Nitrogen In R Patents (Class 514/619)
The nitrogen in r is an amino nitrogen attached indirectly to a ring by acyclic bonding (Class 514/620)
  • Selective androgen receptor modulators and methods of use thereof
    Patent number: 7741371
    Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The compounds are selective androgen receptor modulators (SARM) useful for, inter-alia, suppressing spermatogenesis, treating a subject having a hormone related condition, treating a subject suffering from prostate cancer, delaying the progression of prostate cancer, preventing the recurrence of prostate cancer, and treating the recurrence of prostate cancer.
    Type: Grant
    Filed: March 31, 2006
    Date of Patent: June 22, 2010
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller, Craig A. Marhefka, Wenqing Gao
  • Indene derivatives and process for the preparation thereof
    Patent number: 7741323
    Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.
    Type: Grant
    Filed: April 13, 2005
    Date of Patent: June 22, 2010
    Assignees: Korea Research Institute of Chemical Technology, Jeil Pharm. Co., Ltd., Korea Research Institute of Bioscience and Biotechnology, CJ Corp.
    Inventors: Hyae Gyeong Cheon, Sung-Eun Yoo, Sung Soo Kim, Sung-Don Yang, Kwang-Rok Kim, Sang Dal Rhee, Jin Hee Ahn, Seung Kyu Kang, Won Hoon Jung, Sung Dae Park, Nam Gee Kim, Jang Hyuk Lee, Sun Chul Huh, Jae Mok Lee, Seog Beom Song, Soon Ji Kwon, Jong Hoon Kim, Jeong-Hyung Lee, Seung Jun Kim
  • HISTONE ACETYL TRANSFERASE ACTIVATORS AND HISTONE DEACETYLASE INHIBITORS IN THE TREATMENT OF ALCOHOLISM
    Publication number: 20100144885
    Abstract: The present invention relates to the reduction of a symptom of an alcohol withdrawal state comprising administering a modulator of histone acetylation.
    Type: Application
    Filed: September 28, 2007
    Publication date: June 10, 2010
    Applicant: The board of Trustees of the University of Illinois
    Inventor: Subhash C. Pandey
  • Treatment of breast cancer with a PARP inhibitor alone or in combination with anti-tumor agents
    Patent number: 7732491
    Abstract: In one aspect, the present invention provides a method of treating breast cancer that is negative for at least one of ER, PR, or HER2, comprising administering to a subject at least one PARP inhibitor. In another aspect, the present invention provides a method of treating breast cancer comprising administering to a subject at least one PARP inhibitor in combination with at least one anti-tumor agent.
    Type: Grant
    Filed: November 11, 2008
    Date of Patent: June 8, 2010
    Assignee: BiPar Sciences, Inc.
    Inventors: Barry M. Sherman, Charles Bradley, Valeria S. Ossovskaya
  • NOVEL COMPOUNDS
    Publication number: 20100137377
    Abstract: 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: Application
    Filed: April 9, 2008
    Publication date: June 3, 2010
    Inventors: Anders Klarskov Petersen, Soren Ebdrup
  • TREATING ANDROGEN DECLINE IN AGING MALE (ADAM)-ASSOCIATED CONDITIONS WITH SARMS
    Publication number: 20100137430
    Abstract: This invention provides methods for treatment and inhibition of a male subject having an Androgen Decline in Aging Male (ADAM)-associated condition, for example sexual dysfunction, decreased sexual libido, erectile dysfunction, hypogonadism, sarcopenia, osteopenia, osteoporosis, an alteration in cognition and mood, depression, anemia, hair loss, obesity, muscle loss, dry eye, memory loss, benign prostate hyperplasia and/or prostate cancer, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, pro-drug, polymorph, crystal, or any combination thereof.
    Type: Application
    Filed: December 7, 2009
    Publication date: June 3, 2010
    Inventors: James T. DALTON, Duane D. Miller, Donghua Yin, Yali He
  • N-PHENYL ANTHRANILIC ACID DERIVATIVES AND USES THEREOF
    Publication number: 20100137296
    Abstract: Compounds that can be used as openers or blockers of voltage-dependent potassium channels, and which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and/or depressing or enhancing cortical and/or peripheral neuron activity, compositions containing same and methods utilizing same are disclosed. Also disclosed are modulators of voltage-dependent potassium channels, which exhibit blocking of a TRPV1 channel, and hence are useful in the treatment of TRPV1-related conditions.
