Nitrogen Containing Hetero Ring In The Perservative, Stabilizer, Or Additional Active Ingredient Patents (Class 514/263.32)
  • Publication number: 20110218169
    Abstract: The invention disclosed herein relates to compositions and methods for treating subjects suffering from or at risk of developing neutropenia. In some embodiments, the methods comprise administering to a subject suffering from or at risk of developing neutropenia, an effective amount of pirfenidone and one or more toll-like receptor (TLR) agonists.
    Type: Application
    Filed: February 10, 2011
    Publication date: September 8, 2011
    Applicant: INTERMUNE, INC.
    Inventors: Roderick Phillips, Lawrence M. Blatt
  • Publication number: 20110189130
    Abstract: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
    Type: Application
    Filed: March 22, 2011
    Publication date: August 4, 2011
    Inventors: Takeshi Sagara, Sachie Otsuki, Satoshi Sunami, Toshihiro Sakamoto, Kenji Niiyama, Fuyuki Yamamoto, Takashi Yoshizumi, Hidetomo Furuyama, Yasuhiro Goto, Makoto Bamba, Keiji Takahashi, Hiroshi Hirai, Toshihide Nishibata
  • Publication number: 20110159048
    Abstract: The present invention relates to methods and compositions for reducing Distress Dysfunction by restoring and maintaining homeostatic balance in the neurotransmitter systems underlying the Stress Response and the experience of distress and hedonic tone. Distress Dysfunction refers to the experience of dysfunctional emotional and physical distress that interferes with the individual's quality of life and functioning.
    Type: Application
    Filed: December 20, 2010
    Publication date: June 30, 2011
    Inventors: Steven Crain, William E. Crain, Stanley M. Crain, Michael Crain
  • Publication number: 20110129546
    Abstract: The invention relates to a dermatological pharmaceutical composition for the treatment of skin inflammation diseases, such as dermatitis, atopic dermatitis, vitiligo, alopecia areata, acne, psoriasis and pruritus. The invention comprises a base anti-inflammatory agent, such as indometacin; one or more optional active ingredients selected alternatively from among at least a corticoid and an antibiotic; and a combination of topical antioxidants used to potentiate the anti-inflammatory effect, selected from among green tea, lipoic acid, curcumin, ascorbyl palmitate, Coenzyme Q10, resveratrol, Pycnogenol™, L-camosine, taurine, vitamin E, vitamin C, papaya extract, isoflavones, manganese, lycopene and quercetin. At least one of the topical antioxidants is a peroxisome proliferator-activated receptor-gamma (PPAR-?) activator. The invention also includes at least one antioxidant substance with an antiproliferative effect on keratonocytes, e.g.
    Type: Application
    Filed: June 19, 2009
    Publication date: June 2, 2011
    Inventor: Ignacio Umbert Mill
  • Publication number: 20110123547
    Abstract: Compounds of general formula (II) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(?O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C?O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
    Type: Application
    Filed: January 31, 2011
    Publication date: May 26, 2011
    Applicant: Oxagen Limited
    Inventors: Richard Edward Armer, Eric Roy Pettipher, Mark Whittaker, Graham Michael Wynne, Julia Vile, Frank Schroer
  • Publication number: 20110052527
    Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
    Type: Application
    Filed: November 10, 2010
    Publication date: March 3, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Lawrence S. Melvin, JR., Michael Graupe, Chandrasekar Venkataramani
  • Publication number: 20110038832
    Abstract: Provided herein are methods of treating macular degeneration, which comprises administering to a patient in need thereof a therapeutically effective amount of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, or a pharmaceutically acceptable salt or solvate thereof.
    Type: Application
    Filed: August 16, 2010
    Publication date: February 17, 2011
    Inventor: Jerome B. ZELDIS
  • Patent number: 7879864
    Abstract: Compounds for the treatment of elevated blood glucose levels and the physiological and metabolic disorders arising therefrom are disclosed which are inhibitors of the enzyme dipeptidyl peptidase IV (DDP-IV) and comprise novel substituted bicyclic 8-pyrrolidinoxanthines of formula I and their derivatives: wherein the various R-groups are defined herein. These compounds may be combined with other secondary active compounds which also are effective in the treatment of said disorders and the disease states or physiological manifestations arising therefrom.
