Chalcogen Attached Indirectly To The Morpholine Ring By Acyclic Nonionic Bonding Patents (Class 514/238.8)
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Patent number: 11723910Abstract: Disclosed are compositions and methods for modulating endothelial barrier function.Type: GrantFiled: August 5, 2020Date of Patent: August 15, 2023Assignee: University of South FloridaInventors: Jerome William Breslin, Zeinab Yehia Khalil Motawe
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Patent number: 11578043Abstract: The present invention relates to a non-hygroscopic salt of the compound 2-(3-(4-propylheptyl)morpholino)ethan-1-ol having the INN name delmopinol. In particular, the invention relates to the citrate salt of delmopinol. The present invention also relates to pharmaceutical compositions comprising the citrate salt of delmopinol depicted below.Type: GrantFiled: August 23, 2018Date of Patent: February 14, 2023Assignee: Lundbeck Pharmaceuticals Italy S.P.A.Inventors: Carla De Faveri, Mariano Stivanello
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Patent number: 11427598Abstract: The present invention relates spiro-cyclic amine derivatives of the formula (I) wherein R1; R2; R3; Q; —W-T-; R5; Z; and A have the definitions provided in the claims; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) S1P receptor(s) is(are) involved.Type: GrantFiled: August 31, 2020Date of Patent: August 30, 2022Assignee: ABBVIE DEUTSCHLAND GMBH & CO. KGInventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Maria J. P. van Dongen, Nicolas J.-L. D. Leflemme, Adrian Hobson
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Patent number: 11324741Abstract: Disclosed are methods and compositions for treating visceral fat conditions and/or metabolic syndrome using combinations of naltrexone and bupropion.Type: GrantFiled: March 1, 2017Date of Patent: May 10, 2022Assignee: Nalpropion Pharmaceuticals LLCInventor: Gary D. Tollefson
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Patent number: 11186534Abstract: The disclosure provides chemical compounds possessing therapeutic and/or protective properties against oxidative damage. Methods of making such therapeutic and/or protective compounds and associated compositions are also provided, as are methods for their use, which include protecting cells from oxidative damage and/or inhibiting production of ROS in a cell or subject, as well as preventing or reducing the extent of tissue damage caused by an ischemic event in a subject at elevated risk of such an event.Type: GrantFiled: March 16, 2018Date of Patent: November 30, 2021Assignee: UNIVERSITY OF SOUTH ALABAMAInventors: Gary Piazza, Xi Chen, Herbert Weissbach, Shailaja Kesraju Allani
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Patent number: 10701939Abstract: Provided is a pyribencarb aqueous suspension agrochemical composition which contains an adjuvant for reinforcing the efficacy of pyribencarb, and which is capable of preventing a pharmaceutical preparation from becoming highly viscous or solidified and capable of providing a sufficient controlling effect with a small amount of pyribencarb. The aqueous suspension agrochemical composition includes: pyribencarb which is an agrochemically active component; an adjuvant for pyribencarb, which is one or more compounds selected from polyoxyalkylene siloxanes, polyoxyethylene/polyoxypropylene block copolymers, and polyoxyalkylene alkyl ethers; a nonionic-anionic surfactant which is a polyoxyalkylene aryl ether sulfuric acid salt and/or a polyoxyalkylene aryl ether phosphoric acid salt; and water.Type: GrantFiled: November 28, 2016Date of Patent: July 7, 2020Assignees: KUMIAI CHEMICAL INDUSTRY CO., LTD., NIPPON SODA CO., LTD.Inventors: Toshinobu Yamazaki, Toshio Sugimura, Koichi Ozaki
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Patent number: 10440949Abstract: The present invention is an aqueous suspension agrochemical composition characterized by containing pyribencarb which is an agrochemically active component, a polyacrylic acid salt, a surfactant, a thickener, and water. The present invention is a method for aerial spraying of an aqueous suspension agrochemical composition, which comprises spraying a diluted solution onto agricultural land or non-agricultural land at an amount of 8 to 32 kg/ha from an aircraft equipped with an agricultural preparation spraying function, the diluted solution being prepared by diluting the aqueous suspension agrochemical composition in water for spraying in an amount of 31 times or less the total amount of the composition on mass basis.Type: GrantFiled: November 28, 2016Date of Patent: October 15, 2019Assignees: KUMIAI CHEMICAL INDUSTRY CO., LTD., NIPPON SODA CO., LTD.Inventors: Yuichiro Ohta, Toshinobu Yamazaki
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Patent number: 9499526Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of neurologic diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of depression, Alzheimer's disease, multiple sclerosis, Batten disease, multiple sclerosis, Parkinson's disease (PD) and restless legs syndrome (RLS).Type: GrantFiled: April 19, 2013Date of Patent: November 22, 2016Assignee: CELLIX BIO PRIVATE LIMITEDInventor: Mahesh Kandula