    Type: Application
    Filed: September 18, 2008
    Publication date: June 3, 2010
    Applicant: Ramot At Tel Aviv University Ltd.
    Inventors: Bernard Attali, Asher Peretz
  • Long chain N-alkyl compounds and oxa-derivatives thereof
    Publication number: 20100137365
    Abstract: Long chain N-alkyl amino and imino compounds, oxa-substituted derivatives thereof, and pharmaceutical compositions including such compounds are described. The long chain N-alkyl group is a C8-C16 alkyl group. The long chain N-alkyl compounds and oxa-substituted derivatives thereof can be used in the treatment of viral infections, in particular hepatitis B virus or hepatitis C virus, in a cell or an individual. For example, the long chain N-alkyl compounds or oxa-substituted derivatives thereof can be derived from piperidines, pyrrolidines, phenylamines, pyridines, pyrroles, or amino acids.
    Type: Application
    Filed: January 28, 2010
    Publication date: June 3, 2010
    Inventors: Nicole Zitzmann, Terry D. Butters, Frances M. Platt, Gary S. Jacob, Donald H. Picker, Sandra Carrouee, George W.J. Fleet, Raymond A. Dwek, David Durantel, Anand Mehta, Timothy M. Block
  • PROPHYLACTIC AND THERAPEUTIC USE OF SIRTUIN INHIBITORS IN TNF-ALPHA MEDIATED PATHOLOGIES
    Publication number: 20100137345
    Abstract: The invention relates to the use of sirtuin inhibitors for reducing TNF-alpha production by cells and organisms. The invention also concerns prophylactic and therapeutic applications of sirtuin inhibitors in TNF-alpha mediated pathologies, such as various inflammatory and autoimmune disorders.
    Type: Application
    Filed: May 14, 2008
    Publication date: June 3, 2010
    Applicant: Universite Libre de Bruxelles
    Inventors: Oberdan Leo, Mara Galli, Frédéric Van Gool
  • INSECTICIDAL COMPOUNDS
    Publication number: 20100130601
    Abstract: A compound of formula (I), wherein A1, A2, A3, A4, R1, R2, R3, G1, G2, G3 and Q are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Application
    Filed: February 26, 2008
    Publication date: May 27, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Pierre Jung, Christopher Richard Ayles Godrey, William Lutz, Peter Maienfisch, Andre Stoller, Werner Zambach
  • USE OF HISTONE DEACETYLASE INHIBITORS FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM METASTASES
    Publication number: 20100113602
    Abstract: Disclosed is a method of treating a localized carcinoma central nervous system (CNS) metastasis of extra-CNS origin, the method comprising systemically administering an effective amount of a histone deacetylase (HDAC) inhibitor (HDI) to a subject in need of treatment for the localized carcinoma CNS metastasis of extra-CNS origin. The HDI can be any HDI capable of crossing the blood-brain barrier (BBB) such as vorinostat. The localized carcinoma CNS metastasis of extra-CNS origin can be a localized carcinoma brain metastasis. The localized carcinoma brain metastasis can originate in the breast. The CNS metastasis treated can be a micrometastasis, a brain tumor, or an intervening stage of brain cancer.
    Type: Application
    Filed: February 27, 2008
    Publication date: May 6, 2010
    Applicant: The United States of America,as represented by the Secretary,Department of Health and Human Services
    Inventors: Diane Palmieri, Patricia Steeg
  • PHARMACEUTICAL COMPOSITIONS OF ENTACAPONE
    Publication number: 20100104634
    Abstract: The invention relates to pharmaceutical compositions comprising entacapone or pharmaceutically acceptable salts thereof. The invention also relates to processes for the preparation of such compositions.
    Type: Application
    Filed: December 20, 2007
    Publication date: April 29, 2010
    Inventor: Mahesh Rameshwar KALANTRI
  • Compositions containing opioid antagonists
    Patent number: 7700626
    Abstract: Compositions containing opioid antagonists, particularly alvimopan and its active metabolite, with improved solubility and bioavailability for oral or parenteral administration, injectable dosage formulations, kits, and methods of making and using same are disclosed. In preferred embodiments, invention provides injectable formulations containing opioid antagonists, particularly alvimopan and its active metabolite, having low solubility that may be readily prepared, are stable during storage, and provide maximum levels of opioid antagonists when administered parenterally, particularly via injection. The results are achieved by a combination of processing techniques and component selection.