    Type: Grant
    Filed: February 13, 2007
    Date of Patent: February 1, 2011
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Karl Schoenafinger, Gerhard Jaehne, Elisabeth Defossa, Christian Buning, Georg Tschank, Ulrich Werner
  • Publication number: 20110003016
    Abstract: A hair treatment composition comprising a trichogenic material and an anti-dandruff agent.
    Type: Application
    Filed: October 23, 2008
    Publication date: January 6, 2011
    Inventors: Jason Shaun Burry, Richard Livesey Evans, Graham Andrew Turner
  • Publication number: 20100266535
    Abstract: Compounds of general formula (II) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(?O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C?O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
    Type: Application
    Filed: July 1, 2010
    Publication date: October 21, 2010
    Applicant: Oxagen Limited
    Inventors: Richard Edward ARMER, Eric Roy Pettipher, Mark Whittaker, Graham Michael Wynne, Julia Vile, Frank Schroer
  • Patent number: 7807683
    Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: March 31, 2006
    Date of Patent: October 5, 2010
    Assignee: Schering Corporation
    Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Alan Mallams, Carmen S. Alvarez, Kartik M. Keertikar, Jocelyn Rivera, Tin Yau Chan, Vincent Madison, Thierry O. Fischmann, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park, Vidyadhar M. Paradkar, Douglas Walsh Hobbs
  • Publication number: 20100221211
    Abstract: The invention relates to a compound of general formula (I-0): wherein R1 means a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, or a C3-C6 cycloalkyl group; R2, R3, R4 and R5 mean a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group, or a halo-C1-C6 alkoxy group; R6 means a hydrogen atom, or a C1-C6 alkyl group; R7a means a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group, a hydroxy-C1-C6 alkyl group, -Q2-N(R1c)R1d or a nitrogen-containing heterocyclic group; R8a means a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group or a hydroxy-C1-C6 alkyl group; or R7a and R8a form, as taken together, a C2-C6 alkylene group, or R7a and R8a and the ring atoms to which they bond may form a spiro ring or a bicyclo ring; and X and Y mean a methine group or a nitrogen atom.
    Type: Application
    Filed: October 20, 2008
    Publication date: September 2, 2010
    Inventors: Hidetomo Furuyama, Mikako Kawamura, Toshihiro Sakamoto, Fuyuki Yamamoto, Takashi Yoshizumi
  • Publication number: 20100190752
    Abstract: A composition of matter comprising in combination as component (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and as component (b) at least one antiepileptic, a pharmaceutical formulation and a dosage form comprising said composition of matter, and a method of treating pain, e.g. neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, whereby component (a) may be administered before or after component (b) and whereby components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.
    Type: Application
    Filed: January 26, 2010
    Publication date: July 29, 2010
    Applicant: Gruenenthal GmbH
    Inventors: Klaus Schiene, Petra Bloms-Funke, Thomas Christoph
  • Publication number: 20100189819
    Abstract: Neuro-metabolic and endocrine-function regulating/modulating compositions, are disclosed. The compositions of the present invention comprise Selegiline Hydrochloride, Procaine Hydrochloride, Vinpocetine, trimethylglycine, and an ingredient selected from a group consisting of N-nicotinoyl-gamma-aminobutyric acid (N-GABA), niacin, niacinamide, gamma-aminobutyric acid (GABA), and combinations thereof. Methods of using the compositions, compositions, and compositions of the present invention are also disclosed.
    Type: Application
    Filed: April 5, 2010
    Publication date: July 29, 2010
    Applicant: INTRATHERAPIES LLC
    Inventor: Nathan SASSOVER
  • Patent number: 7763626
    Abstract: Compositions and methods for inhibiting opioid tolerance and opioid withdrawal-induced hyperalgesia are provided.
