Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/469)
  • Patent number: 7547723
    Abstract: The comprehensive pharmacologic therapy for treatment of obesity is a procedure which involves the administration of a desired therapeutic range of Diethylpropion and/or Phentermine in combination with a SSRI medication and nutritional supplementation for brief and long durations which may be 12 months or more. The preferred procedure involves the administration of drugs in combination which are identified as: Citalopram (Celexa) and Phentermine; Citalopram (Celexa) and Diethylpropion; Citalopram (Celexa), Phentermine, and Diethylpropion. In addition nutritional supplementation such as a multivitamin, 5-Hydroxytryptophan, vitamin B6, vitamin C, Tyrosine, Calcium, and Lysine may be used to enhance the performance of the weight loss treatment program.
    Type: Grant
    Filed: June 20, 2005
    Date of Patent: June 16, 2009
    Inventor: Martin C. Hinz
  • Publication number: 20090143408
    Abstract: Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.
    Type: Application
    Filed: November 26, 2008
    Publication date: June 4, 2009
    Applicant: Sequoia Pharmaceuticals, Inc.
    Inventors: Michael EISSENSTAT, Dehui Duan, Ji-Hye Kang
  • Patent number: 7538138
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salts or prodrug thereof which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders ameliorated by histamine-3 receptor ligands.
    Type: Grant
    Filed: April 8, 2005
    Date of Patent: May 26, 2009
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Youssef L. Bennani, Ramin Faghih, Gregory A. Gfesser, Lawrence A. Black
  • Publication number: 20090130156
    Abstract: The present invention relates to a new formulation characterised by the presence of two components, one of which (A) possesses insecticidal, acaricidal, fungicidal, snailcidal or vermicidal activity and the other (B) exhibits synergistic activity with the first by enhancing its effectiveness, and in which the average release time of component (A) is 1 to 12 hours later than the average release time of component (B). The formulation is obtained by: a) separate microencapsulation of both components (A) and (B) within a multilayer system of specific polymers in which component (A) is in a more interior portion of the capsule than component (B), being separated from component (B) by a polymer layer of suitable thickness (FIG. 1); b) microencapsulation of both components within a single layer system (FIG. 2), combined with an immediate-release emulsion/microemulsion containing an additional amount of component (B).
    Type: Application
    Filed: April 20, 2006
    Publication date: May 21, 2009
    Applicant: ENDURA S.P.A.
    Inventors: Valerio Borzatta, Oreste Picolo, Elisa Capparella
  • Publication number: 20090123387
    Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.
    Type: Application
    Filed: January 9, 2009
    Publication date: May 14, 2009
    Inventor: Harry A. Dugger, III
  • Publication number: 20090123446
    Abstract: Methods of treating, inhibiting, or ameliorating gout, including chronic acute (refractory) gout, pseudogout, or drug-induced gout, in a human subject in need thereof, comprising administering to a subject in need a therapeutic amount of an interleukin 1 (IL-1) antagonist, wherein the incidence of a gout flare is reduced or inhibited.
    Type: Application
    Filed: August 28, 2008
    Publication date: May 14, 2009
    Applicant: Regeneron Pharmaceuticals, Inc.
    Inventors: Catherine Vicary, Scott Mellis
  • Publication number: 20090124613
    Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.
    Type: Application
    Filed: November 7, 2008
    Publication date: May 14, 2009
    Inventors: Joanne J. Bronson, Andrew P. Degnan, William D. Schmitz
  • Publication number: 20090124687
    Abstract: The present invention relates to a compound having a leukotriene (particularly leukotriene B4) inhibitory action, and useful for the prophylaxis or treatment of diseases such as allergy, asthma, inflammation, cancer and the like.
    Type: Application
    Filed: November 18, 2005
    Publication date: May 14, 2009
    Applicant: THE NEW INDUSTRY RESEARCH ORGANIZATION
    Inventors: Yoshitaka Oishi, Takehiko Yokomizo
  • Publication number: 20090125331
    Abstract: The present invention provides systems comprising two main components—a static and a dynamic component—that coupled with at least one interactive element of the systems permit providing information and support to a patient having a disease or disorder, responding to potential treatment issues of the patient, tracking a patient's treatment, and thereby improving patient compliance; as well as methods of using the systems, including methods of treating the patient and of ensuring the authenticity of a medication used by the patient.
