Plural Alicyclic Rings In R Patents (Class 514/623)
  • Patent number: 9735800
    Abstract: Provided are, among other things, systems, apparatuses, methods and techniques for converting a discrete-time quantized signal into a continuous-time, continuously variable signal. An exemplary converter preferably includes: (1) multiple oversampling converters, each processing a different frequency band, operated in parallel; (2) multirate (i.e., polyphase) delta-sigma modulators (preferably second-order or higher); (3) multi-bit quantizers; (4) multi-bit-to-variable-level signal converters, such as resistor ladder networks or current source networks; (5) adaptive nonlinear, bit-mapping to compensate for mismatches in the multi-bit-to-variable-level signal converters (e.g., by mimicking such mismatches and then shifting the resulting noise to a frequently range where it will be filtered out by a corresponding bandpass (reconstruction) filter); (6) multi-band (e.g.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: August 15, 2017
    Assignee: Syntropy Systems, LLC
    Inventor: Christopher Pagnanelli
  • Patent number: 9700580
    Abstract: A method of treating humans with cancer by intravenously administering a single dose of arsenic trioxide in a phosphate buffered saline solution having a pH less than 8.0 in a dosage amount of between 6.0 and 7.0 mg/Kg according to the weight of the patient.
    Type: Grant
    Filed: June 14, 2016
    Date of Patent: July 11, 2017
    Inventors: Marguerite Harning, Robert Koppany
  • Patent number: 8916194
    Abstract: A controlled release pharmaceutical compositions comprising Milnacipran or pharmaceutically acceptable salts thereof is provided. The pharmaceutical composition comprises an immediate release core comprising Milnacipran or pharmaceutically acceptable salts thereof, pharmaceutically acceptable excipients and a coating on the immediate release core comprising rate controlling agents.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: December 23, 2014
    Assignee: Lupin Limited
    Inventors: Shirishkumar Kulkarni, Rajesh Kulkarni, Pandharinath Jadhav, Ashish Tiwari
  • Publication number: 20140256782
    Abstract: Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic is visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 11, 2014
    Applicant: Bikam Pharmaceuticals, Inc.
    Inventors: David S. Garvey, Gregory J. Larosa, Jeremy R. Greenwood, Leah L. Frye, Tan Quach, Jamie B. Cote, Judd Berman
  • Patent number: 8809280
    Abstract: The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted ? amino acid, each of the substituting groups in the ? amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: August 19, 2014
    Assignee: Lytix Biopharma AS
    Inventors: Morten Strom, Terkel Hansen, Martina Havelkova, Veronika Torfoss
  • Patent number: 8779003
    Abstract: Disclosed herein is a method for prolonging analgesic effect of a membrane permeable local anesthetic in a subject in need thereof. The method uses cinnamaldehyde as an adjuvant which, when administered prior to or simultaneously with the administration of a local anesthetic, prolongs the analgesic effect of the local anesthetic. Also disclosed herein is a method for providing analgesic effect in a subject in need thereof. The method uses cinnamaldehyde as an analgesic compound which, when administered alone to the subject in an analgesically effective amount, provides the analgesic effect.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: July 15, 2014
    Assignee: Mackay Memorial Hospital
    Inventor: Yu-Chun Hung
  • Publication number: 20140121217
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein A, Y, L, R1, W1 and W2 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: January 2, 2014
    Publication date: May 1, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Jun Jiang, Yu Xie
  • Patent number: 8703824
    Abstract: The present invention discloses novel cationic amphiphiles containing mannose-mimicking shikimic and quinic acid head-groups and a process for preparing cationic amphiphiles with mannose-mimicking polar head-groups such as, shikimic and quinic acids. The findings described herein also demonstrate that compounds of the present invention can target model DNA vaccines to antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs), via mannose receptors expressed on the cell surface of APCs. The cationic amphiphiles disclosed herein show enhanced cellular and humoral immune response compared to their mannosyl counterpart in dendritic cell (DC, the most professional APC) based genetic immunization in mice. Cationic amphiphiles with mannose-mimicking quinic and shikimic acid head-groups described in the present invention are likely to find future applications in the field of genetic immunization.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: April 22, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ramishetti Srinivas, Arup Garu, Sachin B. Agawane, Arabinda Chaudhuri
  • Publication number: 20140088188
    Abstract: Disclosed herein are novel C13-hydroxy 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: March 27, 2014
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventors: Xin JIANG, Christopher F. BENDER, Melean VISNICK
  • Patent number: 8653125
    Abstract: The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted aryl or heterocyclyl; a combination of X and Y is a combination selected from (X, Y)?(C(?O)N(R1), C(?O)N(R2)), (C(?O)N(R1), imidazole-1,3-diyl), (N(R1), C(?O)N(R2)), (O, C(?O)N(R2)), (C(R3)(R4), N(R2)) or (a single bond, C(?O)N(R2)); R1, R2 and R3 are independently hydrogen or substituted or unsubstituted alkyl; R5 is substituted or unsubstituted aryl or heterocyclyl; R6 is halogen, oxo, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy; m is 0 or 1; and n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or fused bicyclic heterocycle.
