The Ring Nitrogen Is Bonded Directly To Nonshared Ring Carbons Of The Five-membered Hetero Ring (e.g., Isoindole, Etc.) Patents (Class 514/416)
  • Patent number: 7569597
    Abstract: Novel isoindoline compounds are disclosed. Methods of treating, preventing and/or managing cancer, diseases and disorders associated with, or characterized by, undesired angiogenesis, and diseases and disorders mediated by PDE 4, using the compounds are also disclosed.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: August 4, 2009
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man
  • Publication number: 20090176858
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: December 19, 2008
    Publication date: July 9, 2009
    Applicant: Avila Therapeutics, Inc.
    Inventors: Deqiang Niu, Russell C. Petter, Juswinder Singh, Arthur F. Kluge, Lixin Qiao
  • Patent number: 7557114
    Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. Compounds of the invention are GlyT-1 inhibitors and are useful for the treatment of CNS disorders such as psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders, or Alzheimer's disease.
    Type: Grant
    Filed: January 31, 2006
    Date of Patent: July 7, 2009
    Assignee: Hoffman-La Roche Inc.
    Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
  • Publication number: 20090170842
    Abstract: A pharmaceutical composition for use in treating, inhibiting, and/or preventing breast and/or ovarian cancer can include: a molecule having a structure of one of Compounds 1-38, pharmaceutically acceptable salt thereof, or analog thereof, and a pharmaceutically acceptable carrier containing the compound. The pharmaceutically acceptable carrier can be configured for oral, systemic, transdermal, intranasal, suppository, parenteral, intramuscular, intravenous, or subcutaneous administration. The compound can be present in the composition in a therapeutically effective amount for treating, inhibiting, and/or preventing breast and/or ovarian cancer. Also, the compound can be present in a therapeutically effective amount for enhancing production of BRCA1.
    Type: Application
    Filed: November 13, 2008
    Publication date: July 2, 2009
    Applicant: University of Kansas
    Inventors: Roy A. Jensen, Lisa M. Harlan-Williams, Frank J. Schoenen, Jeffrey Aube, Gerald H. Lushington
  • Publication number: 20090170835
    Abstract: Provided is a novel isoindoline compound of the formula (I): The compound is useful for anesthesia by inducing sedation in a mammal.
    Type: Application
    Filed: December 30, 2008
    Publication date: July 2, 2009
    Inventors: Kouhei Toyooka, Norimasa Kanamitsu, Masakazu Yoshimura, Haruo Kuriyama, Takashi Tamura
  • Publication number: 20090149505
    Abstract: Compounds of Formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the description, processes for the preparing such compounds, new intermediates employed in their preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.
    Type: Application
    Filed: February 6, 2007
    Publication date: June 11, 2009
    Applicant: AstraZeneca AB
    Inventors: James R. Empfield, James J. Folmer, James R. Arnold, Joshua Clayton, Abdelmalik Slassi, Methvin Isaac, Ian Egle, Fupeng Ma
  • Publication number: 20090143382
    Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.
    Type: Application
    Filed: January 30, 2009
    Publication date: June 4, 2009
    Inventors: George W. Muller, Hon-Wah Man, Weihong Zhang
  • Patent number: 7531569
    Abstract: A method and apparatus for preventing board warpage during the application and curing or drying of liquid epoxies, or the like, on printed circuit boards using a clamping fixture assembly, which includes at least one clamping fixture support and at least one clamping fixture overlay. If desired, a plurality of printed circuit boards may be processed using an appropriate clamping fixture assembly. Furthermore, the clamping fixture may be constructed so a slight bow or curvature thereof can counter either a convex or concave bow or curvature of the printed circuit board. In the method, at least one printed circuit board is mounted to a clamping fixture support whereby a clamping fixture overlay is placed on top of the first printed circuit board.