    Type: Application
    Filed: September 11, 2008
    Publication date: May 14, 2009
    Applicant: H. Lundbeck A/S
    Inventors: Janne Pamsgaard, Jesper Lauridsen
  • Publication number: 20090118323
    Abstract: The present invention provides antitumor compounds of the formula (I); and antitumor methods.
    Type: Application
    Filed: September 11, 2007
    Publication date: May 7, 2009
    Inventors: Mary Margaret Mader, Luisa Maria Martin-Cabrejas, Michael Enrico Richett
  • Publication number: 20090118301
    Abstract: The invention provides compounds useful for treating or effecting prophylaxis of cancers, particularly cervical cancer.
    Type: Application
    Filed: October 30, 2008
    Publication date: May 7, 2009
    Applicant: Arbor Vita Corporation
    Inventors: Peter S. Lu, Michael P. Belmares, Jingjing Wang, Johannes Schweizer, Aida A. Fantaye
  • 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
  • Publication number: 20090118157
    Abstract: The present invention provides a method for producing wine lactone, a method for producing intermediates that are usable in production of wine lactone, and techniques for the application of wine lactone. The method for producing the wine lactone (Compound (6)) of the present invention comprises the following steps (A) to (E): wherein R1 is a C1-4 lower alkyl group.
    Type: Application
    Filed: September 10, 2004
    Publication date: May 7, 2009
    Applicant: San-Ei Gen F.F.I. Inc.
    Inventors: Mineko Omoto, Chiyoki Yukawa, Yoshiteru Nishijo
  • Patent number: 7524878
    Abstract: Disclosed are compounds and pharmaceutically acceptable salts of formula (A): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
    Type: Grant
    Filed: April 30, 2004
    Date of Patent: April 28, 2009
    Assignee: The Institute for Pharmaceuticals Discovery LLC
    Inventors: Darren Whitehouse, Shaojing Hu, Haiquan Fang, Michael C. Van Zandt
  • Patent number: 7524882
    Abstract: A class of benzodihydrofuran compounds having the structure of formula (I) below and pharmaceutically acceptable salts thereof are useful as therapeutic compounds, particularly in the treatment of hyperlipidemia, hypercholesterolemia, dyslipidemia, and other lipid disorders, and in delaying the onset of or reducing the risk of conditions and sequelae that are associated with these diseases, such as atherosclerosis.
    Type: Grant
    Filed: July 25, 2003
    Date of Patent: April 28, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Guo Q. Shi, Yong Zhang
  • Publication number: 20090105333
    Abstract: This invention provides methods of administering (1R-trans)-N-[[2-(2,3-dihydro-4-benzofuranyl)cyclo-propyl]methyl]propanamide as a melatonin receptor agonist to a human subject to treat or prevent a circadian rhythm disorder or sleep disorder.
    Type: Application
    Filed: May 22, 2007
    Publication date: April 23, 2009
    Inventors: Gunther Birznieks, Deepak Phadke, Mihael H. Polymeropoulos
  • Patent number: 7521570
    Abstract: To provide highly safe therapeutic or preventive agents for hyperuricemia, more specifically uricosuric agents, which have potent uricosuric effect and do not cause grave hepatic disorder. Medicinal compositions for the treatment or prevention of hyperuricemia or diseases caused by hyperuricemia, which contain 6-hydroxybenzbromarone or salts thereof, and pharmaceutically acceptable carriers; uricosuric agents, xanthine oxidase inhibitors, and inhibitors against the uptake of uric acid in kidney, which contain 6-hydroxybenzbromarone or salts thereof; and a process for the production of 6-hydroxybenzbromarone.
    Type: Grant
    Filed: June 10, 2005
    Date of Patent: April 21, 2009
    Assignees: Torli Pharmaceutical Co., Ltd., Human Cell Systems, Inc.
    Inventors: Hitoshi Endou, Toshihiro Oikawa
  • Publication number: 20090099135
    Abstract: Embodiments of the present invention provide compositions for controlling a target pest including a pest control product and at least one active agent, wherein: the active agent can be capable of interacting with a receptor in the target pest; the pest control product can have a first activity against the target pest when applied without the active agent and the compositions can have a second activity against the target pest; and the second activity can be greater than the first activity.
