in particular in a flavoring composition.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: December 3, 2013
    Assignees: Centre National de la Recherche Scientifique (CNRS), Universite Montpellier 2 Sciences et Techniques
    Inventors: Alain Morere, Chantal Menut, Yusuf Ziya Gunata, Abdelhamid Agrebi
  • Publication number: 20130310419
    Abstract: The present invention is related to pyrrole derivatives of formula I as the modulators of nicotinic acetylcholine receptors particularly the ?7 subtype. The invention includes pyrrole derivatives, analogues, their prodrugs, their isotopes, their metabolites, pharmaceutically acceptable salts, polymorphs, solvates, optical isomers, clathrates, co-crystals, combinations with suitable medicament and pharmaceutical compositions thereof. The present invention also includes process of preparation of the said compounds and intended use in therapy of them. Owing to the modulatory activity of the pyrrole derivatives on the nicotinic acetylcholine receptors, the invention finds application in the prophylaxis and therapy of disorders encompassing the involvement of cholinergic transmission in the central and peripheral nervous system.
    Type: Application
    Filed: January 31, 2012
    Publication date: November 21, 2013
    Applicant: LUPIN LIMITED
    Inventors: Neelima Sinha, Gourhari Jana, Navnath Popat Karche, Shridhar Keshav Adurkar, Girish Dhanraj Hatnapure, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 8586571
    Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
    Type: Grant
    Filed: October 17, 2008
    Date of Patent: November 19, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
  • Publication number: 20130303466
    Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.
    Type: Application
    Filed: October 18, 2011
    Publication date: November 14, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley, Alain D. Baron
  • Patent number: 8575197
    Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I): wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(?O)—, etc.; Z3a and Z3b are taken together ?O or ?S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: November 5, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroyuki Kai, Yoshiyuki Taoda, Takeshi Endoh, Kentaro Asahi, Hiroyuki Tobinaga
  • Publication number: 20130289075
    Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPB (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.
    Type: Application
    Filed: June 25, 2013
    Publication date: October 31, 2013
    Inventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
  • Publication number: 20130280305
    Abstract: The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.
    Type: Application
    Filed: November 2, 2012
    Publication date: October 24, 2013
    Inventors: Takeshi KUBOYAMA, Tomohiro ERA, Tomoyuki NAOI, Nobuhiro YAGI
  • Publication number: 20130231478
    Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
    Type: Application
    Filed: July 29, 2011
    Publication date: September 5, 2013
    Inventors: Ziao Xu, Yuanhai Zhao, Degang Li, Xiaoxiang Li
  • Patent number: 8524761
    Abstract: The present invention is directed to the compound 2-(4-(hydroxymethyl)phenoxy)-1-(3-(2-(trifluoromethyl)phenoxy)pyrrolidin-1-yl)ethanone, its use as an inhibitor of stearoyl CoA desaturase and to pharmaceutical compositions containing this compound.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: September 3, 2013
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Jin Li, Nicole Lee Kolosko
  • Publication number: 20130210933
    Abstract: The use of an esteramide compound, alone or as a mixture of the following formula (I): R1OOC-A-CONR2R3??(I) is described, wherein: A is a covalent bond or a methylene group —CH2—, R1 is an optionally substituted hydrocarbon group having from 1 to 36 carbon atoms, R2 and R3, either identical or different, are groups selected from a hydrogen atom and optionally substituted hydrocarbon groups comprising from 1 to 36 carbon atoms, R2 and R3 may form together a ring having the nitrogen atom to which they are bound, said ring being, if need be, substituted and/or having an additional heteroatom and R2 and R3 not being simultaneously hydrogens. Also described, are applications for using the esteramide compound as a solvent, a co-solvent, a coalescence agent, a crystallization inhibitor, a plasticizer or an agent for increasing biological activity.
    Type: Application
    Filed: March 16, 2011
    Publication date: August 15, 2013
    Applicant: RHODIA OPERATIONS
    Inventors: Massimo Guglieri, Thierry Vidal
  • Publication number: 20130184322
    Abstract: The invention comprises novel inhibitors of dipeptidyl peptidase IV (DPP-IV) with beta blocker activity, pharmaceutical compositions comprising therapeutically effective amounts of novel inhibitors of DPP-IV, and novel methods of treating medical conditions are provided. The novel inhibitors of DPP-IV described herein are useful in the treatment of neurological disorders, diabetes, inflammatory disorders such as arthritis, obesity, osteoporosis, hypertension, and glaucoma of such other enumerated conditions as can be treated with inhibitors of DPP-IV and beta blockers.
