Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 514/375)
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Patent number: 8334311Abstract: Indoline compounds having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders are provided.Type: GrantFiled: July 25, 2011Date of Patent: December 18, 2012Assignee: Joyant Pharmaceuticals, Inc.Inventors: Gunnar James Hanson, Qi Wei, Charles Caldwell, Ming Zhou, Lai Wang, Susan Harran
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Patent number: 8334290Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: GrantFiled: October 30, 2006Date of Patent: December 18, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Julianne A. Hunt, Florida Kallashi, Jennifer Kowalchick, Dooseop Kim, Cameron J. Smith, Peter J. Sinclair, Ramzi F. Sweis, Gayle E. Taylor, Christopher F. Thompson, Liya Chen, Nazia Quraishi
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Publication number: 20120316106Abstract: Improved antibiotic analogs, and synergistic combinations of antibiotics designed based on structural crystallographic analysis, are provided as well as pharmaceutical compositions that include these improved analogs and synergistic combinations, along with methods for their production and use. The synergistic combinations target neighboring sites in the ribosome demonstrating the importance of the corresponding ribosomal sites for development of clinically-relevant synergistic antibiotics.Type: ApplicationFiled: December 29, 2010Publication date: December 13, 2012Applicant: YEDA RESEARCH AND DEVELOPMENT CO. LTD.Inventors: Ada Yonath, Chen Davidovich, Ella Zimmerman, Anat Bashan, Tamar Auerbach, Matthew Belousoff, Liqun Xiong, Dorota Klepacki, Alexander S. Mankin
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Patent number: 8324213Abstract: In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: GrantFiled: October 6, 2009Date of Patent: December 4, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Youngong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
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Publication number: 20120302601Abstract: The present invention is directed to topical ophthalmic compositions of a lipophilic compound and an oligomeric or polymeric carrier wherein the compositions are useful in the treatment and prevention of macular degeneration. The invention also includes methods of treating macular degeneration by using a topical ophthalmic composition of a lipophilic compound and an oligomeric or polymeric carrier.Type: ApplicationFiled: December 9, 2010Publication date: November 29, 2012Applicant: Neuron Systems, Inc.Inventors: Thomas A. Jordan, John Clifford Chabala, Gerald D. Cagle
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Publication number: 20120302613Abstract: The invention relates generally to novel antibiotics and their analogs, to processes for the preparation of these novel antibiotics, to pharmaceutical compositions comprising the novel antibiotics; and to methods of using the novel antibiotics to treat or inhibit various disorders.Type: ApplicationFiled: May 24, 2012Publication date: November 29, 2012Applicant: NOVOBIOTIC PHARMACEUTICALS LLCInventors: Aaron PEOPLES, Losee Lucy LING, Kim LEWIS, Slava S. EPSTEIN
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Patent number: 8318787Abstract: A prodrug that has a prodrug moiety that degrades into a compound having the general Formula I with R3 being an alcoholic moiety can be useful in therapies for neurodegenerative diseases as well as cancer. Accordingly, the prodrug compounds can have a structure of Formula I, analogs thereof, derivatives thereof, or salts thereof, wherein: A and B are sulfur or oxygen; R1 and R2, in para, meta, or ortho position, are independently halogen, alkyl, alkoxy, haloalkyl, where R1 and R2 independently are straight chain, branched, substituted or unsubstituted; and R3 is a prodrug moiety. As examples, the prodrug can have a structure of any of Formulas I-V, which as shown in the specification.Type: GrantFiled: August 10, 2009Date of Patent: November 27, 2012Assignee: University of KansasInventors: Roger A. Rajewski, Mehmet Tanol, Ingrid Gunda Georg, Michelle P. McIntosh
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Patent number: 8318728Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: GrantFiled: May 14, 2009Date of Patent: November 27, 2012Assignee: Hydra Biosciences, Inc.Inventor: Jayhong A. Chong
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Publication number: 20120295942Abstract: There are described 4-difluoromethoxyphenyl pyrazolo[5.1-b]oxazole derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.Type: ApplicationFiled: January 28, 2011Publication date: November 22, 2012Inventors: Nicholas James Devereux, Jeffrey McKenna