    Type: Grant
    Filed: May 16, 2005
    Date of Patent: July 27, 2010
    Assignee: Trustees of Dartmouth College
    Inventor: Joyce A. DeLeo
  • Publication number: 20100144718
    Abstract: The invention provides a method for the treatment of H4R modulated diseases and/or conditions comprising administering to the subject an effective amount of a H4R agonist. The invention also provides a method for treating COPD comprising administering to the subject an effective amount of a H4R agonist, a H1R antagonist and an anticholinergic drug. Further, the invention provides a pharmaceutical formulation comprising a H4R agonist, a second active agent and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: June 17, 2009
    Publication date: June 10, 2010
    Inventors: Michalis Nicolaou, Emile Loria, Gaetan Terrasse, Yves Trehin
  • Publication number: 20100112090
    Abstract: [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.
    Type: Application
    Filed: April 16, 2008
    Publication date: May 6, 2010
    Applicant: KISSEI PHARMACEUTICAL CO., LTD
    Inventors: Shigeru Yonekubo, Takashi Miyagi, Kohsuke Ohno, Mikie Kambara, Nobuhiko Fushimi
  • Publication number: 20100075935
    Abstract: The present invention relates to new xanthine modulators of adenosine A1 receptors, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: August 24, 2009
    Publication date: March 25, 2010
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventors: Thomas G. Gant, Manouchehr M. Shahbaz
  • Publication number: 20100003330
    Abstract: The present invention relates to compositions and methods for decreasing the infectivity, morbidity, and rate of mortality associated with a variety of pathogenic organisms and viruses. The present invention also relates to methods and compositions for decontaminating areas colonized or otherwise infected by pathogenic organisms and viruses. Moreover, the present invention relates to methods and compositions for decreasing the infectivity of pathogenic organisms in foodstuffs.
    Type: Application
    Filed: June 25, 2002
    Publication date: January 7, 2010
    Applicant: The Regents of the University of Michigan
    Inventors: James R. Baker, JR., Tarek Hamouda, Amy Shih, Andrzej Myc
  • Publication number: 20090197825
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: November 26, 2008
    Publication date: August 6, 2009
    Applicant: ARDEA BIOSCIENCES, INC.
    Inventors: Barry D. QUART, Jean-Luc GIRARDET, Esmir GUNIC, Li-Tain YEH
  • Publication number: 20090191183
    Abstract: Disclosed herein are substituted indole cysteinyl leukotriene receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: July 29, 2008
    Publication date: July 30, 2009
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Publication number: 20090093503
    Abstract: A combination which comprises (a) a PDE4 inhibitor and (b) an antagonist of M3 muscarinic receplors which is (3R)-1-phencthyl-3-(9H-xanthene-9carbonyloxy)-1-azoniabicyclo[2.2.2]octanc, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid.
    Type: Application
    Filed: December 16, 2008
    Publication date: April 9, 2009
    Applicant: Laboratorios Almirall, S.A.
    Inventors: Jordi Gras Escardo, Jesus Llenas Calvo, Hamish Ryder, Pio Orviz Diaz
  • Patent number: 7514442
    Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: March 31, 2006
    Date of Patent: April 7, 2009
    Assignees: Schering Corporation, Pharmacopeia, Inc.
    Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Carmen S. Alvarez, Tin Yau Chan, Chad Knutson, Vincent Madison, Thierry O. Fischmann, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park
  • Patent number: 7470714
    Abstract: An antitumor effect enhancer for enhancing the antitumor effects of an antitumor substance, which comprises a compound represented by the following formula (1): wherein each R independently represents a hydrogen atom, a lower alkyl group, an aryl group, an allyl group, an aralkyl group, a halogen atom, a hydroxyl group, an amino group, R?O—, R?(C?O)—, R?(C?O)O—, or R?O(C?O)—, wherein R? is an alkyl group containing 1 to 5 carbon atoms, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 4, 2004
    Date of Patent: December 30, 2008
    Assignee: Sosei Co., Ltd.