    Type: Grant
    Filed: December 1, 2004
    Date of Patent: May 12, 2009
    Assignee: sanofi-aventis Deutschland GmbH
    Inventors: Gerrit Schubert, Joerg Rieke-Zapp, Johannes Keil, Heinz-Werner Kleemann, Reda Hanna, Bao-Guo Huang, Xiao-Dong Wu, Yves Gouraud
  • Publication number: 20090118268
    Abstract: This invention relates to the use of a group of aryl ureas in treating p38 mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: October 10, 2008
    Publication date: May 7, 2009
    Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
  • Patent number: 7528165
    Abstract: This invention relates to methods of inhibiting tubulin polymerization and treating cancer and other angiogenesis-related disorders with indole compounds of the formula: wherein L1, L2, R1, R2, Ra, Rb, Rc, Rd, and Re are defined herein.
    Type: Grant
    Filed: August 1, 2005
    Date of Patent: May 5, 2009
    Assignee: National Health Research Institutes
    Inventors: Hsing-Pang Hsieh, Jing-Ping Liou, Jang-Yang Chang, Chun-Wei Chang
  • Publication number: 20090099186
    Abstract: The embodiments provide compounds of the general Formulas I-IV, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
    Type: Application
    Filed: October 10, 2006
    Publication date: April 16, 2009
    Inventors: Leonid Beigelman, Steven W. Andrews, Kevin R. Condroski, Indrani Gunawaradana, Julia Haas
  • Publication number: 20090082368
    Abstract: Disclosed are compositions which modulate the interaction with nerve growth factor and precursors thereof with neurotrophic receptors. Also disclosed are methods of using the compositions of the invention, including methods of administration.
    Type: Application
    Filed: September 24, 2008
    Publication date: March 26, 2009
    Applicant: PainCeptor Pharma Corporation
    Inventors: Rahul VOHRA, Gilles Dube, Zhonghong Gan, Nachhattarpal Gill, Xilin Cui
  • Publication number: 20090075978
    Abstract: The present invention relates to substituted propiolic acid amides, to methods for the production thereof, to medicaments containing these compounds and to the use thereof for producing medicaments.
    Type: Application
    Filed: June 26, 2008
    Publication date: March 19, 2009
    Applicant: Grunenthal GmbH
    Inventors: Michael HAURAND, Klaus SCHIENE, Sven KUHNERT, Melanie REICH, Saskia ZEMOLKA
  • Patent number: 7504427
    Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.
    Type: Grant
    Filed: November 16, 2006
    Date of Patent: March 17, 2009
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man, Weihong Zhang
  • Publication number: 20090062284
    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 that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.
    Type: Application
    Filed: August 27, 2008
    Publication date: March 5, 2009
    Applicant: Cephalon, Inc.
    Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, Marie-Edith Gourdel, Greg A. Hostetler, Mohamed Iqbal, Brigitte Lesur, Philippe Louvet, Eric Riguet, Dominique Schweizer, Christophe Yue
  • Publication number: 20090054462
    Abstract: The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
    Type: Application
    Filed: June 23, 2006
    Publication date: February 26, 2009
    Inventors: Jinlong Jiang, Robert J. DeVita, Sanjeev Kumar, Sander G. Mills, Richard A. Tschirret-Guth
  • Patent number: 7485643
    Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, R10, R20, R21, and R22 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: November 18, 2004
    Date of Patent: February 3, 2009
    Assignee: Array BioPharma Inc.
    Inventors: Eli Wallace, Joseph P. Lyssikatos, Hong Woon Yang
  • Publication number: 20090030063
    Abstract: For controlling the condition of type 2 diabetes, a pharmaceutical including a combination of mitiglinide, a pharmacologically acceptable salt thereof or a hydrate thereof and an ?-glucosidase inhibitor such as voglibose or acarbose, and a therapeutic method using the pharmaceutical are provided. The pharmaceutical according to the present invention has an extremely strong effect of decreasing a morning fasting blood glucose level, a postprandial blood glucose level and HbA1C of a patient with type 2 diabetes, and can improve glucose spike, insulin resistance and lipid metabolism.