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Patent number: 9416196Abstract: There is provided a composition for prophylaxis or treatment of vascular or valvular calcification including a dipeptidylpeptidase-4 (DPP-4) inhibitor. The DPP-4 according to one exemplary embodiment of the present disclosure is expressed at an increased level when blood vessels and valves are calcified, and the calcification decreases remarkably upon administration of the DPP-4 inhibitor. Therefore, the DPP-4 inhibitor can be useful in treatment or prophylaxis of blood vessels or valves.Type: GrantFiled: August 29, 2014Date of Patent: August 16, 2016Assignees: THE ASAN FOUNDATION, UNIVERSITY OF ULSAN FOUNDATION FOR INDUSTRY COOPERATIONInventors: Jae Kwan Song, Eun Ju Chang, Mi Jeong Kim, Bongkun Choi, Sahmin Lee
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Patent number: 9029371Abstract: The present invention relates to bisaryl (thio)morpholine derivatives of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof, with the proviso that the derivative of formula (I) is not 2-[4-(4-chlorophenoxy)-2-chlorophenyl]-4 -morpholineethanol. The compounds of the invention have affinity to S1 Preceptors and may be used in the treatment, alleviation or prevention of S1 Preceptor mediated diseases and conditions.Type: GrantFiled: July 8, 2011Date of Patent: May 12, 2015Assignee: Abbvie B.V.Inventors: Wouter I. Iwema Bakker, Raymond Bronger
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Patent number: 8987263Abstract: Basic esters of fatty alcohols of the general formula: R1-O—CO-A or pharmaceutically acceptable salts thereof, wherein R1 is C12-C24 alkyl or C10-C24 alkenyl, and A is a residue containing at least one acyclic or cyclic amino group and/or at least one heteroaromatic ring containing a tertiary or quaternary nitrogen atom, are anti-inflammatory and immunomodulatory agents, useful in the treatment of immunologically-mediated inflammation, as adjuvants for antigens involved in both cellular and humoral responses.Type: GrantFiled: October 9, 2003Date of Patent: March 24, 2015Inventors: Meir Shinitzky, Irun R. Cohen, Raanan Margalit, Yaacov Herzig, Jeffrey Sterling, Gyorgy Toth, Istvan Miskolczi, Ferenc Rantal, Tivadar Tamas
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Publication number: 20150010479Abstract: The present invention relates to the use of compositions in the prevention and/or treatment of infections by a number of microbial species associated with the pathological colonisation of wounds and periodontal lesions. The compositions of the invention comprise a morpholino compound in combination with a cetylpyridinium salt, which have been found by the present inventors to exert either a potentiating or synergistic antimicrobial effect on a range of microbes associated with the above pathological activity. Accordingly, the present invention provides novel uses of such compositions in treating or preventing infections or conditions in wounds or periodontal lesions, caused by the microbial species, in addition to methods for treating or preventing such disorders.Type: ApplicationFiled: March 20, 2013Publication date: January 8, 2015Inventor: Simon Youlton
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Publication number: 20150005306Abstract: Provided is a pharmaceutical composition for preventing or treating a cognitive impairment-related disease, the pharmaceutical composition including N-(2-hydroxyethyl)piperazine-N?(3-propane sulfonic acid), a pharmaceutically acceptable salt thereof or a derivative thereof, and donepezil, a pharmaceutically acceptable salt thereof or a derivative thereof. The composition may be used in preventing or treating a cognitive impairment-related disease.Type: ApplicationFiled: June 27, 2014Publication date: January 1, 2015Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Dong Jin KIM, Young Soo Kim, Hye Yun Kim, Hyun Jin Kim
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Patent number: 8906908Abstract: The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.Type: GrantFiled: November 19, 2012Date of Patent: December 9, 2014Assignees: Research Triangle Institute, Dignity Health, Virginia Commonwealth UniversityInventors: F. Ivy Carroll, Bruce E. Blough, Hernan A. Navarro, S. Wayne Mascarella, Ana Zamfira Muresan, M. Imad Damaj, Ronald J. Lukas
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Patent number: 8895077Abstract: The present invention relates to methods for preventing or treating infectious diseases caused by extracellular microorganisms, such as bacteria and fungi, by systemically administering to a patient a compound containing gallium. The extracellular microorganisms targeted by the present methods include methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecalis (VRE), E. coli O157:H7, fluoroquinolone-resistant Salmonella typhi, and the like. Furthermore, in the present methods, gallium compounds can be co-administered with one or more conventional antimicrobial agents to treat infectious diseases with reduced risks of creating multi-drug resistant pathogens. The methods of the present invention is also applicable to those microorganisms, such as ulcer-causing Helicobacter pylori, complete eradication of which so far has been difficult to achieve.Type: GrantFiled: March 28, 2008Date of Patent: November 25, 2014Assignee: Mount Sinai School of MedicineInventors: Daniel P. Perl, Sharon Moalem