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Publication number: 20120295897Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: July 25, 2012Publication date: November 22, 2012Applicant: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Yurevna Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
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Patent number: 8309543Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium 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.Type: GrantFiled: May 23, 2012Date of Patent: November 13, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jesus E. Gonzalez, III, Andreas P. Termin, Esther Martinborough, Nicole Hilgraf
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Publication number: 20120283300Abstract: This application relates to a novel benzo-heterocycle derivative and more particularly, it relates a composition for preventing and treating cancer or for inhibiting metastasis comprising benzo-heterocycle derivative or pharmaceutically acceptable salts thereof as an active ingredient. The present inventors confirmed that KRS has an effect on cancer metastasis by facilitating cancer (or tumor) cell migration through interaction with 67LR, and also found that a substance inhibiting the interaction between KRS and 67LR can prevent and treat cancer by inhibiting cancer cell metastasis. Accordingly, the composition of the present invention can inhibit cancer metastasis, and thus provide a novel means for prevention and treatment of cancer.Type: ApplicationFiled: May 7, 2012Publication date: November 8, 2012Applicant: SNU R&DB FOUNDATIONInventors: Sunghoon Kim, Jin Woo Choi, Jin Young Lee, Dae Gyu Kim, Gyoon Hee Han, Jee Sun Yang, Chul Ho Lee
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Patent number: 8304409Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.Type: GrantFiled: December 11, 2009Date of Patent: November 6, 2012Assignee: Nicox S.A.Inventors: Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
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Publication number: 20120277240Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: February 17, 2011Publication date: November 1, 2012Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
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Publication number: 20120276047Abstract: The present invention relates to novel fused tricyclic compounds, compositions comprising at least one fused tricyclic compound, and methods of using fused tricyclic compounds for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: November 23, 2010Publication date: November 1, 2012Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge
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Publication number: 20120277259Abstract: The present invention relates to substituted benzofused derivatives, which can be used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.Type: ApplicationFiled: July 10, 2012Publication date: November 1, 2012Applicant: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant Atmaram GHARAT, Uday Mukund JOSHI, Neelima KHAIRATKAR-JOSHI, Suresh Mahadev KADAM
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Publication number: 20120270841Abstract: Diazonamide analogs having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders, and related pharmaceutical compositions are provided.Type: ApplicationFiled: April 15, 2012Publication date: October 25, 2012Inventors: Qi Wei, Ming Zhou, Xiaoming Xu, Charles Caldwell, Susan Harran, Lai Wang
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Publication number: 20120270863Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.Type: ApplicationFiled: October 21, 2010Publication date: October 25, 2012Applicant: Fibrotech Therapeutics Pty LtdInventors: Spencer John Williams, Steven Zammit, Darren James Kelly
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Patent number: 8293774Abstract: The present invention relates to an optically active (R)-aryloxypropionic acid amide compound which has high selectivity and safety for protecting a crop such as rice, wheat, barley and soy bean, and exhibits excellent herbicidal activity against weeds, and a herbicidal composition comprising the same.Type: GrantFiled: July 2, 2008Date of Patent: October 23, 2012Assignee: Kyung Nong CorporationInventors: Joo-kyung Kim, Dong-hoo Kim, Hyung-ho Kim, Kyung-hyun Kim, Cheol-su Yoon, In-cheon Hwang
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Patent number: 8293775Abstract: The present invention relates to benzoxazolone derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, in the treatment of movement disorders, in particular in Parkinson's disease.Type: GrantFiled: May 24, 2005Date of Patent: October 23, 2012Assignee: UCB Pharma, S.A.Inventors: Jean-Philippe Starck, Benoît Kenda