    Type: Application
    Filed: April 18, 2006
    Publication date: January 29, 2009
    Inventors: Yuji Kiyono, Yoshio Okubo, Katsumi Hontani, Imao Mikoshiba, Kazuma Ojima
  • Publication number: 20090031435
    Abstract: This invention relates to therapies for diseases involving splicing defects, such as spinal muscular atrophy (SMA), and methods to identify compounds for treating this disease. The invention specifically provides for therapies comprised of small molecule compounds identified by cell-based high-throughput screening assays. These assays utilize engineered splicing constructs that fuse pre-mRNA fragments to a reporter gene. The fragments contain exons and at least one intron of a gene mutated in such a way to cause disease. Additionally, the invention provides for methods to monitor the effects of drugs on splicing and gene expression in vivo, in transgenic animals.
    Type: Application
    Filed: November 29, 2007
    Publication date: January 29, 2009
    Inventors: Brent R. Stockwell, David E. Root
  • Publication number: 20090030064
    Abstract: A preparation wherein an active ingredient unstable to oxygen is stabilized by coating a portion containing the active ingredient unstable to oxygen with a sugar-coated layer containing (1) sugar alcohol as a sugar-coating base material and (2) a binder is provided.
    Type: Application
    Filed: June 9, 2006
    Publication date: January 29, 2009
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Yoshihiro Uchiyama, Yoshinori Nakano
  • Patent number: 7482336
    Abstract: The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: June 17, 2005
    Date of Patent: January 27, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Danqing Feng, Ying-Duo Gao, Suresh Singh, Ann E. Weber
  • Patent number: 7482472
    Abstract: The invention relates to coagulation of the blood. Disclosed are novel compounds of formula (I), a method for the production of these compounds, pharmaceutical compositions containing them, and methods of using them for the prevention and/or treatment of various diseases.
    Type: Grant
    Filed: March 12, 2007
    Date of Patent: January 27, 2009
    Assignee: Bayer Healthcare AG
    Inventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Rohrig, Elisabeth Perzborn, Karl-Heinz Schlemmer
  • Publication number: 20090017003
    Abstract: The present invention relates to novel thiosulfonates derivatives. The present invention also provides methods for preventing, treating and/or reducing inflammation-associated diseases in the cardiovascular, connective tissue, pulmonary, gastrointestinal, respiratory, urogenital, nervous or cutaneous systems as well as infective and tumoral diseases employing said compounds.
    Type: Application
    Filed: March 1, 2007
    Publication date: January 15, 2009
    Applicant: SULFIDRIS S.R.L.
    Inventors: Piero Del Soldato, Giancarlo Santus, Anna Sparatore
  • Publication number: 20090010886
    Abstract: Methods of treating, preventing and/or managing a myeloproliferative disease are disclosed. Specific methods encompass the administration of a selective cytokine inhibitory drug, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active agent, and/or the transplantation of blood or cells. Particular second active agent is capable of suppressing the overproduction of hematopoietic stem cells or ameliorating one or more of the symptoms of MPD. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
    Type: Application
    Filed: May 5, 2004
    Publication date: January 8, 2009
    Applicant: CELGENE CORPORATION
    Inventor: Jerome B. Zeldis
  • Patent number: 7468387
    Abstract: Imidoalkancarboxylic acids of formula (I) are described, wherein A, X and M are as defined in the application, said acids being in a crystalline form which in contact with water gives rise to crystals having sizes lower than 30 micron.
    Type: Grant
    Filed: July 8, 2003
    Date of Patent: December 23, 2008
    Assignee: Solvay Solexis S.p.A.
    Inventors: Ugo Piero Bianchi, Roberto Garaffa
  • Patent number: 7456183
    Abstract: Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH2, N, NR9, C?O, C?S, S?O, SO2, S, O, (CR6R7)n, C(?O)—(CR6R7)n, and C(?S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S?O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: November 25, 2008
    Assignee: Novartis Vaccines and Diagnostics, Inc.