    Type: Grant
    Filed: June 2, 2005
    Date of Patent: April 20, 2010
    Assignee: Adolor Corporation
    Inventor: John D. Buehler
  • STABILIZED PHARMACEUTICAL SUB-MICRON SUSPENSIONS AND METHODS OF FORMING SAME
    Publication number: 20100076045
    Abstract: The present invention is directed to a pharmaceutical submicron suspension and a method of forming the submicron suspension. The submicron suspension is useful for delivery of relatively hydrophobic and/or low solubility therapeutic agent. The submicron suspension and method of forming the submicron suspension typically employ a polymeric material that aids in preventing aggregation of the therapeutic agent.
    Type: Application
    Filed: September 16, 2009
    Publication date: March 25, 2010
    Inventors: Ernesto J. Castillo, Bahram Asgharian, Masood A. Chowhan
  • COMPOUNDS AND USES THEREOF
    Publication number: 20100063144
    Abstract: There is provided a compound of formula (I) wherein R1a, R2a, R3, X1 to X6, a, b and c have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, inhibitors of HDAC enzyme activity, and thus, in particular, in the treatment of conditions where inhibition of HDAC enzyme activity is required.
    Type: Application
    Filed: October 24, 2007
    Publication date: March 11, 2010
    Applicant: IMPERIAL INNOVATIONS LTD
    Inventors: Eric Ofori Aboagye, David Michael Vigushin, Wendy Vigushin
  • Oral and Injectable Formulations of Tetracycline Compounds
    Publication number: 20100056638
    Abstract: Injectable and oral formulations of a tetracycline compound are described. In one embodiment, the invention pertains to an oral formulation of a 9-aminomethyl tetracycline compound, or a salt thereof, in tablet form or capsule. The formulations may be used, for example, to treat infections.
    Type: Application
    Filed: March 30, 2009
    Publication date: March 4, 2010
    Applicant: Paratek Pharmaceuticals, Inc.
    Inventor: Sean Johnston
  • INSECTICIDAL COMPOUNDS
    Publication number: 20100056639
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Application
    Filed: December 12, 2007
    Publication date: March 4, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Pierre Jung, Christopher Richard Syles Godfrey, William Lutz, Peter Maienfisch, Andre Stoller, Werner Zambach
  • INTRAOCULAR PRESSURE-LOWERING AGENT COMPRISING COMPOUND HAVING HISTONE DEACETYLASE INHIBITOR EFFECT AS ACTIVE INGREDIENT
    Publication number: 20100056522
    Abstract: An object of the present invention is to find a novel pharmacological effect of a compound having an HDAC inhibitory effect. The compound having an HDAC inhibitory effect of the invention has an excellent effect of cell morphological change on trabecular meshwork cells and/or effect of intraocular pressure reduction, and is therefore useful as a preventive and/or therapeutic agent for a disease considered to be associated with aqueous humor circulation and/or intraocular pressure, particularly as a preventive and/or therapeutic agent for glaucoma or ocular hypertension.
    Type: Application
    Filed: March 28, 2008
    Publication date: March 4, 2010
    Applicant: Santen Pharmaceutical Co., Ltd.
    Inventors: Shinji Yoneda, Koushi Fujisawa, Katsuhiko Watanabe, Junko Fujikawa, Atsushi Shimazaki, Tomoko Kirihara, Hisashi Tajima
  • INSECTICIDAL COMPOUNDS
    Publication number: 20100048715
    Abstract: A compound of formula (I), wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Application
    Filed: June 26, 2007
    Publication date: February 25, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Peter Maienfisch, Werner Zambach, Pierre Jung, William Lutz, Thomas Pitterna, Peter Renold
  • Histone Deacetylase Inhibitors for the Treatment of Ocular Neovascular or Edematous Disorders and Diseases
    Publication number: 20100048608
    Abstract: Ophthalmic compositions containing HDAC inhibitors and their use for treating ocular neovascular or edematous diseases and disorders are disclosed.
    Type: Application
    Filed: October 30, 2009
    Publication date: February 25, 2010
    Applicant: ALCON, INC.