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: February 18, 2014
    Assignee: Shionogi Co., Ltd.
    Inventors: Hiroshi Yoshida, Keisuke Tonogaki, Masahiro Sakagami, Kenji Takaya
  • Publication number: 20130345254
    Abstract: Disclosed are the CCR2 antagonists of Formula I: I or pharmaceutically acceptable salts thereof, wherein A, B, R, and R6 are as defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.
    Type: Application
    Filed: March 14, 2012
    Publication date: December 26, 2013
    Inventors: Anilkumar G. Nair, Joseph A. Kozlowski
  • Publication number: 20130203712
    Abstract: In one aspect, the invention relates methods for inhibiting or preventing muscle atrophy or increasing muscle mass by providing to a subject in need thereof an effective amount of ursolic acid, a derivative thereof, or an analog of the ursane scaffold. 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: Application
    Filed: May 19, 2011
    Publication date: August 8, 2013
    Applicant: University of Iowa Research Foundation
    Inventors: Christopher M. Adams, Steven D. Kunkel
  • Publication number: 20130156854
    Abstract: A controlled release pharmaceutical compositions comprising Milnacipran or pharmaceutically acceptable salts there—of is provided. The pharmaceutical composition comprises an immediate release core comprising Milnacipran or pharmaceutically acceptable salts thereof, pharmaceutically acceptable excipients and a coating on the immediate release core comprising rate controlling agents.
    Type: Application
    Filed: August 26, 2011
    Publication date: June 20, 2013
    Applicant: LUPIN LIMITED
    Inventors: Shirishkumar Kulkarni, Rajesh Kulkarni, Pandharinath Jadhav, Ashish Tiwari
  • Patent number: 8445540
    Abstract: The present invention provides methods for the regulation of osteopontin activity in a subject as well as for treating or preventing conditions associated with an increased activity of osteopontin activity in a subject.
    Type: Grant
    Filed: March 10, 2008
    Date of Patent: May 21, 2013
    Assignee: Pathologica LLC
    Inventors: Kenneth G. Hadlock, Hope Lancero, Stephanie Yu, Hien Kim Do
  • Publication number: 20130045177
    Abstract: An excellent potential-dependent cation channel inhibitor or an excellent masking agent is provided.
    Type: Application
    Filed: April 26, 2011
    Publication date: February 21, 2013
    Inventors: Hiroko Takatoku, Kentaro Kumihashi, Daisuke Yamazaki
  • Publication number: 20130035296
    Abstract: The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted ? amino acid, each of the substituting groups in the ? amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.
    Type: Application
    Filed: November 2, 2010
    Publication date: February 7, 2013
    Applicant: LYTIX BIOPHARMA AS
    Inventors: Morten Strom, Terkel Hansen, Martina Havelkova, Veronika Torfoss
  • Publication number: 20130030055
    Abstract: Described herein are compositions including at least one prostaglandin or prostamide and methods for using these compositions for increasing hair growth on the scalp eyebrow growth.
