Abstract: The invention provides methods and compositions for preparing amphetamine conjugates, such as lisdexamfetamine, homoarginine-D-amphetamine, and salts thereof. In one embodiment, the invention provides methods of preparing an amphetamine conjugate from a chloramphetamine intermediate.
Type:
Grant
Filed:
June 18, 2010
Date of Patent:
December 24, 2013
Assignee:
Cambrex Charles City, Inc.
Inventors:
Paul Alan Jass, Todd Jeffrey Johnson, Jason Scott Douglas, Matthew Wendell Schiesher
Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
Type:
Grant
Filed:
November 19, 2012
Date of Patent:
December 10, 2013
Assignee:
Calithera Biosciences Inc.
Inventors:
Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
Abstract: The present invention offers compounds or their salts expressed by formula (I) (in the formula, X indicates an alkyl group, or the like; Y indicates an alkyl group; Z indicates a respectively independent nitro group, or the like; n indicates any integer from 0 to 3; A indicates carbon atom, or the like, and hydrogen atom is bonded thereto in the case where the carbon atom is not substituted with Z; D indicates oxygen atom, or the like; W indicates hydrogen atom, or the like; R1 and R2 indicate respectively independent hydrogen atoms, or the like; R1 and R2 may be bonded, and may form a heterocycle together with the nitrogen atom between R1 and R2).
Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.
Type:
Grant
Filed:
September 14, 2012
Date of Patent:
November 12, 2013
Assignee:
President and Fellows of Harvard College
Abstract: A synthetic method is provided, wherein the method comprises stereoselectively reducing a ketone of a morphinone to form a reduced morphinone and optionally covalently attaching a water soluble polymer to the reduced morphinone.
Abstract: The present invention provides novel 1,5 and 1,3,5-substituted imidazole compounds in hydrophilic or lipophilic form, which are useful as angiotensin II ATI receptor antagonists suitable for transdermal delivery. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing compounds and their use in methods of treating hypertension and cardiovascular diseases.
Type:
Grant
Filed:
May 23, 2008
Date of Patent:
October 22, 2013
Assignee:
Eldrug S.A.
Inventors:
John Matsoukas, Michael Maragoudakis, Dimitrios Vlaxakos
Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
Type:
Grant
Filed:
January 24, 2012
Date of Patent:
October 15, 2013
Assignee:
Ambit Biosciences Corporation
Inventors:
Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
Abstract: The present invention relates to 4,5-ring annulated indole derivatives, compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. Wherein ring Z, of formula (I), is a cyclopentyl, cyclopentenyl, 5-membered heterocycloalkyl, 5-membered heterocycloalkenyl or 5-membered heteroaryl ring.
Type:
Grant
Filed:
December 17, 2007
Date of Patent:
October 15, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Kevin X. Chen, Srikanth Venkatraman, F. George Njoroge, Stuart B. Rosenblum, Charles A. Lesburg, Jose S. Duca, Neng-Yang Shih, Francisco Velazquez, Gopinadhan N. Anilkumar, Qingbei Zeng, Joseph A. Kozlowski
Abstract: The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.
Type:
Grant
Filed:
March 31, 2009
Date of Patent:
October 15, 2013
Assignee:
The General Hospital Corporation
Inventors:
Douglas E. Raines, Stuart A. Forman, Keith W. Miller, Syed Shaukat Husain, Joseph F. Cotten
Abstract: A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.
Type:
Grant
Filed:
December 14, 2010
Date of Patent:
October 15, 2013
Assignee:
Allergan, Inc.
Inventors:
Yariv Donde, Robert M. Burk, Michael Garst
Abstract: A process for aziridination of olefins using NaIO4/alkali metal bromide/H+/Chloramine-T combination in presence of dipolar aprotic solvent under ambient conditions to obtain aziridines is disclosed.