    Inventors: Daniel Chu, Rustum Boyce, David Duhl, Bryan Chang
  • Patent number: 7446123
    Abstract: This invention generally relates to muscarinic receptor antagonists of formula (I) which are useful, among other uses for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through muscarinic receptors.
    Type: Grant
    Filed: January 7, 2004
    Date of Patent: November 4, 2008
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Mohammad Salman, Anita Mehta, Pakala Kumara Savithru Sarma, Naresh Kumar, Sankaranarayanan Dharmarajan, Kirandeep Kaur, Anita Chugh
  • Publication number: 20080267905
    Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of a selective cytokine inhibitory drug alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of a selective cytokine inhibitory drug. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
    Type: Application
    Filed: May 5, 2004
    Publication date: October 30, 2008
    Applicant: CELGENE CORPORATION
    Inventor: Jerome B. Zeldis
  • Publication number: 20080255149
    Abstract: The invention relates to the use of carboxyamine compounds and salts thereof in the treatment of HDAC dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases.
    Type: Application
    Filed: September 25, 2006
    Publication date: October 16, 2008
    Inventors: Markus Rolf Dobler, Jonathan E. Grob, Arup Patnaik, Branko Radetich, Micheal Shultz, Yanyi Zhu
  • Publication number: 20080234358
    Abstract: A compound of formula (I) wherein R1 and R3 are the same or different and represent ?O, hydrogen, C1-6alkyl, C1-6dialkyl, ?CHC1-C5alkyl, ?S, or a 5- or 6-membered aryl; R4 to R9 are the same or different and represent hydrogen, C1-6alkoxy, OCF3, OCH2CF3, O-cyclopropyl, OCH2-cyclopropyl, C1-C6alkyl, S-alkyl, NR210 where R10 is hydrogen or C1-6alkyl, halogen, NO2, OH, CH2OC1-C6alkyl, CH2OH, or CF3; Q1 is hydrogen, C1-6alkyl, C1-6dialkyl, C1-6alkoxy, NHAc, NR210 where R10 is hydrogen or C1-6alkyl, difluoro, fluoro, ?O, or OH; Q2, Q3, Q4 and Q5 are the same or different and represent hydrogen, C1-6alkoxy, OCF3, OCH2CF3, O-cyclopropyl, OCH2-cyclopropyl, C1-C6alkyl, S-alkyl, NR210 where R10 is hydrogen or C1-6alkyl, halogen, NO2, OH, CH2OC1-C6alkyl, CH2OH, or a 5- or 6-membered aryl; with the proviso that the compounds [4-(1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]-2-propionic acid, sodium salt and [4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetic acid are excluded; and pharmac
    Type: Application
    Filed: April 30, 2008
    Publication date: September 25, 2008
    Inventors: Miles Stuart Congreve, Gerard Martin, Paul Giblin, Andrew McMurtrie Mason, Neil Derek Miller, Susan Roomans, Ann Louise Walker
  • Patent number: 7427638
    Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Grant
    Filed: April 13, 2005
    Date of Patent: September 23, 2008
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Publication number: 20080221196
    Abstract: Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with an ?-(3,4-disubstituted phenyl)alkyl group and in the 4- and/or 5-position with a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF? and phosphodiesterase. A typical embodiment is 2-[1-(3-ethoxy-4-methoxyphenyl)2-methylsulfonylethyl]4,5-diaminoisoindoline-1,3-dione.