    Type: Application
    Filed: March 23, 2011
    Publication date: January 31, 2013
    Applicant: ALLERGAN, INC.
    Inventors: John G. Walt, David F. Woodward, Amanda M. Vandenburgh
  • Publication number: 20120322770
    Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.
    Type: Application
    Filed: August 21, 2012
    Publication date: December 20, 2012
    Inventor: Robert P. RICCIARDI
  • Patent number: 8314270
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Grant
    Filed: September 9, 2010
    Date of Patent: November 20, 2012
    Assignee: Abbott Laboratories
    Inventors: James T. Link, Qi Shuai, Martin Winn, Hong Yong
  • Publication number: 20120238634
    Abstract: Described herein are chemical compounds and pharmaceutical compositions, including novel chemical compounds and pharmaceutical compositions thereof, useful in the treatment of various diseases and disease states. Also described are methods of synthesizing natural products and novel, structurally-related chemical compounds. More particularly, disclosed are new analogs of and processes for the preparation of compounds and pharmaceutical compositions thereof useful in the treatment of, for example, inflammation, cancer, multiple myeloma, cachexia, cardiovascular disease, anti-infectious, diabetes, otitis media, sinusitis and transplant rejection.
    Type: Application
    Filed: March 9, 2012
    Publication date: September 20, 2012
    Applicant: NEREUS PHARMACEUTICALS, INC.
    Inventors: Michael A. Palladino, Emmanuel A. Theodorakis, Venkat Rami Reddy Macherla, Ta-Hsiang Chao, Young-Ger Suh
  • Publication number: 20120203102
    Abstract: This invention is directed to non-benzenoid aromatic compounds. Other aspects include methods of using non-benzenoid aromatic compounds for imaging and phototherapeutic uses thereof. Non-benzenoid compounds provided herein generally have one or more substituent groups which allow tailoring of the spectral properties or provide photoreactivity or targeting ability.
    Type: Application
    Filed: September 10, 2010
    Publication date: August 9, 2012
    Applicant: MALLINCKRODT LLC
    Inventor: Raghavan Rajagopalan
  • Publication number: 20120122870
    Abstract: Ischemia-reperfusion injury remains a primary cause of morbidity and mortality in individuals who experience disruption of normal blood flow to one or more major organs. For example, there are no clinically proven strategies that prevent acute renal failure following cardiac surgery. The present invention provides a variety of methods for the treatment or prevention of ischemia-reperfusion injury. In one aspect of the invention, a method for treating or preventing ischemia-reperfusion injury includes administering to a subject an effective amount of a sphingosine kinase inhibitor. Sphingosine kinase inhibitors are very effective in the protection against IR-induced acute renal failure and liver failure. Moreover, the effects occur very early after administration, requiring only a very short time of treatment. Toxicology studies with sphingosine kinase inhibitors demonstrate that they have low toxicity, even in long-term treatment.
    Type: Application
    Filed: May 10, 2010
    Publication date: May 17, 2012
    Applicants: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT, APOGEE BIOTECHNOLOGY CORPORATION
    Inventors: Charles D. Smith, Zhi Zhong, Lynn W. Maines
  • Publication number: 20120095004
    Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.