    Type: Application
    Filed: January 16, 2008
    Publication date: April 16, 2009
    Applicant: TyraTech, Inc.
    Inventor: Essam Enan
  • Publication number: 20090099169
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein R1, R2a, R2b, R2c, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
    Type: Application
    Filed: April 3, 2007
    Publication date: April 16, 2009
    Applicant: GLAXO GROUP LIMITED
    Inventors: Mairi Gibson, Adrian Hall, David Nigel Hurst, Derek Anthony Rawlings
  • Patent number: 7517908
    Abstract: A method of treating a subject for a serotonergic neurotransmission dysregulation disorder, comprises administering the subject a serotonin enhancer (e.g., a serotonin reuptake inhibitor) in an amount effective to treat the disorder; and concurrently administering the subject 5-hydroxytryptophan in an amount effective to enhance the activity of the serotonin enahancer, (e.g., serotonin reuptake inhibitor). In preferred embodiments the disorder is depression, anxiety, or substance abuse.
    Type: Grant
    Filed: May 20, 2005
    Date of Patent: April 14, 2009
    Assignee: Duke University
    Inventors: Ranga R. Krishnan, Marc G. Caron, Xiaodong Zhang, Martin Beaulieu, Raul R. Gainetdinova, Tatiana D. Sotnikova
  • Publication number: 20090093485
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).
    Type: Application
    Filed: October 26, 2005
    Publication date: April 9, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Hakan Bladh, Krister Henriksson, Vijaykumar Hulikal, Matti Lepisto
  • Publication number: 20090088469
    Abstract: Method for the preparation of citalopram comprising reaction of a compound of Formula (IV) wherein R is halogen, or CF3—(CF2)n—SO2—, n being 0 to 8, with a cyanide source in the presence of a palladium catalyst and a catalytic amount of Cu+ or Zn2+, or with Zn(CN)2 in the presence of a palladium catalyst.
    Type: Application
    Filed: December 8, 2008
    Publication date: April 2, 2009
    Applicant: H. Lundbeck A/S
    Inventors: Hans Petersen, Michael Harold Rock, Henrik Svane
  • Publication number: 20090087409
    Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7 and R8 and Q are as defined herein; Y2 is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, al
    Type: Application
    Filed: November 26, 2008
    Publication date: April 2, 2009
    Applicant: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, Eric Jolicoeur, James Gillard, Marc-Andre Poupart, Jean Rancourt
  • Publication number: 20090088468
    Abstract: This invention relates to a stable epoprostenol composition that can be combined with commercially available IV fluids and can be administered in its reconstituted and/or diluted form under ambient conditions of about 15-30° C. for greater than 24 hours. The composition preferably contains (a) epoprostenol or a salt thereof; (b) a alkalinization agent; and (c) a base, such that when reconstituted or in solution, the solution has a pH>11. Methods for making the lyophilized composition are also disclosed.
    Type: Application
    Filed: February 2, 2007
    Publication date: April 2, 2009
    Inventor: Nagesh R. Palepu
  • Publication number: 20090082392
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance or hyperglycemia. These compounds include inhibitors of protein tyrosine phosphatase (PTP-1B) that are useful in the treatment of diabetes and other PTP-1B mediated diseases, such as cancer, neurodegenerative diseases and the like. The compounds of the invention are also useful in pharmaceutical compositions and methods of treating the aforementioned conditions.
    Type: Application
    Filed: April 15, 2008
    Publication date: March 26, 2009
    Inventors: Michael C. Van Zandt, Darren Whitehouse, Kerry Combs, Shaojing Hu
  • Publication number: 20090082434
    Abstract: Compounds of Formula 1 or pharmaceutically acceptable salts thereof are provided: which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
    Type: Application
    Filed: September 15, 2008
    Publication date: March 26, 2009
    Applicant: Wyeth
    Inventors: Jonathan Laird Gross, Marla Jean Williams, Gary Paul Stack, Hong Gao, Dahul Zhou
  • Patent number: 7507839
    Abstract: Various divalent ligands based on khellinone derivatives are described. These derivatives can be useful in the modulation of potassium channel activity in cells, including among others Kv1.3 channels found in T-cells. The compounds may also be useful in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis.