    Inventors: Kazuo Shinya, Tetsuzo Tauchi, Toshiro Morohoshi, Takashi Ono
  • Patent number: 7470695
    Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: March 31, 2006
    Date of Patent: December 30, 2008
    Assignee: Schering Corporation
    Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park
  • Patent number: 7468372
    Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: March 31, 2006
    Date of Patent: December 23, 2008
    Assignee: Schering Corporation
    Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Chad Knutson, Brian McKittrick, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park
  • Publication number: 20080207644
    Abstract: Disclosed are methods for treating various cancers. Methods encompass the administration of an mTOR inhibitor in combination with a second drug selected from an ImiD, a PDE4 inhibitor, a p38 MAP kinase inhibitor, a xanthine anticytokine, a dual TACE/MMP inhibitor and a proteasome inhibitor. The methods are aimed at providing a desirable therapeutic window while maintaining prior, if not higher, dose levels of the mTOR inhibitor.
    Type: Application
    Filed: November 27, 2007
    Publication date: August 28, 2008
    Inventors: Stephen T. Sonis, Camille L. Bedrosian
  • Publication number: 20080167326
    Abstract: The present invention relates to the discovery of an association between the gene encoding FGF-BP1 (fibroblast growth factor-binding protein) and chronic obstructive pulmonary disease (COPD). The invention identifies a role for FGF-BP1 in COPD. The present invention therefore relates to diagnostic techniques for the detection of COPD by detecting all or part of this gene, its precursors or products (mRNA, cDNA, genomic DNA, or protein). The present invention also provides methods and as-says for identifying compounds which modulate FGF-BP1 and which may be used for treating respiratory diseases such as COPD. Furthermore, the invention relates to polymorphisms in the genes encoding FGF-BP1. The invention also relates to the use of polymorphisms in the FGF-BP1-encoding genes in assessing predisposition and/or susceptibility of an individual to chronic obstructive pulmonary disease (COPD).
    Type: Application
    Filed: April 3, 2006
    Publication date: July 10, 2008
    Applicant: ASTRAZENECA AB
    Inventors: Witte Koopmann, Simon Smith
  • Publication number: 20080139584
    Abstract: A method for healing a wound comprising the steps of: topically administering a wound healing composition to a wounded area, wherein the wound healing composition comprises: a first medicament characterized as a calcium channel blocker or pharmaceutically acceptable salts or solvates thereof; a second medicament characterized as a hemorrheologic agent or pharmaceutically acceptable salts or solvates thereof; and a dermal penetrating agent or pharmaceutically acceptable salts or solvates thereof.
    Type: Application
    Filed: October 29, 2007
    Publication date: June 12, 2008
    Inventors: Matthew H. Kopacki, Michael J. Torsiello
  • Publication number: 20080113902
    Abstract: The invention features a method of treating or preventing a disease associated with the use of antibiotics in a patient in need thereof by administering to the patient ramoplanin in an amount and for a duration effective to treat said disease. The disease may be caused, for example, by the presence of a bacterium such as enterotoxin producing strains of C. difficile, C. perfringens, or S. aureus.
    Type: Application
    Filed: October 3, 2007
    Publication date: May 15, 2008
    Applicant: Oscient Pharmaceuticals Corporation
    Inventors: Daniela Jabes, Timothy S. Leach, Richard F. Labaudiniere, Steven M. Rauscher, Giorgio Mosconi
  • Publication number: 20080085858
    Abstract: The present invention provides a pharmaceutical composition comprising (a) a phosphodiesterase (PDE)-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) an immunosuppressant, a therapeutic and/or preventive agent for chronic skin diseases comprising (a) a PDE-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) an immunosuppressant, a therapeutic and/or preventive agent for chronic skin diseases to be administered simultaneously or separately with an interval comprising (a) a PDE-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) an immunosuppressant, as active ingredients; and the like.
    Type: Application
    Filed: October 13, 2005
    Publication date: April 10, 2008
    Applicant: KYOWA HAKKO KOGYO CO., LTD.
    Inventors: Daisuke Harada, Katsuya Kobayashi, Haruhiko Manabe, Etsuo Ohshima
  • Publication number: 20080025949
    Abstract: This invention is in the field of chemical restructuring of pharmaceutical agents known to cause tissue toxicity as a side effect, by producing their orotate derivatives. More particularly, it concerns orotate derivatives of the anthracyclines, doxorubicin and daunorubicin, that are found to reduce levels of the pharmaceutical agent in noncancerous tissues. There orotate derivatives are equally efficacious in inhibiting the SCCAKI-1 kidney tumor in animals and the reduction in the heart tissue of doxorubicin compared with doxorubicin HCl suggests a reduction in toxicity induced by free radical generation by the anthrracyclines.