    Type: Application
    Filed: October 19, 2011
    Publication date: April 19, 2012
    Applicant: APOGEE BIOTECHNOLOGY CORPORATION
    Inventors: Charles D. Smith, Kevin J. French, Yan Zhuang
  • Patent number: 8133915
    Abstract: Described herein are chemical compounds and pharmaceutical compositions, including novel chemical compounds and pharmaceutical compositions thereof, useful in the treatment of various diseases and disease states. Also described are methods of synthesizing natural products and novel, structurally-related chemical compounds. More particularly, disclosed are new analogs of and processes for the preparation of compounds and pharmaceutical compositions thereof useful in the treatment of, for example, inflammation, cancer, multiple myeloma, cachexia, cardiovascular disease, anti-infectious, diabetes, otitis media, sinusitis and transplant rejection.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: March 13, 2012
    Assignees: Nereus Pharmaceuticals, Inc., The Regents of the University of California
    Inventors: Michael A. Palladino, Emmanuel A. Theodorakis, Venkat Rami Reddy Macherla, Ta-Hsiang Chao, Young-Ger Suh
  • Publication number: 20120053141
    Abstract: The present invention pertains to novel uses of glycyrrhetinic acid (GA), glycyrrhizic acid (GLA) and related compounds for prevention and/or treatment of pulmonary fibrosis, in particular, irradiation-induced pulmonary fibrosis. Also embodied are therapeutic uses of prodrugs, metabolites, derivatives (e.g., acids, esters and ethers), and salts of glycyrrhetinic acid (GA) and glycyrrhizic acid (GLA). The present invention also provides for therapeutic or pharmaceutical compositions comprising a compound of the invention in a form that can be combined with a pharmaceutically acceptable carrier.
    Type: Application
    Filed: August 25, 2010
    Publication date: March 1, 2012
    Inventors: Lurong ZHANG, Weijian Zhang, Jianhua Xu, Shanmin Yang
  • Publication number: 20110319454
    Abstract: The invention provides well defined compounds having FPRL-1 agonist or antagonist activity. As such, the compounds of the invention are useful for treating a variety of ocular disorders.
    Type: Application
    Filed: June 24, 2011
    Publication date: December 29, 2011
    Applicant: ALLERGAN, INC.
    Inventors: Richard L. Beard, John E. Donello, Vidyasagar Voligonda, Michael E. Garst
  • Patent number: 8053435
    Abstract: The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.
    Type: Grant
    Filed: November 1, 2007
    Date of Patent: November 8, 2011
    Assignees: Korea Research Institute of Chemical Technology, Crystalgenomics, Inc.
    Inventors: Cheol Hae Lee, Hee Jung Jung, Jae Hak Kim, Won Jang Jeong, Joong Myung Cho, Seong Gu Ro, Young Lan Hyun, Cheol Soon Lee, Dongkyu Shin
  • Publication number: 20110160309
    Abstract: Described herein are chemical compounds and pharmaceutical compositions, including novel chemical compounds and pharmaceutical compositions thereof, useful in the treatment of various diseases and disease states. Also described are methods of synthesizing natural products and novel, structurally-related chemical compounds. More particularly, disclosed are new analogs of and processes for the preparation of compounds and pharmaceutical compositions thereof useful in the treatment of, for example, inflammation, cancer, multiple myeloma, cachexia, cardiovascular disease, anti-infectious, diabetes, otitis media, sinusitis and transplant rejection.
    Type: Application
    Filed: January 14, 2011
    Publication date: June 30, 2011
    Applicant: Nereus Pharmaceuticals, Inc.
    Inventors: Michael A. Palladino, Emmanuel A. Theodorakis, Venkat Rami Reddy Macherla, Ta-Hsiang Chao, Young-Ger Suh
  • Publication number: 20110145970
    Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.
    Type: Application
    Filed: August 26, 2009
    Publication date: June 23, 2011
    Applicant: BASF SE
    Inventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
  • Publication number: 20110092582
    Abstract: Novel terpenes and macrocycles are activators of TGR5 and can be used for the prevention and/or treatment of Diabetes Type 2, obesity, neuropathy and/or nephropathy.
    Type: Application
    Filed: May 8, 2009
    Publication date: April 21, 2011
    Inventors: Delphine Jacquot, Oliver Poeschke, Christa Burger
  • Patent number: 7888355
    Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: February 15, 2011
    Assignee: Burnham Institute for Medical Research
    Inventors: Ze′ev A. Ronai, Anindita Bhoumik, Nicholas D. P. Cosford, Russell Dahl
  • Publication number: 20100305129
    Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.