    Inventors: Peter G. Klimko, David P. Bingaman
  • METHODS FOR TREATING RETROVIRAL INFECTIONS
    Publication number: 20100041648
    Abstract: The present invention provides compositions for treating an HIV infection comprising administering a compound according to formula I where Ar, R1-R5, R11c and X1 are as defined herein with at least one carrier, excipient or diluent.
    Type: Application
    Filed: October 27, 2009
    Publication date: February 18, 2010
    Inventors: James Patrick Dunn, Donald Roy Hirschfeld, Tania Silva, Zachary Kevin Sweeney, Harit Vora
  • OPHTHALMIC DEVICE HAVING THERAPEUTIC AGENT DELIVERY CAPABILITY AND METHOD OF FORMING SAME
    Publication number: 20100016439
    Abstract: The present invention is directed to ophthalmic devices that are loaded with therapeutic agent. The devices provide prolonged release of the therapeutic agent to the eye. The ophthalmic devices are typically formed of an ophthalmic material that is particularly desirable for the loading of therapeutic agent and/or the therapeutic agent is typically particularly desirable for loading to the ophthalmic material.
    Type: Application
    Filed: July 20, 2009
    Publication date: January 21, 2010
    Inventors: Brett E. Thomes, Stephen J. Van Noy, Chi-Chun Tsai
  • Novel nitrophenyl mustard and nitrophenylaziridine alcohols and their corresponding phosphates and their use as targeted cytotoxic agents
    Publication number: 20100010094
    Abstract: The present invention relates to novel nitrophenyl mustard and nitrophenylaziridine alcohols, to their corresponding phosphates, to their use as targeted cytotoxic agents; as bioreductive drugs in hypoxic tumours, and to their use in cell ablation, including gene-directed enzyme-prodrug therapy (GDEPT) and antibody-directed enzyme-prodrug therapy (ADEPT), in conjunction with nitroreductase enzymes.
    Type: Application
    Filed: August 11, 2009
    Publication date: January 14, 2010
    Applicant: Auckland Uniservices Limited
    Inventors: William Alexander Denny, Graham John Atwell, Shangjin Yang, William Robert Wilson, Adam Vorn Patterson, Nuala Ann Helsby
  • Administration of nepafenac or derivatives thereof for treating dermatological/keratinization disorders
    Publication number: 20090312429
    Abstract: Nepafenac or derivatives thereof are useful for the treatment of dermatological conditions related to a keratinization disorder that may have an inflammatory immunoallergic component, for example rosacea, acne, psoriasis or atopic dermatitis.
    Type: Application
    Filed: June 19, 2009
    Publication date: December 17, 2009
    Applicant: GALDERMA RESEARCH&DEVELOPMENT
    Inventors: Irina Safonova, Cecile Cousin, Leila Zarif
  • Oral Therapeutic Compound Delivery System
    Publication number: 20090311327
    Abstract: The present, invention provides an oral delivery system for a therapeutic compound that is an acid, a salt of an acid or an unionized compound or a proactive form thereof with pharmacological, physiological or biochemical activity. The present invention particularly provides a swallow formulation comprising a therapeutic compound that is an acid, a salt of an acid or an unionized compound or a proactive form thereof which facilitates the rapid delivery of the therapeutic compound to the circulatory system.
    Type: Application
    Filed: November 28, 2006
    Publication date: December 17, 2009
    Applicant: IMAGINOT PTY LTD
    Inventors: Michael Stephen Roberts, George Alexander Davidson, Ruoying Jiang, Geraldine Ann Elliott, Keivan Bezanehtak, Stephen Douglas Chandler, Greg Davey, Mantu Sarkar
  • PHARMACEUTICAL COMPOSITION
    Publication number: 20090298944
    Abstract: The present invention relates to a pharmaceutical composition of practically water insoluble or low water soluble compounds containing catechol moiety by enhancing the solubility of such compounds using one or more alkalising agent and optionally adding one or more pharmaceutically acceptable excipient.
    Type: Application
    Filed: November 9, 2006
    Publication date: December 3, 2009
    Inventors: Samanta Gour, Nanda Nagesh
  • Selective androgen receptor modulators and methods of use thereof
    Patent number: 7622503
    Abstract: This invention provides SARM compounds and their use in treating a variety of diseases or conditions in a subject, including, inter-alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.