    Type: Grant
    Filed: March 20, 2003
    Date of Patent: March 24, 2009
    Assignee: The Walter and Eliza Hall Institute of Medical Research
    Inventors: Jonathan B. Baell, Heike Wulff, Andrew J. Harvey, Raymond S. Norton, George K. Chandy
  • Publication number: 20090076137
    Abstract: The present application describes deuterium-enriched dronedarone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 21, 2008
    Publication date: March 19, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Publication number: 20090075938
    Abstract: There are disclosed compound of Formula (1): A1, A2, A3 and A4 which may be the same or different, represent N or CR1, X is a divalent group selected from O, S(O)n, C?W, NR4, NC(?O)R5 and CR6R7, W is O, S, NR20, Y is N or CR8, one of R4, R5, R6, R8, R9 and NR20 represents -L-R3, in which L is a single bond or a linker group, additionally, R1, R3-R9, which may be the same or different, independently represent hydrogen or a substituent and R20 represents hydrogen, hydroxyl, alkyl optionally substituted by aryl, alkoxy optionally substituted by aryl, aryl, CN, optionally substituted alkoxy, optionally substituted aryloxy, optionally substitute alkanoyl, optionally substituted aroyl, NO2, NR30R31, in which R30 and R31, which may be the same or different, represent hydrogen, optionally substituted alkyl or optionally substituted aryl; additionally, one of R30 and R31 may represent optionally substituted alkanoyl or optionally substituted aroyl, n represents an integer from 0 to 2, in addition, when an adjacent pai
    Type: Application
    Filed: February 9, 2007
    Publication date: March 19, 2009
    Inventors: Graham Michael Wynne, Stephen Paul Wren, Peter David Johnson, Paul Damien Price, Olivier De Moor, Gary Nugent, Richard Storer, Richard Joseph Pye, Colin Richard Dorgan
  • Publication number: 20090076138
    Abstract: The present application describes deuterium-enriched darunavir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 22, 2008
    Publication date: March 19, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Publication number: 20090069417
    Abstract: The present invention relates to a method for the chemoprevention and treatment of cancer, by administering a pharmaceutical composition comprising a carotenoid derivative, such as a derivative of lycopene, a- and b-carotene, phytoene, phytofluene, lutein, zeaxanthin, ?- and ?-cryptoxanthin, canthaxanthin, astaxanthin, or other carotenoid. The carotenoid derivative is a carotenoid oxidation product, and is preferably an aldehyde derivative, a dialdehyde derivative or a ketone derivative. The carotenoid derivative can be a derivative of any naturally occurring carotenoid, such as those found in tomatoes and other fruits and vegetables.
    Type: Application
    Filed: October 5, 2006
    Publication date: March 12, 2009
    Inventors: Yoav Sharoni, Joseph Levy, Yoram Sela, Zohar Nir
  • Publication number: 20090062382
    Abstract: The present invention provides a preventive or a remedy for penile erectile dysfunction, which promotes blood-flow in a penile sponge body over long time and thus induces erection while showing high safety without any adverse effect on a body as a whole, when externally administered to a penis. Use of a drug of the present invention enables to prevent or treat male penile erectile dysfunction and, at the same time, overcome a problem of female insertion impediment caused by increased resistance due to vaginal secretion disorder. Namely, a sexual life of patients (including aged persons) having coital dysfunction can be normalized and thus QOL can be improved.
    Type: Application
    Filed: August 25, 2008
    Publication date: March 5, 2009
    Applicant: CARDIOVASCULAR INSTITUTE, LTD.
    Inventors: Yasumi UCHIDA, Yasuto Uchida, Haruko Uchida
  • Publication number: 20090060905
    Abstract: The invention concerns the treatment of obesity, in particular abdominal visceral obesity. More specifically, the invention concerns the use of selective 15-lipoxygenase (LO) inhibitors for preparing medicines useful in the treatment of obesity, or at least abdominal visceral obesity, and/or its consequences.