    Type: Application
    Filed: August 11, 2010
    Publication date: December 2, 2010
    Applicant: Burnham Institute for Medical Research
    Inventors: Zéev A. Ronai, Anindita Bhoumik, Nicholas D.P. Cosford, Russell Dahl
  • Patent number: 7776894
    Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: August 17, 2010
    Assignee: Burnham Institute for Medical Research
    Inventors: Ze'ev A. Ronai, Anindita Bhoumik, Nicholas D. P. Cosford, Russell Dahl
  • Publication number: 20100152179
    Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.
    Type: Application
    Filed: August 21, 2008
    Publication date: June 17, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Yixian Chen, Jurgen Dinges, Karla Drescher, Peer Jacobson, Hwan-soo Jae, Ravi Kurukulasuriya, James T. Link, David J. Madar, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Lynne E. Rueter, Qi Shuai, Bryan K. Sorensen, Jiahong Wang, Karsten M. Wicke, Martin Winn, Dariusz Wodka, Vince Yeh, Hong Yong
  • Publication number: 20100087413
    Abstract: The present invention relates to the use of an 11-?-HSD-type 1 and or type 2 inhibitor for the manufacture of a pharmaceutical agent for the prevention and/or treatment of inflammation-induced and/or immune-mediated loss of bone and/or cartilage.
    Type: Application
    Filed: September 21, 2004
    Publication date: April 8, 2010
    Inventor: Thomas Wilckens
  • Patent number: 7645780
    Abstract: Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.
    Type: Grant
    Filed: June 6, 2006
    Date of Patent: January 12, 2010
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Varghese John, Michel Maillard, James P. Beck, Eric T. Baldwin, Robert Hughes, Shon R. Pulley, Ruth T. TenBrink
  • Patent number: 7560591
    Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta p
    Type: Grant
    Filed: April 30, 2008
    Date of Patent: July 14, 2009
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Simona Zanzola, Roberto Artusi, Lucio Claudio Rovati
  • Patent number: 7511175
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Grant
    Filed: January 5, 2006
    Date of Patent: March 31, 2009
    Assignee: Abbott Laboratories
    Inventors: Jyoti R. Patel, Qi Shuai, James T. Link, Jeffrey J. Rohde, Jurgen Dinges, Bryan K. Sorensen, Martin Winn, Hong Yong, Peer B. Jacobson, Michael E. Brune
  • Publication number: 20090054426
    Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.
    Type: Application
    Filed: August 21, 2008
    Publication date: February 26, 2009
    Applicant: ABBOTT LABORATORIES
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Yixian Chen, Jurgen Dinges, Karla Drescher, Peer Jacobson, Hwan-soo Jae, Ravi Kurukulasuriya, James T. Link, David J. Madar, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Lynne E. Rueter, Qi Shuai, Bryan K. Sorensen, Jiahong Wang, Karsten M. Wicke, Martin Winn, Dariusz Wodka, Vince Yeh, Hong Yong
  • Publication number: 20090054438
    Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.
    Type: Application
    Filed: August 15, 2008
    Publication date: February 26, 2009
    Applicant: Burnham Institute for Medical Research
    Inventors: Ze'ev A. Ronai, Anindita Bhoumik, Nicholas D.P. Cosford, Russell Dahl
  • Patent number: 7432302
    Abstract: Proliferative cutaneous disease states or conditions are treated by administering a polyamine transport inhibitor R-X-L-polyamine wherein R is a straight or branched C10-50 saturated or unsaturated aliphatic, carboxyalkyl, carbalkoxyalkyl, or alkoxy; a C1-8 alicyclic; a single or multiring aryl substituted or unsubstituted aliphatic; and aliphatic-substituted or unsubstituted single or multiring aromatic; a single or multiring heterocyclic; a single or multiring heterocyclic aliphatic; an aryl sulfonyl; X is —CO—, —SO2—, or —CH2—; and L is a covalent bond or a naturally occurring amino acid, lysine, ornithine, 2,4-diaminobutyric acid, or pharmaceutically acceptable salts thereof or prodrug thereof, and a polyamine biosynthesis inhibitor.