    Type: Application
    Filed: May 12, 2008
    Publication date: September 11, 2008
    Inventors: Hon-Wah Man, George W. Muller
  • Publication number: 20080213213
    Abstract: Methods of treating, preventing and/or managing a myelodysplastic syndrome are disclosed. Specific methods encompass the administration of a selective cytokine inhibitory drug, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active ingredient, and/or blood or cells for transplantation therapy. Specific second active ingredients are capable of affecting or improving blood cell production. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
    Type: Application
    Filed: April 14, 2004
    Publication date: September 4, 2008
    Inventor: Jerome B. Zeldis
  • Publication number: 20080207689
    Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Application
    Filed: July 3, 2007
    Publication date: August 28, 2008
    Inventors: Alan Daniel Brown, Mark Edward Bunnage, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Paul Alan Glossop, Kim James, David Anthony Price
  • Patent number: 7417063
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4, X5, R4, and W are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: April 11, 2005
    Date of Patent: August 26, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joanne M. Smallheer, James R. Corte
  • Publication number: 20080199538
    Abstract: A compound that contains herbal supplements to increase the frequency and lucidity of a person's erotic or sexual dreams. The compound can be used by anyone wishing to enhance their lucid erotic dreams, or may also be taken by people suffering from jet lag or insomnia. Modes of delivery are by capsule, tablet, soft gel, transdermal patch, liquid, and gum.
    Type: Application
    Filed: January 10, 2006
    Publication date: August 21, 2008
    Inventor: Yronne Filopelrick
  • Publication number: 20080200531
    Abstract: The invention provides new methods for inhibiting the CDKI pathway and specifically inhibiting tumor cell growth. The invention further provides new and specific inhibitors of tumor cell growth, as well as means for discovery of additional such inhibitors. The present inventors have surprisingly discovered that Cyclin-Dependent Kinase 3 (CDK3) is specifically required for tumor cell growth, in contrast to other members of the CDK family.
    Type: Application
    Filed: May 15, 2007
    Publication date: August 21, 2008
    Inventors: Bey-Dih Chang, Igor B. Roninson, Donald Porter
  • Publication number: 20080194565
    Abstract: The present invention relates to C ompounds having the structure of Formula I: wherein n is an integer from 1 to 5; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, alkoxy, aryloxy, alkenyloxy or alkynyloxy; R2 is alkenyl, allcynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, NR4R5, —NHC(?Y)R4, —NHC(?Y)NR5Rx, —NHC(?O)OR4, —NHSO2R4, C(?Y)NR4R5, C(?O)OR6 [wherein Y is oxygen or sulphur], OR5, —O(C?O)NR4R5, O-acyl, S(O)mR4, —SO2N(R4)2, cyano, amidino or guanidino [wherein R4 is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl and m is an integer 0-2; R5 is hydrogen or R4; Rx is R4 or —SO2N(R4)2 and R6 is hydrogen, alkyl, cycloalkyl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl]; R3 is hydrogen, fluorine, alkyl, cycloalkylalkyl or aralkyl; A is OH, OR4, —OC(?O)NR4R5, O-acyl, NH2, NR4R5, —NHC(?Y)R4, —NHC(?Y)NR5Rx, —NHC(?O)OR4, —NHSO2R4, and to processes for
    Type: Application
    Filed: February 21, 2006
    Publication date: August 14, 2008
    Inventors: Venkata P. Palle, Viswajanani Jitendra Sattigeri, Manoj Kumar Khera, Sreedhara Rao Voleti, Abhijit Ray, Sunanda G. Dastidar
  • Patent number: 7405237
    Abstract: Novel isoindoline compounds are disclosed. Methods of treating, preventing and/or managing cancer, diseases and disorders associated with, or characterized by, undesired angiogenesis, and diseases and disorders mediated by PDE 4, using the compounds are also disclosed.
    Type: Grant
    Filed: July 28, 2004
    Date of Patent: July 29, 2008
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man
  • Publication number: 20080176920
    Abstract: The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.
    Type: Application
    Filed: February 14, 2007
    Publication date: July 24, 2008
    Inventors: Richard Ambron, Ying-Ju Sung, Jeremy Greenwood, Leah Frye, Shi-Xian Deng, Yuli Xie, Donald W. Landry
  • Publication number: 20080176868
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6?R7?); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocylcyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7? are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.