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Publication number: 20120264763Abstract: Indoline compounds having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders are provided.Type: ApplicationFiled: July 25, 2011Publication date: October 18, 2012Inventors: Gunnar James Hanson, Qi Wei, Charles Caldwell, Ming Zhou, Lai Wang, Susan Harran
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Publication number: 20120264794Abstract: Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.Type: ApplicationFiled: June 7, 2012Publication date: October 18, 2012Applicants: DANA-FARBER CANCER INSTITUTE, INC., COLORADO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Robert M. Williams, James E. Bradner, Albert Bowers, Tenaya Newkirk, Ann E. Youngman
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Publication number: 20120263675Abstract: The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.Type: ApplicationFiled: October 20, 2010Publication date: October 18, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Haiying Sun
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Patent number: 8277688Abstract: This invention relates to galvanic aluminum alloy powder-pigments coated with a semi-conducting corrosion inhibiting oxide and the process for preparing said coated powder-pigments in combination with film-forming binders for coating metal substrates to inhibit corrosion. The coated aluminum alloy powder-pigments are electrically active and prevent corrosion of metals which are more cathodic (electropositive) than the aluminum alloy pigments.Type: GrantFiled: July 27, 2011Date of Patent: October 2, 2012Assignee: The United States of America as represented by the Secretary of the NavyInventors: Craig Matzdorf, William Nickerson
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Publication number: 20120245186Abstract: Disclosed is a method for treating a subject with cancer, comprising administering to the subject an effective amount of paclitaxel or a paclitaxel analogue and an effective amount of a compound represented by the following structural formula: a tautomer, or a pharmaceutically acceptable salt thereof. The variables depicted in the structural formula are defined herein.Type: ApplicationFiled: October 19, 2010Publication date: September 27, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Ronald K. Blackman, Kevin Paul Foley, David Proia
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Publication number: 20120245209Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases (e.g., cancer and inflammation).Type: ApplicationFiled: December 7, 2010Publication date: September 27, 2012Applicant: NOVARTIS AGInventors: Dinesh Chikkanna, Mark Gary Bock, Clive McCarthy, Henrik Moebitz, Chetan Pandit, Ramulu Poddutorri
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Publication number: 20120238541Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: September 17, 2010Publication date: September 20, 2012Applicant: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
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Publication number: 20120238595Abstract: The invention provides compounds of formula (I) wherein u, d, v, m, n, R1, W, X, Y, and Z have any values defined herein, as well as salts thereof. The compounds have activity as anti-proliferative agents.Type: ApplicationFiled: November 5, 2010Publication date: September 20, 2012Applicants: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY, RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Edmond J. LaVoie, Joseph E. Rice, Suzanne G. Rzuczek, Daniel S. Pilch
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Patent number: 8268812Abstract: The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.Type: GrantFiled: January 10, 2011Date of Patent: September 18, 2012Assignee: Morphochem Aktiengesellschaft fül Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Hans Locher, Christine Schmitt
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Publication number: 20120232071Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Patent number: 8263632Abstract: The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is 0 or CH2; R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R10; R5 is H or OCH3; R10 is F or Cl; or a pharmaceutically acceptable salt or ester thereofType: GrantFiled: March 15, 2010Date of Patent: September 11, 2012Assignees: Vertex Pharmaceuticals Incoporated, MSD K.K.Inventors: Toshiharu Iwama, Nobuhiko Kawanishi, Michael Mortimore, Mitsuru Ohkubo, Tomoko Sunami