    Type: Application
    Filed: July 30, 2008
    Publication date: March 5, 2009
    Applicant: Genfit
    Inventors: Genevieve Martin, Sebastien Barradeau, Sakina Sayah-Jeanne
  • Patent number: 7498349
    Abstract: Aromatic compounds exemplified by exhibit antimicrobial activity.
    Type: Grant
    Filed: August 1, 2003
    Date of Patent: March 3, 2009
    Assignee: Genesoft Pharmaceuticals, Inc.
    Inventors: Roland W. Burli, Eldon E. Baird, Jacob A. Kaizerman, Dustin L. McMinn
  • Publication number: 20090054235
    Abstract: The present invention relates to novel benzoheterocyclylethylbenzamide derivatives of formula (I) in which the substituents are in the description, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions, and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.
    Type: Application
    Filed: July 6, 2006
    Publication date: February 26, 2009
    Inventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
  • Publication number: 20090047278
    Abstract: The present invention relates to a pharmaceutical composition, a kit and a method for treating cancer, comprising a sulfonamide compound in combination with a substance having an EGF inhibitory activity.
    Type: Application
    Filed: February 28, 2006
    Publication date: February 19, 2009
    Applicant: Eisai R & D Management Co., Ltd.
    Inventors: Takashi Owa, Yoichi Ozawa, Taro Semba, Toshiaki Wakabayashi
  • Publication number: 20090048336
    Abstract: Escitalopram oxalate powders having definite particle size distribution parameters, processes for preparing the powders, and solid pharmaceutical formulations containing the powders.
    Type: Application
    Filed: August 18, 2008
    Publication date: February 19, 2009
    Inventors: Naveen Kumar Kolla, Ravi Ram Elati, Srinivas Gangula
  • Publication number: 20090042875
    Abstract: The present invention relates to substituted heterocyclic compounds and compositions comprising a substituted heterocyclic compound. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof one or more substituted heterocyclic compounds. In particular, the invention relates to methods for preventing or treating cancer or an inflammatory disorder by administering to a subject in need thereof one or more substituted heterocyclic compounds. The present invention further relates to articles of manufacture and kits comprising one or more substituted heterocyclic compounds.
    Type: Application
    Filed: September 29, 2008
    Publication date: February 12, 2009
    Inventors: George W. Muller, Hon-Wah Man
  • Patent number: 7488752
    Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein z,1 represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein A, B, G, M, X, J, n, Het, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
    Type: Grant
    Filed: October 5, 2005
    Date of Patent: February 10, 2009
    Assignee: Schering Corporation
    Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yan Xia, Keith A. Eagen
  • Publication number: 20090035292
    Abstract: Disclosed herein are methods of treating neuroblastomas and medulloblastomas in a subject comprising administering to the subject a phosphatase ligand in an amount effective to treat the subject. Also disclosed herein are method of treating neuroblastomas and medulloblastomas in a subject comprising administering to the subject a histone deacteylase ligand in an amount effective to treat the subject.
    Type: Application
    Filed: August 1, 2008
    Publication date: February 5, 2009
    Inventors: John S. Kovach, Zhengping Zhuang
  • Publication number: 20090036309
    Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.
    Type: Application
    Filed: February 6, 2008
    Publication date: February 5, 2009
    Inventors: John S. Kovach, Francis Johnson
  • Publication number: 20090029947
    Abstract: The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.
    Type: Application
    Filed: March 11, 2008
    Publication date: January 29, 2009
    Inventors: Grier A. Wallace, Eric C. Breinlinger, Kevin P. Cusack, Shannon R. Fix-Stenzel, Thomas D. Gordon, Adrian D. Hobson, Martin E. Hayes, Graham K. Ansell, Pintipa Grongsaard
  • Publication number: 20090030073
    Abstract: A therapeutic agent for a malignant tumor containing a compound represented by the following formula (1) or (2): (wherein each of R1 and R2 represents a methyl group, or R1 and R2 may be linked together to form a methylene group; and R3 represents a hydrogen atom or a methoxy group).