    Type: Grant
    Filed: June 7, 2005
    Date of Patent: November 24, 2009
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller, Karen A. Veverka
  • NEUROPROTECTIVE BENZOATE AND BENZAMIDE COMPOUNDS
    Publication number: 20090286876
    Abstract: The invention provides a therapeutic method for treating at least one symptom of a neurological disorder or disease such as Alzheimer's disease in a mammal, such as a human, wherein the toxicity of a pathogen of ? amyloid peptide and/or glutamate in mammalian cells is implicated and inhibition of the subsequently-induced pathological pathways is desired comprising administering to a mammal in need of such therapy, an effective amount of an N-arylamide or an (N-aminoalkyl)benzamide, including pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: November 12, 2008
    Publication date: November 19, 2009
    Inventors: Laurent Lecanu, Janet Greeson, Vassilios Papadopoulos
  • USE OF HDAC INHIBITORS FOR THE TREATMENT OF LYMPHOMAS
    Publication number: 20090281159
    Abstract: The present invention relates to the use of an HDAC inhibitor, especially an HDAC inhibitor of formula (I): wherein the radicals and symbols have the meanings as defined in the specification, for the preparation of a medicament for the treatment of lymphoproliferative diseases, in particular, cutaneous T-cell lymphomas.
    Type: Application
    Filed: June 26, 2007
    Publication date: November 12, 2009
    Applicant: NOVARTIS AG
    Inventors: Peter Wisdom Atadja, Wenlin Shao
  • SELECTIVE ANDROGEN RECEPTOR MODULATORS
    Publication number: 20090264534
    Abstract: The present invention relates to androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity, which are nonsteroidal ligands for the androgen receptor.
    Type: Application
    Filed: April 8, 2009
    Publication date: October 22, 2009
    Inventors: James T. Dalton, Duane D. Miller, Yali He, Donghua Yin
  • AMINO- AND AMIDO-AMINOTETRALIN DERIVATIVES AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS
    Publication number: 20090247627
    Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: March 31, 2009
    Publication date: October 1, 2009
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
  • 5-Substituted-2-Phenylamino Benzamides as MEK Inhibitors
    Publication number: 20090233915
    Abstract: An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].
    Type: Application
    Filed: July 26, 2005
    Publication date: September 17, 2009
    Inventors: Yoshiaki Isshiki, Yasunori Kohchi, Eisaku Mizuguchi, Hitoshi Iikura, Yasuaki Matsubara, Shinji Tsujii, Nobuo Shimma, Masanori Miwa, Satoshi Aida, Masami Kohchi, Takeshi Murata, Kosuke Aso
  • Methods and compositions for nasal administration of modafinil
    Patent number: 7576133
    Abstract: Systemic delivery of Modafinil to the nasal mucous membrane elicits rapid systemic therapeutic response with reduced side effects compared to current methods of administration.
    Type: Grant
    Filed: March 7, 2003
    Date of Patent: August 18, 2009
    Inventors: Carl Henry Lawyer, Matthew Carl Lawyer, Edward Zadok Lawyer
  • ANDROGEN MODULATORS
    Publication number: 20090192202
    Abstract: The present invention is directed to a new class of 4-cyano-phenoxy-alkyl carboxyl derivatives and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.
    Type: Application
    Filed: February 9, 2009
    Publication date: July 30, 2009
    Inventors: Lain-Yen Hu, Huangshu Lei, Daniel Y. Du, Bruce A. Lefker, Yvonne Dorothy Smith, Victor Fedij
  • Histone deacetylase inhibitors
    Publication number: 20090182019
    Abstract: The present invention provides novel HDAC inhibitors and methods of treating diseases using the same.
    Type: Application
    Filed: April 18, 2006
    Publication date: July 16, 2009
    Applicants: The Johns Hopkins University, Wayne State University
    Inventors: Robert A. Casero, Patrick M. Woster, Sheeba Varghese
  • Inhibitors of Histone Deacetylase
    Publication number: 20090181971
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Application
    Filed: August 13, 2007
    Publication date: July 16, 2009
    Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg
  • ANILINE DERIVATIVES AS SELECTIVE ANDROGEN RECEPTOR MODULATORS
    Publication number: 20090163588
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
    Type: Application
    Filed: February 25, 2009
    Publication date: June 25, 2009
    Applicant: SMITHKLINE BEECHAM CORPORATION
    Inventors: Philip Stewart Turnbull, Rodolfo Cadilla, David John Cowan, Andrew Lamont Larkin, Istvan Kaldor, Eugene Lee Stewart
  • INDENE DERIVATIVES, THEIR PREPARATION AND USE AS MEDICAMENTS
    Publication number: 20090163547
    Abstract: The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.