    Type: Application
    Filed: July 31, 2006
    Publication date: January 31, 2008
    Inventor: Rashida A. Karmali
  • Publication number: 20070270362
    Abstract: Methods and compositions are provided for treating inflammatory-related diseases and related disorders in a mammalian subject. The method provides administering to the mammalian subject one or more modulators of cyclin dependent kinase 4 (Cdk4) activity in an amount effective to reduce or eliminate the inflammatory-related disease or disorder or prevent its occurrence or recurrence. Methods are also provided for reducing or eliminating ligand-induced adhesion in a mammalian subject. The method provides administering to the subject one or more modulators of cyclin dependent kinase 4 (Cdk4) activity in an amount effective to reduce or eliminate ligand-induced adhesion.
    Type: Application
    Filed: May 18, 2006
    Publication date: November 22, 2007
    Applicant: The University of Washington
    Inventors: John M. Harlan, Lynn M. Schnapp, Barbara R. Schwartz, Li Liu, Elaine White Raines, Yoshiaki Tsubota
  • Patent number: 7192962
    Abstract: Crystalline polymorphs of 1-ethyl-3,7-dihydro-8-[(1R,2R) -(hydroxycyclopentyl)amino]-3-(2-hydroxyethyl)-7-[(3-bromo-4-methoxyphenyl)methyl]-1H-Purine-2,6-dione in Form 1 and Form 2, which exhibit x-ray powder diffraction profiles substantially the same as those shown in FIGS. 5 and 6, respectively, and which exhibit differential scanning calorimtery profiles substantially the same as those shown in FIGS. 2 and 4, respectively, and are represented by the formula: Pharmaceutical compositions comprising the polymorph Form 1 or 2 of Compound 13 and at least one excipient or carrier, and methods of using the polymorph Form 1 or 2 of Compound 13 to treat a variety of physiological disorders, such as erectile dysfunction.
    Type: Grant
    Filed: May 30, 2003
    Date of Patent: March 20, 2007
    Assignee: Schering Corporation
    Inventors: Vilas H. Dahanukar, Hoa N. Nguyen, Cecilia A. Orr, Funcheng Zhang, Ilia A. Zavialov, Kevin Klopfer, Jeffrey M. Skell, Albert W. Buchholz, Jr., Craig D. Boyle
  • Patent number: 6995164
    Abstract: The invention provides a method of inhibiting tumor growth in a mammal, by administering to the mammal composition containing taurolidine, taurultam, or a biologically active derivative thereof. The composition is administered to directly contact a tumor cell at a dose sufficient to induce cell death by apoptosis.
    Type: Grant
    Filed: November 21, 2002
    Date of Patent: February 7, 2006
    Assignee: Rhode Island Hospital
    Inventors: Paul Calabresi, James Darnowski
  • Publication number: 20040259809
    Abstract: The present invention provides pharmaceutical compositions including a sedating antihistamine and a stimulant, and methods of use thereof. The stimulant reduces the sedation caused by the antihistamine, thereby allowing potent, but sedating, antihistamines to be used effectively.
    Type: Application
    Filed: June 17, 2003
    Publication date: December 23, 2004
    Applicant: PediaMed Pharmaceuticals, Inc.
    Inventor: Gilbert Rene Gonzales
  • Publication number: 20040254202
    Abstract: The present invention is directed to a method of promoting sleep by topically applying onto the skin a composition that comprises a non-hypnotic, vasoactive agent. The non-hypnotic, vasoactive agent is highly effective in providing for the improved quality of sleep through the use of topical application.