    Type: Application
    Filed: February 15, 2007
    Publication date: January 29, 2009
    Inventors: Takashi Suzuki, Yasuo Fujimoto, Taketo Uchiyama, Keiichi Tabata
  • Publication number: 20090023800
    Abstract: A cannabinoid receptor modulator containing a compound represented by Formula (I0) wherein, X is an oxygen atom, etc., R0 is an optionally substituted acylamino group, ring A0 is a benzene ring which may further have a substituent in addition to R0, and ring B is an optionally substituted 5-membered heterocycle, or a salt thereof or a prodrug thereof.
    Type: Application
    Filed: August 29, 2008
    Publication date: January 22, 2009
    Inventors: Shigenori Ohkawa, Tetsuya Tsukamoto, Yoshihiro Kiyota, Mika Goto, Shouzou Yamamoto, Masato Shimojou, Masaki Setou
  • Publication number: 20090023783
    Abstract: The invention relates to novel benzofuran derivatives, processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders
    Type: Application
    Filed: August 29, 2008
    Publication date: January 22, 2009
    Inventors: Chengzhi Zhang, Jacques Dumas, Gaetan H. Ladouceur, Qian Zhao, Martin Hentemann, Sharad K. Verma, Qingming Zhu, Rico C. Lavoie, Jianmei Fan, Barton Phillips
  • Publication number: 20090023798
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase. Also described herein are methods of using such HDAC inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC activity.
    Type: Application
    Filed: June 16, 2008
    Publication date: January 22, 2009
    Applicant: PHARMACYCLICS, INC.
    Inventors: Darren Magda, Zhong Wang
  • Publication number: 20090018161
    Abstract: The present invention provides a more effective gastrointestinal function promoter. The present invention also provides a method for the prophylaxis or improvement of functional gastrointestinal disorders, a method for appetite regulation and the like. The present invention also provides a method for screening for a substance capable of promoting a gastrointestinal function. The present invention provides a gastrointestinal function promoter containing a T1R agonist as an active ingredient and a method for the prophylaxis or improvement of functional gastrointestinal disorders, a method for appetite regulation and the like by administering a T1R agonist. The present invention also provides a method of screening for a substance capable of promoting a gastrointestinal function which method uses a cell expressing T1R receptor.
    Type: Application
    Filed: May 2, 2008
    Publication date: January 15, 2009
    Applicant: AJINOMOTO CO. INC.
    Inventors: Tatsuro Tanaka, Hisayuki Uneyama, Shinichi Fujita, Saori Ogawa, Yusuke Amino, Seiji Shiraishi, Koichi Fujita, Tatsuhiro Yamada, Takashi Yamamoto, Takeshi Aihara, Manabu Suzuki
  • Patent number: 7476763
    Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I: methods for their production, pharmaceutical formulations containing these compounds, methods of producing such pharmaceutical formulations and related methods of treating or inhibiting certain diseases or conditions.
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: January 13, 2009
    Assignee: Gruenenthal GmbH
    Inventors: Corinna Sundermann, Bernd Sundermann
  • Patent number: 7476690
    Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, Y, R1 and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: January 13, 2009
    Assignee: Cephalon France
    Inventors: Brigitte Lesur, Christophe Yue, Sophie Chasset, Olivier Renault
  • Publication number: 20090012081
    Abstract: An agent for promoting the proliferation or differentiation of a stem cell and/or neural progenitor cell, comprising a compound represented by Formula: wherein each of R1 and R2 is H, a hydrocarbon group or a heterocyclic group, or taken together with the adjacent carbon atom to form a ring, R3 is H, a hydrocarbon group or a heterocyclic group, W is a group represented by Formula: wherein Ring A is an optionally substituted benzene ring, Ring B is an optionally substituted 5- to 7-membered nitrogen-containing heterocyclic ring, R4 is an acyl group having an aliphatic hydrocarbon group, which is substituted by an aromatic group and may have a further substitutent, or aromatic group, R5 is H, C1-6 alkyl or acyl, R4c is an aromatic group, an aliphatic hydrocarbon group or acyl, and X is O or S; Y is O, S or NH, Ring C is an optionally substituted benzene ring, or a salt or prodrug thereof is provided.
    Type: Application
    Filed: December 14, 2007
    Publication date: January 8, 2009
    Applicant: Takeda Pharmaceutical Company Ltd.
    Inventors: Shigenori Okawa, Masaomi Miyamoto, Masahiro Okura