    Type: Application
    Filed: November 7, 2006
    Publication date: June 25, 2009
    Inventors: Maria De Las Ermitas Alcalde-Pais, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria De Les Neus Mesquida-Estevez, Sara Lopez-Perez
  • Pharmaceutical Composition Comprising an Amide Derivative
    Publication number: 20090163549
    Abstract: The present invention provides a novel modulator of the TRPV1-receptor function, comprising a compound of the formula; wherein ring A is an optionally substituted carbocycle or heterocycle, ring B is an optionally substituted benzene ring or an optionally substituted 6-membered heteroaromatic ring containing N atom, a dashed line means existence or absence of a bond, n is 1 or 2, R1 and R2 are hydrogen etc., R3 is lower alkyl, R4 is lower alkyl or aryloxy, or R3 and R4 taken together may form optionally substituted 5- or 6-membered non-aromatic heterocycle.
    Type: Application
    Filed: December 13, 2006
    Publication date: June 25, 2009
    Inventor: Hiroyuki Kai
  • Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease
    Patent number: 7550481
    Abstract: The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: December 15, 2004
    Date of Patent: June 23, 2009
    Assignee: Merck & Co., Inc.
    Inventors: James C. Barrow, Craig A. Coburn, Philippe G. Nantermet, Harold G. Selnick, Shawn J. Stachel, Matthew G. Stanton, Shaun R. Stauffer, Linghang Zhuang, Jennifer R. Davis
  • Solid phase synthesis of arylretinamides
    Patent number: 7550510
    Abstract: A solid phase synthetic method for preparing arylretinamides is provided. The method comprises reacting hexachloroacetone with a solvent-suspended resin-bound triphenylphosphine to provide a suspension comprising an activated chlorinating reagent; reacting retinoic acid with the activated chlorinating reagent to provide retinoyl chloride; adding pyridine and a select arylamine to the resulting mixture; and stirring the resulting mixture for a time and at a temperature sufficient for the select arylamine to react with the retinoyl chloride and provide the arylretinamide. Also provided, are select arylretinamides that can be prepared by the present method, and methods of using such arylretinamides to induce apoptosis in cancer cells.
    Type: Grant
    Filed: November 21, 2003
    Date of Patent: June 23, 2009
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Robert W. Curley, Jr., Serena M. Mershon, Derek W. Barnett, Margaret Clagett-Dame, Jason S. Chapman
  • Treating muscle wasting with selective androgen receptor modulators
    Patent number: 7547728
    Abstract: This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide or any combination thereof, as described herein.
    Type: Grant
    Filed: December 5, 2002
    Date of Patent: June 16, 2009
    Assignee: University of Tennessee Research Foundation
    Inventors: Mitchell S. Steiner, Karen A. Veverka, James T. Dalton, Duane D. Miller
  • TREATMENT OF CANCER WITH COMBINATIONS OF TOPOISOMERASE INHIBITORS AND PARP INHIBITORS
    Publication number: 20090149397
    Abstract: In one aspect, the present invention provides a composition and a kit comprising a combination of topoisomerase inhibitor and PARP inhibitor for treatment of cancer. In another aspect, the invention provides a method of treating cancer comprising administering to a subject a combination of topoisomerase inhibitor and PARP inhibitor. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase and a topoisomerase, as well as providing formulations and modes of administering such compositions.
    Type: Application
    Filed: December 5, 2008
    Publication date: June 11, 2009
    Inventors: Valeria Ossovskaya, Charles Bradley, Barry Sherman
  • Methods for Assessing Suitability of Cancer Patients for Treatment with Histone Deacetylase Inhibitors
    Publication number: 20090137451
    Abstract: This invention is in the field of cancer therapy and provides the use of E2F1 activity for assessing suitability of a cancer patient for treatment with histone deacetylase inhibitors (HDACIs).