    Type: Application
    Filed: June 13, 2003
    Publication date: December 16, 2004
    Applicant: The Procter & Gamble Company
    Inventor: James Patrick Ebel
  • Publication number: 20040204339
    Abstract: Compositions and methods are provided for treating diseases associated with aberrant silencing of gene expression such as cancer by reestablishing the gene expression through inhibition of DNA hypomethylation and histone deacetylase. The method comprises: administering to a patient suffering from the disease a therapeutically effective amount of a DNA methylation inhibitor such as a cysteine analog such as decitabine, in combination with an effective amount of histone deacetylase inhibitor such as hydroxamic acid, cyclic peptide, benzamide, butyrate, and depudecin.
    Type: Application
    Filed: April 24, 2001
    Publication date: October 14, 2004
    Inventor: Jorge F. DiMartino
  • Publication number: 20040202677
    Abstract: A method of enhancing regional body fat reduction is disclosed. The method includes topically applying a fat reduction topical composition on a region of a human body where a regional fat reduction is desired for a treatment period, and administering an amount of a fat reduction oral composition daily during the treatment period. The topical composition includes hydroglycolic fluid extract of Palmaria palmata, Laminaria digitata extract, mannitol, and a pharmaceutically acceptable carrier. The oral composition includes synephrine, methylxanthine, chromium, a herbal combination having diuretic effect and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: April 8, 2004
    Publication date: October 14, 2004
    Inventors: Kevin J. Hopkins, Gerard Dente
  • Publication number: 20040198695
    Abstract: A series of beverages and/or foods, which have protecting and enhancing effects on human's joints and bones and can therefore prevent and treat osteoarthritis, is provided. The beverages and/or foods comprise one or more cartilage- and synovial fluid-enhancing active ingredients or combinations of these ingredients with bone-enhancing calcium and phosphorus additives. Active ingredients in these beverages and/or foods are taken in liquid forms. So they can be easily absorbed and utilized thoroughly by human body.
    Type: Application
    Filed: March 5, 2004
    Publication date: October 7, 2004
    Inventors: Anhu Li, Qingren Xu
  • Publication number: 20040180909
    Abstract: Disclosed herein are a process for producing mixed crystals of disodium 5′-guanylate and disodium 5′-inosinate which comprises precipitating mixed crystals of disodium 5′-guanylate and disodium 5′-inosinate (I+G mixed crystals) by adding an aqueous mixed solution of disodium 5′-guanylate and disodium 5′-inosinate and a hydrophilic organic solvent at the same time into a crystallization vessel in such manner that the ratio of the hydrophilic organic solvent to the liquid phase in the crystallization vessel is maintained in a range of 30 to 70 vol %, as well as such process for producing I+G mixed crystals wherein said producing of I+G mixed crystals is carried out by seeding crystallization wherein crystals of 5′-IMP2Na or/and I+G mixed crystals are used as seed crystals.
    Type: Application
    Filed: January 5, 2004
    Publication date: September 16, 2004
    Inventors: Toyokazu Kaneko, Yasuo Yonou, Naoto Hirano, Shigematsu Abe, Kunihiko Toumori
  • Publication number: 20040157784
    Abstract: A composition comprising the tannate of an opioid. Suitable opioids include alfentanil, buprenorphine, butorphanol, carfentanil, cocaine, codeine, dezocine, diacetylmorphine, dihydrocodeine, dihydromorphine, diphenoxylate, diprenorphine, etorphine, fentanyl, heroin, hydrocodone, hydromorphone, &bgr;-hydroxy-3-methylfentanyl, levo-&agr;-acetylmethadol, levorphanol, lofentanil, meperidine, methadone, morphine, nalbuphine, nalmefene, o-methylnaltrexone, naloxone, naltrexone, oxycodone, oxymorphone, pentazocine, pethidine, propoxyphene, remifentanil, sufentanil, tilidine and tramadol. The opioid tannate may be readily prepared by reacting an opioid free base with tannic acid, either neat or in the presence of up to about 30 wt. % water, at a temperature of about 60 to about 150° C. and thereafter recovering the resultant opioid tannate. The opioid tannate may also be prepared by an alternative process that involves reacting the opioid free base with water at a temperature such that not more than about 10 wt.
    Type: Application
    Filed: December 12, 2003
    Publication date: August 12, 2004
    Applicant: Jame Fine Chemicals, Inc.