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Patent number: 8877747Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.Type: GrantFiled: October 21, 2009Date of Patent: November 4, 2014Assignee: Korea Research Institute of Chemical TechnologyInventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
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Publication number: 20140271955Abstract: Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicants: The Scripps Research Institute, The California Institute for Biomedical ResearchInventors: Peter G. SCHULTZ, Arnab K. CHATTERJEE, Shoutian ZHU, Joshua PAYETTE, Hongchul YOON, Baiyuan YANG
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Publication number: 20140243334Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: May 5, 2014Publication date: August 28, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
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Publication number: 20140194416Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins UniversityInventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
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Patent number: 8772336Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: October 11, 2012Date of Patent: July 8, 2014Assignees: Merck Frosst Canada Ltd., Axys Pharmaceuticals, Inc.Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra I. Baskaran
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Publication number: 20140163017Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 19, 2013Publication date: June 12, 2014Applicant: UNIVERSITY OF UTAHInventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
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Publication number: 20140142107Abstract: Antimicrobial agents, compositions that include the agent(s) and use(s) thereof are provided. Also disclosed are screening assays for identifying antimicrobial agents.Type: ApplicationFiled: September 4, 2013Publication date: May 22, 2014Applicant: University of MassachusettsInventors: Paul Kaufman, Jessica Lopes Da Rosa-Spiegler, Reeta Prusty Rao, Ahmed Fazly
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Patent number: 8691977Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.Type: GrantFiled: August 22, 2011Date of Patent: April 8, 2014Assignee: Neupharma, Inc.Inventors: Xiangping Qian, Yong-Liang Zhu
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Publication number: 20140094445Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: August 15, 2012Publication date: April 3, 2014Applicant: University of Utah Research FoundationInventors: Hariprasad Vakayalapati, Venkataswamy Soma, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
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Publication number: 20140093490Abstract: The present invention investigate the two modes of glutamate release and the releasing rate of glutamate, and thus can provide a useful technique for neuron protection and acceleration of neurotransmission by controlling the glutamate release in astroctye. Thus, the present invention provides an inhibitor of the fast-mode release and/or the slow-mode release of astrocytic glutamate, a screening method of the inhibitor and a pharmaceutical composition or method of ameliorating, preventing and/or treating the disease associated with the over-release of glutamate via the Ca2+-activated anion channel, with the inhibition of fast-mode glutamate release.Type: ApplicationFiled: July 23, 2013Publication date: April 3, 2014Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Changjoon Justin LEE, Soo Jin OH, Eun Mi HWANG, Dong Ho WOO
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Publication number: 20140080833Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.Type: ApplicationFiled: November 11, 2013Publication date: March 20, 2014Applicant: MannKind CorporationInventors: Gary A. Flynn, Sandra A. Lee, Mary Faris, David W. Brandt, Subrata Chakravarty
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Patent number: 8604031Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.Type: GrantFiled: May 18, 2007Date of Patent: December 10, 2013Assignee: MannKind CorporationInventors: Gary A. Flynn, Sandra Aeyoung Lee, Mary Faris, David William Brandt, Subrata Chakravarty
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Publication number: 20130323286Abstract: This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.Type: ApplicationFiled: November 7, 2012Publication date: December 5, 2013Applicant: PROGENICS PHARMACEUTICALS, INC.Inventor: Progenics Pharmaceuticals, Inc.