    Type: Application
    Filed: March 10, 2006
    Publication date: May 28, 2009
    Applicant: Agency for Science, Technology and Research
    Inventor: Qiang Yu
  • 4- (OR 5-) SUBSTITUTED CATECHOL DERIVATIVES
    Publication number: 20090131530
    Abstract: Compounds of the formula: are disclosed. The compounds act as phosphodiesterase-4 modulators, and useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions. Other embodiments are also disclosed.
    Type: Application
    Filed: November 20, 2008
    Publication date: May 21, 2009
    Applicant: DECODE GENETICS EHF
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov
  • TREATMENT OF BREAST CANCER WITH A PARP INHIBITOR ALONE OR IN COMBINATION WITH ANTI-TUMOR AGENTS
    Publication number: 20090131529
    Abstract: In one aspect, the present invention provides a method of treating breast cancer that is negative for at least one of ER, PR, or HER2, comprising administering to a subject at least one PARP inhibitor. In another aspect, the present invention provides a method of treating breast cancer comprising administering to a subject at least one PARP inhibitor in combination with at least one anti-tumor agent.
    Type: Application
    Filed: November 11, 2008
    Publication date: May 21, 2009
    Inventors: Barry M. Sherman, Charles Bradley, Valeria Ossovskaya
  • TREATMENT OF UTERINE CANCER AND OVARIAN CANCER WITH A PARP INHIBITOR ALONE OR IN COMBINATION WITH ANTI-TUMOR AGENTS
    Publication number: 20090123419
    Abstract: In one aspect, the present invention provides a method of treating uterine cancer, endometrial cancer, or ovarian cancer, comprising administering to a subject at least one PARP inhibitor. In another aspect, the present invention provides a method of treating uterine cancer, endometrial cancer, or ovarian cancer, comprising administering to a subject at least one PARP inhibitor in combination with at least one anti-tumor agent.
    Type: Application
    Filed: November 12, 2008
    Publication date: May 14, 2009
    Inventors: Barry M. Sherman, Charles Bradley, Valeria Ossovskaya
  • Compounds and their salts specific to the PPAR receptors and the EGF receptors and their use in the medical field
    Publication number: 20090118357
    Abstract: Therefore the present invention relates specifically to the compounds of general formula (I), in which R1 and R2, which may be identical or different, are selected from the group comprising H, —CnH2n-1, a linear or branched alkyl group having from 1 to 6 carbon atoms, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R3 is selected from —CO—CH3, —NHOH, —OH, —OR6 in which R6 is a linear or branched alkyl group having from 1 to 6 carbon atoms; R4 is selected from H, a linear or branched alkyl group having from 1 to 6 carbon atoms, phenyl, benzyl, —CF3 or —CF2CF3, vinyl or allyl; R5, R7, R8 are hydrogen atoms; or R3 and R4, R4 and R5, or R7 and R8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O, and use thereof in the medical field.
    Type: Application
    Filed: July 24, 2006
    Publication date: May 7, 2009
    Applicant: Giuliani International Limited
    Inventors: Giancarlo Naccari, Sergio Baroni
  • LYSINE RELATED DERIVATIVES AS HIV ASPARTYL PROTEASE INHIBITORS
    Publication number: 20090118339
    Abstract: The present invention concerns lysine related derivatives, their use as protease inhibitors, in particular as HIV aspartyl protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present lysine related derivatives with another anti retroviral agent. It further relates to their use in assays as reference compounds or as reagents.
    Type: Application
    Filed: May 30, 2007
    Publication date: May 7, 2009
    Inventors: Tim Hugo Maria Jonckers, Inge Dierynck, Stefaan Julien Last, Herman De Kock
  • Methods for Producing Pesticide Compositions
    Publication number: 20090110707
    Abstract: Disclosed are compositions and methods related to powder and granular emulsifiable concentrate pesticide formulations. As disclosed, emulsions from non-aqueous based liquid or solvent soluble pesticide actives may be prepared using a high purity, high molecular weight sulfonated lignin as the emulsion stabilizer. The resulting emulsions may then be dried to obtain a powder or granular emulsion concentrate where the high molecular weight sulfonated lignin acts as a solid matrix for the pesticide active. The powder or granular emulsifiable concentrate formulations thus formed have high loading rates, good storage properties and are easily reconstituted when added to water.
    Type: Application
    Filed: October 29, 2007
    Publication date: April 30, 2009
    Inventors: Thomas S. Winowiski, Stuart E. Lebo, JR., Scott E. Davis, Stig Are Gundersen