    Type: Application
    Filed: January 18, 2013
    Publication date: July 18, 2013
    Inventors: Weixing Li, Catherine Yang
  • Patent number: 8470855
    Abstract: Compounds of the general formulae (1) and (2) A-B-D-B?-A???(1) and A-B-D-E??(2) in which A and A? may be identical or different and are the residue in which X is S, O, CH2, CH2CH2, CH2O or CH2NH, and Y is H or CN, and * designates a chiral carbon atom preferably in S- or L-configuration; B and B? may be identical or different and are an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkylene residue, cycloalkylene residue, aralkylene residue, heterocycloalkylene residue, heteroarylalkylene residue, arylamidoalkylene residue, heteroarylamidoalkylene residue, unsubstituted or mono- or poly-substituted arylene residue or heteroarylene residue having one or more five-, six- or seven-membered ring(s); D is —S—S— or —Se—Se—; and E is the group —CH2—CH(NH2)—R9 or —CH2—*CH(NH2)—R9 respectively in which R9 is an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkyl residue, cycloalkyl residue, aralkyl residu
    Type: Grant
    Filed: November 10, 2006
    Date of Patent: June 25, 2013
    Assignee: IMTM GmbH
    Inventors: Siegfried Ansorge, Klaus Neubert, Ute Bank, Irene Reichstein, Jürgen Faust, Michael Täger, Petra Fuchs, Bianca Senns
  • Patent number: 8466145
    Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.
    Type: Grant
    Filed: January 7, 2010
    Date of Patent: June 18, 2013
    Assignee: Orchid Chemicals & Pharmaceuticals Limited
    Inventors: Gopalan Balasubramanian, Sukumar Sakamuri, Gajendra Singh, Sivanesan Dharmalingam, Franklin Pooppady Xavier, Shridhar Narayanan, Jeyamurugan Mookkan, Jeganatha Sivakumar Balasubramanian, Agneeswari Rajalingam, Jayanarayan Kulathingal
  • Publication number: 20130150578
    Abstract: The present invention relates to novel hypoglycemic compounds of formula (1) and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 1, 2011
    Publication date: June 13, 2013
    Applicant: CADILA PHARMACEUTICALS LIMITED
    Inventors: Bakulesh Mafatlal Khamar, Chandan Singh, Rajiv Indravadan Modi
  • Publication number: 20130137852
    Abstract: The present invention relates to process for preparation of novel compounds which are acting as inhibitors of dipeptidyl peptidase-IV enzyme and is depicted by the structural formula as given below: Formula VI. Which are useful in the treatment or prevention of diseases in which the dipeptidylpeptidase-IV enzyme is involved, such as diabetes and particularly type-2 diabetes.
    Type: Application
    Filed: August 3, 2011
    Publication date: May 30, 2013
    Applicant: Cadila Corporate Campus
    Inventors: Bakulesh Mafatlal Khamar, Nirav Kishorbhai Joshi, Chandan Hardhan Singh, Uday Rajaram Bapat, Bipin Dhanjibhai Gadhiya, Nirav Sureshbhai Sagar, Indravadan Ambalal Modi
  • Publication number: 20130137018
    Abstract: The invention provides a dye compound having a partial structure represented by the following formula (5): wherein in formula (5), Dye represents a dye structure; G1 represents NR or an oxygen atom; G2 represents a monovalent substituent group having an ?Es? value as a steric parameter of 1.5 or more; p represents an integer from 1 to 8; when p is 2 or greater, the two or more structures represented by p may be the same or different from each other; and R represents a hydrogen atom or a monovalent substituent group.
    Type: Application
    Filed: January 22, 2013
    Publication date: May 30, 2013
    Applicant: FUJIFILM CORPORATION
    Inventor: FUJIFILM CORPORATION
  • Publication number: 20130109721
    Abstract: The present disclosure relates to N-benzyl pyrrole compounds of formula (I) useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment or prevention of various disorders.
    Type: Application
    Filed: December 8, 2010
    Publication date: May 2, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Kevin Sprott, John Jeffrey Talley, Jane Yang, Bo Peng