Type:
Grant
Filed:
October 7, 2011
Date of Patent:
October 15, 2013
Assignee:
Council of Scientific & Industrial Research
Abstract: A salt of (E)-N-{2-amino-phenyl)-3-{1-[4-(1-methyl-1 H-pyrazol-4-yl)-be?zenesulfonyl]-1 H-pyrrol-3-yl)-acrylamide selected from the group consisting of the hydrobromide, methansulfonate, hemi ethane-1,2-disulfonate, benzenesulfonate, toiuenesulfonate and 2-naphthalenesulfonate.
Type:
Grant
Filed:
March 11, 2009
Date of Patent:
October 15, 2013
Assignee:
4SC AG
Inventors:
Jürgen Volz, Martin Feth, Rolf-Peter Hummel, Matthias Müller, Thomas Maier, Bernd Müller
Abstract: The disclosed subject matter relate to a di-tert-butylphenyl alkylsulfonate compound, tert-butylphenyl alkylsulfonate compound, di-tert-butylphenyl arylsulfonate compound or tert-butylphenyl arylsulfonate compound useful as an intermediate raw material of a pharmaceutical, agricultural chemical, electronic material or polymer material and the like, or as a battery material, and also provides a nonaqueous electrolytic solution for a lithium secondary battery having superior cycle performance and other battery properties through the use thereof, and a lithium secondary battery. The disclosed embodiments further relate to a nonaqueous electrolytic solution for use as in a lithium secondary battery containing, in a nonaqueous electrolytic solution in which an electrolyte salt is dissolved in a nonaqueous solvent, 0.
Abstract: The present invention discloses a process for preparing eprosartan mesylate, in which eprosartan is dissolved or suspended in glacial acetic acid, then methanesulfonic acid is added and a solution of eprosartan mesylate in glacial acetic acid is obtained by stirring, a solid of eprosartan mesylate is precipitated by continuously stirring and then obtained by filtration, or a solid of eprosartan mesylate is obtained by concentrating the glacial acetic acid to dry, or a solid of eprosartan mesylate is obtained by adding dropwise an organic ester solvent into the glacial acetic acid under stirring to precipitate a crystal and separate the crystal.
Abstract: A sulfenamide vulcanization accelerator is provided that acts satisfactorily slowly on a vulcanization reaction, produces no carcinogenic nitrosamine, and is free from environmental hygiene problems such as bioaccumulation. Also provided is an N-alkyl-N-t-butylbenzothiazole-2-sulfenamide represented by formula [I]. The vulcanization accelerator is a vulcanization accelerator for rubber, containing this compound. Furthermore provided is a process for producing the vulcanization accelerator. wherein R represents methyl, ethyl, n-propyl, or n-butyl.
Type:
Grant
Filed:
December 24, 2008
Date of Patent:
October 1, 2013
Assignee:
Ouchi Shinko Chemical Industrial Co., Ltd.
Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF—or combinations thereof.
Type:
Grant
Filed:
November 9, 2009
Date of Patent:
September 24, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Joseph A. Kozlowski, Wensheng Yu, Michael K. C. Wong, Seong Heon Kim, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, De-Yi Yang, Robert Feltz, Aneta Maria Kosinski, Guowei Zhou, Razia K. Rizvi, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristin E. Rosner, M. Arshad Siddiqui, Liping Yang
Abstract: The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
Type:
Grant
Filed:
July 31, 2009
Date of Patent:
September 24, 2013
Assignee:
Simon Fraser University
Inventors:
David Jaro Vocadlo, Ernest John McEachern, Keith Stubbs
Abstract: The present invention provides processes for the stereoselective synthesis of 6-alpha-amino N-substituted morphinans. In particular, the invention provides processes for the reductive amination of 6-keto N-substituted morphinans by catalytic hydrogen transfer.
Type:
Grant
Filed:
June 10, 2010
Date of Patent:
August 27, 2013
Assignee:
Mallinckrodt LLC
Inventors:
Christopher W. Grote, Gary L. Cantrell, Joseph P. McClurg, Catherine E. Thomasson, Frank W. Moser