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Patent number: 8262938Abstract: Chromate-free corrosion-inhibiting coating compositions comprising film-forming binders and galvanic aluminum alloy powders prepared in an oxygen (oxidizing), nitrogen (inert) or nitrogen-hydrogen (reducing) atmosphere having particle sizes ranging up to 100 microns. The aluminum alloy powders having the formula: aluminum-zinc-X (AlZnX) wherein X is an element selected from the group consisting of indium, gallium, tin and bismuth. Improvement in corrosion protection is obtained by the addition of chemical inhibitors such as an azole or talcite clay to the coating which further inhibits the self-corrosion of the aluminum alloy and extends the corrosion protection of the metal substrate being protected.Type: GrantFiled: January 21, 2011Date of Patent: September 11, 2012Assignee: The United States of America, as represented by the Secretary of the Navy.Inventors: Craig Matzdorf, William Nickerson
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Publication number: 20120220611Abstract: Compounds of the formula I, the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases that are caused, mediated and/or propagated by angiogenesis. Compounds of the formula I are effective inhibitors of tyrosine kinases, in particular TIE-2 and VEGFR, and of Raf kinases.Type: ApplicationFiled: May 8, 2012Publication date: August 30, 2012Applicant: MERCK PATENT GMBHInventors: Wolfgang STÄHLE, Alfred JONCZYK, Wilfried RAUTENBERG
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Patent number: 8247398Abstract: The present invention relates to the use of zinc complexes of natural amino acids, especially L-arginine, L-lysine, L-ornithine, and other natural amino acids, in a molar ratio of about 1:2 (metal:amino acid), and formulations thereof. These pharmaceutical compositions offer better tolerated and faster acting regimens than common zinc salts (i.e., acetate, sulfate, etc.) for long term maintenance therapy of diseases caused by abnormal elevated copper levels, such as in Wilson's disease, inflammatory and fibrotic diseases and Alzheimer's disease.Type: GrantFiled: February 17, 2007Date of Patent: August 21, 2012Assignee: SSV Therapeutics, Inc.Inventor: Om P. Goel
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Publication number: 20120208827Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of benzimidazoles in the treatment of cancer.Type: ApplicationFiled: October 27, 2010Publication date: August 16, 2012Inventors: Steven Dock, Jason Hallman, Christopher Laudeman, Ronggang Liu, Aaron Miller, Michael Lee Moore, David Musso, Cynthia Parrish
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Publication number: 20120208856Abstract: This invention relates to benzoxazole compounds, compositions and devices for delivering them, processes for manufacturing them, and methods of using them in the treatment of Hepatitis C Virus.Type: ApplicationFiled: October 18, 2010Publication date: August 16, 2012Inventors: Paul Smith, Dawn N. Ward
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Publication number: 20120207729Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.Type: ApplicationFiled: April 24, 2012Publication date: August 16, 2012Applicant: DECODE GENETICS EHFInventors: Jasbir SINGH, Mark E. GURNEY, Alex BURGIN, Alexander KISELYOV, Munagala RAO
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Publication number: 20120208812Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: October 21, 2010Publication date: August 16, 2012Applicant: Janssen Pharmaceutica N.V.Inventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode-Johnson, Emily M. Stocking, Devin M. Swanson
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Patent number: 8242128Abstract: The invention relates to compounds of formula 1, the production and use thereof as a medicament for the treatment of diseases, particularly tumours and/or diseases caused, mediated or propagated by angiogenesis. The compounds of formula 1 are effective inhibitors of tyrosin kinases, particularly TIE-2 and VEGFR, and Raf-kinases.Type: GrantFiled: September 1, 2004Date of Patent: August 14, 2012Assignee: Merck Patent GmbHInventors: Wolfgang Stähle, Alfred Jonczyk, Wilfried Rautenberg
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Patent number: 8236837Abstract: The present invention provides a compound represented by the formula which is useful as an agent for the prophylaxis or treatment of diseases related to the action of melatonin, or a salt thereof and the like.Type: GrantFiled: March 14, 2011Date of Patent: August 7, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Osamu Uchikawa, Tatsuki Koike, Yasutaka Hoashi, Takafumi Takai
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Publication number: 20120196907Abstract: Novel diazonamide analogs having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders are provided.Type: ApplicationFiled: March 26, 2012Publication date: August 2, 2012Inventors: Gunnar James Hanson, Ming Zhou, Qui Wei, Charles Caldwell