    Type: Application
    Filed: June 12, 2006
    Publication date: July 24, 2008
    Inventors: Andrew Stamford, Guoqing Li, William Greenlee, Zhaoning Zhu, Brian McKittrick, Robert Mazzola, Ying Huang, Tao Guo, Thuy X.H. Le, Gang Qian, Yuefei Shao
  • Publication number: 20080171781
    Abstract: Agents which contains a serotonin derivative as an active ingredient are effective for improving hemodynamics and for preventing or improving deterioration of hemodynamics associated with aging and progression of cardiovascular diseases.
    Type: Application
    Filed: March 14, 2008
    Publication date: July 17, 2008
    Applicant: AJINOMOTO CO., INC.
    Inventors: Shin-ichiro Katsuda, Akihiro Hazama, Naoto Koyama, Katsuya Suzuki
  • Publication number: 20080171771
    Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
    Type: Application
    Filed: June 13, 2007
    Publication date: July 17, 2008
    Applicants: AstraZeneca AB, Astex Therapeutics Ltd
    Inventors: James Arnold, Phil Edwards, Mark Sylvester, Stefan Berg, Jorg Holenz, Annika Kers, Karin Kolmodin, Laszlo Rakos, Liselotte Ohberg, Rotticci Didier, Gianni Chessari, Miles Congreve, Christopher Murray, Sahil Patel
  • Publication number: 20080149097
    Abstract: The present invention relates to multifunctional ?-agonist compounds comprising a reactive oxygen species scavenger group and a nitric oxide donor, and to methods of treating chronic obstructive airway diseases, such as asthma and chronic bronchitis.
    Type: Application
    Filed: March 10, 2008
    Publication date: June 26, 2008
    Applicant: Yissum Research Development Company of Hebrew University of Jerusalem
    Inventor: Abdullah Ibrahim Haj-Yehia
  • Publication number: 20080153758
    Abstract: The invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention more specifically relates to new uses of compounds that inhibit the prenylation of proteins, in particular the geranylgeranyl and/or farnesyl modifications of proteins, for treating neurodegeneration involving oxidative stress and, more particularly, Parkinson's disease. The invention also relates to corresponding methods of treatment, and can be used in human subjects for preventive or curative treatment, either alone is or in combination with other active agents or treatments.
    Type: Application
    Filed: November 14, 2005
    Publication date: June 26, 2008
    Inventors: Fabien Schweighoffer, Laurent Desire
  • Patent number: 7390821
    Abstract: The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associated with or resulting from angiogenesis, particularly pathological angiogenesis. The invention further provides methods of treating a condition associated with or resulting from angiogenesis.
    Type: Grant
    Filed: March 1, 2006
    Date of Patent: June 24, 2008
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: John Cooke, Christopher Heeschen, Michael Weis
  • Publication number: 20080145336
    Abstract: Novel isoindoline compounds are disclosed. Methods of treating, preventing and/or managing cancer, diseases and disorders associated with, or characterized by, undesired angiogenesis, and diseases and disorders mediated by PDE 4, using the compounds are also disclosed.
    Type: Application
    Filed: February 15, 2008
    Publication date: June 19, 2008
    Inventors: George W. Muller, Hon-Wah Man
  • Publication number: 20080138295
    Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of a selective cytokine inhibitory drug alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of a selective cytokine inhibitory drug. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
    Type: Application
    Filed: February 11, 2008
    Publication date: June 12, 2008
    Inventor: Jerome B. Zeldis
  • Patent number: 7378438
    Abstract: The present invention relates to multifunctional ?-agonist compounds comprising a reactive oxygen species scavenger group and a nitric oxide donor, and their use for the treatment of respiratory diseases involving airway obstruction, such as asthma and chronic bronchitis. The invention further relates to methods and devices for administering the compounds.
    Type: Grant
    Filed: April 15, 2003
    Date of Patent: May 27, 2008
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventor: Abdullah Ibrahim Haj-Yehia
  • Patent number: 7354948
    Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of a selective cytokine inhibitory drug alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of a selective cytokine inhibitory drug. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
    Type: Grant
    Filed: November 6, 2003
    Date of Patent: April 8, 2008
    Assignee: Celgene Corporation
    Inventor: Jerome B. Zeldis