    Type: Grant
    Filed: February 23, 2005
    Date of Patent: October 7, 2008
    Assignee: MediQuest Therapeutics, Inc.
    Inventors: Mark R. Burns, Gerard F. Graminski, Nand Baindur, Reitha S. Weeks
  • Publication number: 20080200467
    Abstract: Disclosed are alpha keto amide and alpha hydroxy amide compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.
    Type: Application
    Filed: November 2, 2007
    Publication date: August 21, 2008
    Inventors: Dinesh Patel, Richard D. Gless, Heather K. Webb Hsu, Sampath Kumar Anandan, Bhaskar R. Aavula
  • Publication number: 20080182881
    Abstract: A purpose of the present invention is to provide TNF-? production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-? production inhibitory activities, wherein A is —(NR4)—, —(CR5R6)— or —O—, B is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantyl or the like, R3 is aryl or an unsaturated heterocycle, and X is oxygen or sulfer respectively.
    Type: Application
    Filed: August 15, 2007
    Publication date: July 31, 2008
    Applicant: SANTEN PHARMACEUTICAL, CO., LTD.
    Inventors: Masakazu Ban, Hiroshi Suhara, Masato Horiuchi, Noriyoshi Yamamoto, Hiroshi Enomoto, Hiroyuki Inoue
  • Publication number: 20080090913
    Abstract: The present invention relates to specific sphingolipids/sphingolipid derivatives as pharmaceutical compositions as well as their use in the preparation of medicaments for the treatment, prevention and/or amelioration of disorders relating to pathological processes in lipid rafts.
    Type: Application
    Filed: June 29, 2005
    Publication date: April 17, 2008
    Inventors: Tobias Braxmeier, Tim Friedrichson, Wolfgang Frohner, Gary Jennings, Georg Schlechtingen, Cornelia Schroeder, Hans-Joachim Knolker, Kai Simons, Marino Zerial, Teymuras Kurzchalia
  • Patent number: 7244768
    Abstract: Compositions, methods, and pharmaceutical products related to prostaglandin-related compounds and trefoil factor family peptides are disclosed herein. Of particular interest are compositions and methods useful for the treatment of glaucoma with a reduced occurrence of hyperemia.
    Type: Grant
    Filed: August 25, 2004
    Date of Patent: July 17, 2007
    Assignee: Allergan, Inc.
    Inventors: Peter G. Bakhit, Richard Graham, Orest Olejnik
  • Patent number: 7202277
    Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta p
    Type: Grant
    Filed: February 6, 2002
    Date of Patent: April 10, 2007
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Simona Zanzola, Roberto Artusi, Lucio Claudio Rovati
  • Patent number: 7179943
    Abstract: Bicyclic amide derivatives of formula (I) or tautomers or pharmaceutically acceptable salts thereof or both are provided: Also provided are processes for preparing the bicyclic amide derivatives as well as pharmaceutical compositions containing the same and therapeutic uses. The bicyclic amide derivatives are useful for treating a variety of conditions associated with the abnormal modulation of one or more Kv1.1 voltage-gated potassium channels.
    Type: Grant
    Filed: June 13, 2005
    Date of Patent: February 20, 2007
    Assignee: Wyeth
    Inventors: Wayne E. Childers, Jerome C. Wu, Callain Y. Kim, Edward J. Podlesny
  • Patent number: 7138546
    Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Grant
    Filed: August 16, 2001
    Date of Patent: November 21, 2006
    Assignee: Emisphere Technologies, Inc.
    Inventor: Pingwah Tang
  • Patent number: RE42700
    Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: September 13, 2011
    Assignees: Sanford-Burnham Medical Research Institute, Oregon State University, SRI International, Molecular Medicine Research Institute, Department of Veterans Affairs, Wayne State University
    Inventors: Marcia Dawson, Joseph A. Fontana, Xiao-Kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs
  • Patent number: RE43327
    Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: April 24, 2012
    Assignee: Aminex Therapeutics, Inc.
    Inventors: Mark R. Burns, Gerard F. Graminski, Nand Baindur