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Patent number: 8227618Abstract: This invention provides an anorectic or anti-obesity composition comprising a compound of the formula (I): formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted lower alkyl, Y is —S(O)n- wherein n is 1 or 2, or —CO—, R2 is hydrogen or lower alkyl, R7 is hydrogen or lower alkyl, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, and Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like.Type: GrantFiled: April 23, 2010Date of Patent: July 24, 2012Assignee: Shionogi & Co., Ltd.Inventors: Takayuki Okuno, Masahiro Sakagami
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Patent number: 8222277Abstract: The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders comprising administration of novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent.Type: GrantFiled: December 28, 2010Date of Patent: July 17, 2012Assignee: NiCox S.A.Inventors: Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
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Patent number: 8217044Abstract: There are provided compounds of the formula wherein X, Y and R1 to R8 are as described herein and the enantiomers and pharmaceutically acceptable salts and esters thereof which compounds have anticancer activity.Type: GrantFiled: March 28, 2011Date of Patent: July 10, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jing Zhang, Zhuming Zhang
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Publication number: 20120172402Abstract: Substituted tricyclic diproline analogues of the formula (I): wherein the variables are as defined herein. Also disclosed are methods for the production thereof, the use thereof for the induction of an alpha-helix conformation in peptides and/or proteins, pharmaceuticals containing said compounds, methods for the production of a peptide library containing said compounds, and peptide libraries containing said compounds.Type: ApplicationFiled: July 9, 2010Publication date: July 5, 2012Applicants: FORSCHUNGSVERBUND BERLIN E.V., UNIVERSITAT ZU KOLNInventors: Hans-Günther Schmalz, Ronald Kuhne, Verena Hack, Cédric Reuter
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Publication number: 20120165331Abstract: The invention relates to compounds of the formula I A-D-C(R1)2—B??(I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: December 19, 2011Publication date: June 28, 2012Inventors: Sangamesh BADIGER, Dirk BEHNKE, Claudia BETSCHART, Vinod CHAUDHARI, Simona COTESTA, Samuel HINTERMANN, Andreas LERCHNER, Fatma LIMAM, Silvio OFNER, Chetan PANDIT, Jürgen WAGNER
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Publication number: 20120165377Abstract: An FGF21 production promoting agent containing, as an active ingredient, a compound represented by the following formula (1): wherein each of R1 and R2, which may be identical to or different from each other, represents, for example, a hydrogen atom; each of R3a, R3b, R4a, and R4b, which may be identical to or different from one another, represents, for example, a hydrogen atom or a halogen atom, or R3a and R3b or R4a and R4b may bond together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R5 (R5 represents, for example, a hydrogen atom or a C1-4 alkyl group); Y represents, for example, an oxygen atom, an S(O)l group (l is a number of from 0 to 2), or a carbonyl group; Z represents CH or N; n is a number of from 1 to 6; and m is a number from 2 to 6, a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: September 27, 2010Publication date: June 28, 2012Applicant: Kowa Co., Ltd.Inventors: Toshiaki Takizawa, Kentaro Murakami
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Publication number: 20120157434Abstract: The present invention provides heterocyclic compounds of the following formula I: or pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof useful as antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: ApplicationFiled: February 29, 2008Publication date: June 21, 2012Inventors: Mikhail Fedorovich Gordeev, Zhengyu Yuan, Jinqian Liu
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Patent number: 8202861Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium 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.Type: GrantFiled: August 9, 2004Date of Patent: June 19, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jesus E Gonzales, III, Andreas P Termin, Esther Martinborough, Nicole Zimmerman
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Publication number: 20120149718Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.Type: ApplicationFiled: December 13, 2011Publication date: June 14, 2012Inventors: Christine E. Brotherton-Pleiss, Keith A. M. Walker