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Publication number: 20130310384Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.Type: ApplicationFiled: October 4, 2011Publication date: November 21, 2013Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Corinne E. Augelli-Szafran, Dai Lu, Hanxun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe
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Patent number: 8546392Abstract: The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.Type: GrantFiled: March 27, 2008Date of Patent: October 1, 2013Assignee: Universitaet des SaarlandesInventors: Rolf Hartmann, Martin Frotscher, Sandrine Oberwinkler, Erika Ziegler, Josef Messinger, Heinrich-Hubert Thole
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Publication number: 20130237542Abstract: The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.Type: ApplicationFiled: October 17, 2011Publication date: September 12, 2013Applicants: DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION, KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGYInventors: Kyeong Lee, Mi Sun Won, Hwan Mook Kim, Song Kyu Park, Kiho Lee, Ki Hoon Lee, Chang Woo Lee, Jung Joon Lee, Kyung Sook Chung, Bo Kyung Kim, Yinglan Jin, Seung-hee Lee
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Publication number: 20130231341Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.Type: ApplicationFiled: January 11, 2013Publication date: September 5, 2013Applicant: HIGH POINT PHARMACEUTICALS, LLCInventor: Soren Ebdrup
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Publication number: 20130196998Abstract: The present invention relates to spiro-cyclic amine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms, monocyclic heterocycle optionally independently substituted with halogen, (1-6C)aType: ApplicationFiled: July 8, 2011Publication date: August 1, 2013Applicant: AbbVie B.V.Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Maria J.P. van Dongen, Nicolas J.-L.D. Leflemme
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Patent number: 8399456Abstract: Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: GrantFiled: April 21, 2010Date of Patent: March 19, 2013Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Marie Chantal Siu-Ying Tran, Erik Dean Raaum
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Publication number: 20130065889Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: October 26, 2012Publication date: March 14, 2013Applicant: AXIKIN PHARMACEUTICALS, INC.Inventor: Axikin Pharmaceuticals, Inc.
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Publication number: 20130035312Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: ApplicationFiled: October 11, 2012Publication date: February 7, 2013Applicants: Axys Pharmaceuticals, Inc., Merck, Sharp & Dohme, Corp.Inventors: Merck, Sharp & Dohme, Corp., Axys Pharmaceuticals, Inc.