    Inventors: Vilas M. Chopdekar, Sham N. Redkar, James R. Schlek
  • Publication number: 20040147534
    Abstract: The present invention provides a topical composition comprising about 6% to about 15% nifedipine and about 6% to about 15% pentoxifylline for treating severe vascular occlusive wounds. The present invention also provides a method and a kit for treating the vascular occlusive wound by applying the composition to the open wound, and cleaning and dressing the wound at least once daily.
    Type: Application
    Filed: January 23, 2003
    Publication date: July 29, 2004
    Inventors: Mary Ann Foote, Mark Harlan Mandel
  • Publication number: 20040101582
    Abstract: Methods and compositions for the topical or transdermal treatment of neuropathy. More particularly, transdermal or topical compositions including a combination of ingredients that provide a surprising degree of effective relief from the symptoms of peripheral neuropathy and methods for administering the compositions to treat various neuropathies.
    Type: Application
    Filed: November 25, 2002
    Publication date: May 27, 2004
    Inventor: Richard Wolicki
  • Publication number: 20040058018
    Abstract: A method of treating gastric acid disorders by administering to a patient a pharmaceutical composition comprising a proton pump inhibitor (PPI) in a pharmaceutically acceptable carrier.
    Type: Application
    Filed: August 15, 2003
    Publication date: March 25, 2004
    Applicant: THE CURATORS OF THE UNIVERSITY OF MISSOURI
    Inventor: Jeffrey O. Phillips
  • Publication number: 20030219500
    Abstract: A composition for human consumption, comprising creatine and creatinine, the latter being in sufficient quantity to render creatine in an aqueous medium substantially stable, and a methyl xanthine; and a method of making the composition is provided.
    Type: Application
    Filed: February 20, 2003
    Publication date: November 27, 2003
    Inventors: Alan N. Howard, Roger C. Harris
  • Publication number: 20030215527
    Abstract: A method of treating gastric acid disorders by administering to a patient a pharmaceutical composition comprising a proton pump inhibitor (PPI) in a pharmaceutically acceptable carrier.
    Type: Application
    Filed: April 4, 2003
    Publication date: November 20, 2003
    Inventor: Jeffrey Owen Phillips
  • Publication number: 20030215442
    Abstract: The present invention provides methods of suppressing immune disorders such as allograft rejection in a patient by a combination of inhibition of the binding of LIGHT to HVEM and immunosuppressive therapy. Various therapeutic regimens are provided. The present invention further provides kits and pharmaceutical compositions useful in the present methods.
    Type: Application
    Filed: February 19, 2003
    Publication date: November 20, 2003
    Inventors: Christopher C. Fraser, Wayne Hancock
  • Publication number: 20030213006
    Abstract: The present invention relates to promoters, enhancers and other regulatory elements that direct expression within tumor cells, comprising nucleotide sequences from the 5′ regulatory region, and transcriptionally active fragments thereof, that control expression of a testicular carcinoma related protein, &bgr;-HCG. Specifically provided are expression vectors, host cells and transgenic animals wherein an &bgr;-HCG regulatory region is capable of controlling expression of a heterologous gene, over-expressing an endogenous gene or an inhibitor of a pathological process or knocking out expression of a specific gene believed to be important in cancer development and/or progression. The invention also relates to methods for using said vectors, cells and animals for screening candidate molecules for agonists and antagonists of cancer development and/or progression.
    Type: Application
    Filed: March 31, 2003
    Publication date: November 13, 2003
    Inventors: Ri-Hyun Back, Thomas A. Gardner, Akinobu Gotoli
  • Publication number: 20030212033
    Abstract: A weight reduction and inhibition of Hypertriglyceridemia medicine contain ATP as an effective ingredient, and more particularly to one that takes advantage of a cyclic adenosine monophosphate, Cyclic AMP) produced from the decomposed ATP in human body to promote the increase of lipase, thus to activate the metabolism and decomposition of triglyceride in the human body.
    Type: Application
    Filed: May 8, 2002
    Publication date: November 13, 2003
    Inventor: Chao Song Hsue