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Patent number: 8288444Abstract: A device for iontophoretically delivering a charged curcuminoid across the skin of an Alzheimer's Disease patient.Type: GrantFiled: June 29, 2011Date of Patent: October 16, 2012Assignee: Codman & Shurtleff, Inc.Inventors: Sean Lilienfeld, Thomas M DiMauro
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Publication number: 20120225848Abstract: Methods for treating an individual to improve cognitive function are provided. In the subject methods, an effective amount of a GABAB antagonist, or a blocker of Kir3.2 potassium channels, is administered to the individual, resulting in an improvement in cognitive function of the host. The subject methods find use in a variety of different applications.Type: ApplicationFiled: September 17, 2010Publication date: September 6, 2012Inventors: Alexander M. Kleschevnikov, William C. Mobley
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Publication number: 20120225108Abstract: Morpholino compounds of Formula (I) wherein R1 is a straight or branched alkyl group containing 8 to 16 carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing 2 to 10 carbon atoms, substituted with a hydroxy group except in the alpha-position, or pharmaceutically acceptable salts thereof, have been found to be surprisingly effective at promoting the healing of a wound.Type: ApplicationFiled: May 21, 2012Publication date: September 6, 2012Applicant: SINCLAIR PHARMACEUTICALS LIMITEDInventor: OLOF TORGNY SJODIN
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Publication number: 20120220552Abstract: The present disclosure relates to (thio)morpholine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, —SO2-(1-4C)alkyl, —CO-(1-4C)alkyl, —CO—O-(1-4C)alkyl, —NH—CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl; A is selected from —Type: ApplicationFiled: August 27, 2010Publication date: August 30, 2012Inventors: Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Axel Stoit, Harmen Mons, Eric Ronken, Elizabeth Van Der Kam, Jurjen Frankena
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Patent number: 8252788Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed, wherein a dashed line represents the presence or absence of a bond; and, wherein Y, A, R, D, and n are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 13, 2009Date of Patent: August 28, 2012Assignee: Allergan, Inc.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20120178732Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: December 6, 2011Publication date: July 12, 2012Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Publication number: 20120101039Abstract: A compound of general formula I their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, methods of treating diseases with said compounds, and the use of said compounds in the manufacture of medicaments.Type: ApplicationFiled: May 26, 2010Publication date: April 26, 2012Applicant: LEO PHARMA A/SInventors: Jef Fenscholdt, Thomas Høyer, Xifu Liang, Sophie Elisabeth Havez
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Publication number: 20120094977Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: ApplicationFiled: May 25, 2011Publication date: April 19, 2012Applicant: Dendreon CorporationInventors: Sateesh K. Natarajan, Ofir Moreno, Thomas J. Graddis, David F. Duncan, Reiner Laus, Feng Chen
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Publication number: 20120052019Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.Type: ApplicationFiled: August 22, 2011Publication date: March 1, 2012Inventors: Xiangping Qian, Yong-Liang Zhu
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Publication number: 20120052026Abstract: Antiplaque oral compositions are provided that contain an orally acceptable carrier and an antibacterial effective amount of the compound of formula (I). In various embodiments, the compositions contain from about 0.001% to about 10% by weight of the compound of formula (I).Type: ApplicationFiled: November 9, 2011Publication date: March 1, 2012Applicant: COLGATE-PALMOLIVE COMPANYInventors: Ravi Subramanyam, Prem Sreenivasan
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Publication number: 20120035175Abstract: The present invention relates to a salt selected from the group comprising the N-methyl-D-glucamine salt (NMG), the diethylamine salt (DEA) salt, the magnesium salt, the tromethamine salt, the choline salt, the L-arginine salt, the zinc salt, and the 4-(2-hydroxyethyl)morpholine (HEM) salt of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1; and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.Type: ApplicationFiled: July 1, 2011Publication date: February 9, 2012Applicant: 4SC AGInventors: Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT
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Publication number: 20120035176Abstract: Analogs of 3-O-acetyl-11-keto-beta-boswellic acid and their method of preparation are presented. The analogs may be used as anti-inflammatory and anti-cancer agents. The compounds inhibit 5-lipoxygenase enzyme and various cell lines related to inflammation as well as to cancer showing a significantly better efficacy when compared to the normal boswellic acids. The analogs are capable of controlling and treating various inflammatory diseases and cancers.Type: ApplicationFiled: September 30, 2011Publication date: February 9, 2012Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Subbaraju Gottumukkala, Trimurtulu Golakoti, Krishanu Sengupta
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Publication number: 20120022070Abstract: Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors are disclosed. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases and conditions, such as inflammation and neurodegenerative disorders. Methods of treating and preventing cancer and other Hsp90 related diseases and conditions are disclosed that include administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. Methods of preparing the novel Hsp90 inhibitors are also provided.Type: ApplicationFiled: October 6, 2009Publication date: January 26, 2012Applicant: EMORY UNIVERSITYInventors: Jaeki Min, Pahk Thepchatri, Yuhong Du, Dennis C. Liotta, Haian Fu
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Publication number: 20120015942Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: July 18, 2011Publication date: January 19, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma