The Ring Nitrogen Is Bonded Directly To Nonshared Ring Carbons Of The Five-membered Hetero Ring (e.g., Isoindole, Etc.) Patents (Class 514/416)
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Patent number: 7569597Abstract: 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: GrantFiled: February 15, 2008Date of Patent: August 4, 2009Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man
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Publication number: 20090176858Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: December 19, 2008Publication date: July 9, 2009Applicant: Avila Therapeutics, Inc.Inventors: Deqiang Niu, Russell C. Petter, Juswinder Singh, Arthur F. Kluge, Lixin Qiao
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Patent number: 7557114Abstract: 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: GrantFiled: January 31, 2006Date of Patent: July 7, 2009Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
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Publication number: 20090170842Abstract: 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: ApplicationFiled: November 13, 2008Publication date: July 2, 2009Applicant: University of KansasInventors: Roy A. Jensen, Lisa M. Harlan-Williams, Frank J. Schoenen, Jeffrey Aube, Gerald H. Lushington
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Publication number: 20090170835Abstract: Provided is a novel isoindoline compound of the formula (I): The compound is useful for anesthesia by inducing sedation in a mammal.Type: ApplicationFiled: December 30, 2008Publication date: July 2, 2009Inventors: Kouhei Toyooka, Norimasa Kanamitsu, Masakazu Yoshimura, Haruo Kuriyama, Takashi Tamura
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Publication number: 20090149505Abstract: 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: ApplicationFiled: February 6, 2007Publication date: June 11, 2009Applicant: AstraZeneca ABInventors: James R. Empfield, James J. Folmer, James R. Arnold, Joshua Clayton, Abdelmalik Slassi, Methvin Isaac, Ian Egle, Fupeng Ma
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Publication number: 20090143382Abstract: 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: ApplicationFiled: January 30, 2009Publication date: June 4, 2009Inventors: George W. Muller, Hon-Wah Man, Weihong Zhang
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Patent number: 7531569Abstract: 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: GrantFiled: December 1, 2004Date of Patent: May 12, 2009Assignee: sanofi-aventis Deutschland GmbHInventors: Gerrit Schubert, Joerg Rieke-Zapp, Johannes Keil, Heinz-Werner Kleemann, Reda Hanna, Bao-Guo Huang, Xiao-Dong Wu, Yves Gouraud
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Publication number: 20090118268Abstract: 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: ApplicationFiled: October 10, 2008Publication date: May 7, 2009Inventors: 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
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Patent number: 7528165Abstract: 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: GrantFiled: August 1, 2005Date of Patent: May 5, 2009Assignee: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Jing-Ping Liou, Jang-Yang Chang, Chun-Wei Chang
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Publication number: 20090099186Abstract: 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: ApplicationFiled: October 10, 2006Publication date: April 16, 2009Inventors: Leonid Beigelman, Steven W. Andrews, Kevin R. Condroski, Indrani Gunawaradana, Julia Haas
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Publication number: 20090082368Abstract: 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: ApplicationFiled: September 24, 2008Publication date: March 26, 2009Applicant: PainCeptor Pharma CorporationInventors: Rahul VOHRA, Gilles Dube, Zhonghong Gan, Nachhattarpal Gill, Xilin Cui
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Publication number: 20090075978Abstract: 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: ApplicationFiled: June 26, 2008Publication date: March 19, 2009Applicant: Grunenthal GmbHInventors: Michael HAURAND, Klaus SCHIENE, Sven KUHNERT, Melanie REICH, Saskia ZEMOLKA
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Patent number: 7504427Abstract: 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: GrantFiled: November 16, 2006Date of Patent: March 17, 2009Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man, Weihong Zhang
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Publication number: 20090062284Abstract: 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: ApplicationFiled: August 27, 2008Publication date: March 5, 2009Applicant: 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
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Publication number: 20090054462Abstract: 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: ApplicationFiled: June 23, 2006Publication date: February 26, 2009Inventors: Jinlong Jiang, Robert J. DeVita, Sanjeev Kumar, Sander G. Mills, Richard A. Tschirret-Guth
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Patent number: 7485643Abstract: 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: GrantFiled: November 18, 2004Date of Patent: February 3, 2009Assignee: Array BioPharma Inc.Inventors: Eli Wallace, Joseph P. Lyssikatos, Hong Woon Yang
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Publication number: 20090030063Abstract: 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: ApplicationFiled: April 18, 2006Publication date: January 29, 2009Inventors: Yuji Kiyono, Yoshio Okubo, Katsumi Hontani, Imao Mikoshiba, Kazuma Ojima
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Publication number: 20090031435Abstract: 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: ApplicationFiled: November 29, 2007Publication date: January 29, 2009Inventors: Brent R. Stockwell, David E. Root
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Publication number: 20090030064Abstract: 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: ApplicationFiled: June 9, 2006Publication date: January 29, 2009Applicant: Takeda Pharmaceutical Company LimitedInventors: Yoshihiro Uchiyama, Yoshinori Nakano
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Patent number: 7482336Abstract: 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: GrantFiled: June 17, 2005Date of Patent: January 27, 2009Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Danqing Feng, Ying-Duo Gao, Suresh Singh, Ann E. Weber
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Patent number: 7482472Abstract: 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: GrantFiled: March 12, 2007Date of Patent: January 27, 2009Assignee: Bayer Healthcare AGInventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Rohrig, Elisabeth Perzborn, Karl-Heinz Schlemmer
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Publication number: 20090017003Abstract: 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: ApplicationFiled: March 1, 2007Publication date: January 15, 2009Applicant: SULFIDRIS S.R.L.Inventors: Piero Del Soldato, Giancarlo Santus, Anna Sparatore
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Publication number: 20090010886Abstract: 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: ApplicationFiled: May 5, 2004Publication date: January 8, 2009Applicant: CELGENE CORPORATIONInventor: Jerome B. Zeldis
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Patent number: 7468387Abstract: 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: GrantFiled: July 8, 2003Date of Patent: December 23, 2008Assignee: Solvay Solexis S.p.A.Inventors: Ugo Piero Bianchi, Roberto Garaffa
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Patent number: 7456183Abstract: 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: GrantFiled: April 8, 2002Date of Patent: November 25, 2008Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Daniel Chu, Rustum Boyce, David Duhl, Bryan Chang
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Patent number: 7446123Abstract: 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: GrantFiled: January 7, 2004Date of Patent: November 4, 2008Assignee: Ranbaxy Laboratories LimitedInventors: Mohammad Salman, Anita Mehta, Pakala Kumara Savithru Sarma, Naresh Kumar, Sankaranarayanan Dharmarajan, Kirandeep Kaur, Anita Chugh
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Publication number: 20080267905Abstract: 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: ApplicationFiled: May 5, 2004Publication date: October 30, 2008Applicant: CELGENE CORPORATIONInventor: Jerome B. Zeldis
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Publication number: 20080255149Abstract: 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: ApplicationFiled: September 25, 2006Publication date: October 16, 2008Inventors: Markus Rolf Dobler, Jonathan E. Grob, Arup Patnaik, Branko Radetich, Micheal Shultz, Yanyi Zhu
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Publication number: 20080234358Abstract: 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 pharmacType: ApplicationFiled: April 30, 2008Publication date: September 25, 2008Inventors: Miles Stuart Congreve, Gerard Martin, Paul Giblin, Andrew McMurtrie Mason, Neil Derek Miller, Susan Roomans, Ann Louise Walker
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Patent number: 7427638Abstract: 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: GrantFiled: April 13, 2005Date of Patent: September 23, 2008Assignee: Celgene CorporationInventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
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Publication number: 20080221196Abstract: 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: ApplicationFiled: May 12, 2008Publication date: September 11, 2008Inventors: Hon-Wah Man, George W. Muller
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Publication number: 20080213213Abstract: 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: ApplicationFiled: April 14, 2004Publication date: September 4, 2008Inventor: Jerome B. Zeldis
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Publication number: 20080207689Abstract: 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: ApplicationFiled: July 3, 2007Publication date: August 28, 2008Inventors: Alan Daniel Brown, Mark Edward Bunnage, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Paul Alan Glossop, Kim James, David Anthony Price
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Patent number: 7417063Abstract: 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: GrantFiled: April 11, 2005Date of Patent: August 26, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Joanne M. Smallheer, James R. Corte
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Publication number: 20080199538Abstract: 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: ApplicationFiled: January 10, 2006Publication date: August 21, 2008Inventor: Yronne Filopelrick
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Publication number: 20080200531Abstract: 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: ApplicationFiled: May 15, 2007Publication date: August 21, 2008Inventors: Bey-Dih Chang, Igor B. Roninson, Donald Porter
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Publication number: 20080194565Abstract: 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 forType: ApplicationFiled: February 21, 2006Publication date: August 14, 2008Inventors: Venkata P. Palle, Viswajanani Jitendra Sattigeri, Manoj Kumar Khera, Sreedhara Rao Voleti, Abhijit Ray, Sunanda G. Dastidar
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Patent number: 7405237Abstract: 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: GrantFiled: July 28, 2004Date of Patent: July 29, 2008Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man
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Publication number: 20080176920Abstract: 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: ApplicationFiled: February 14, 2007Publication date: July 24, 2008Inventors: Richard Ambron, Ying-Ju Sung, Jeremy Greenwood, Leah Frye, Shi-Xian Deng, Yuli Xie, Donald W. Landry
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Publication number: 20080176868Abstract: 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: ApplicationFiled: June 12, 2006Publication date: July 24, 2008Inventors: Andrew Stamford, Guoqing Li, William Greenlee, Zhaoning Zhu, Brian McKittrick, Robert Mazzola, Ying Huang, Tao Guo, Thuy X.H. Le, Gang Qian, Yuefei Shao
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Publication number: 20080171781Abstract: 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: ApplicationFiled: March 14, 2008Publication date: July 17, 2008Applicant: AJINOMOTO CO., INC.Inventors: Shin-ichiro Katsuda, Akihiro Hazama, Naoto Koyama, Katsuya Suzuki
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Publication number: 20080171771Abstract: 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: ApplicationFiled: June 13, 2007Publication date: July 17, 2008Applicants: AstraZeneca AB, Astex Therapeutics LtdInventors: 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
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Publication number: 20080149097Abstract: 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: ApplicationFiled: March 10, 2008Publication date: June 26, 2008Applicant: Yissum Research Development Company of Hebrew University of JerusalemInventor: Abdullah Ibrahim Haj-Yehia
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Publication number: 20080153758Abstract: 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: ApplicationFiled: November 14, 2005Publication date: June 26, 2008Inventors: Fabien Schweighoffer, Laurent Desire
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Patent number: 7390821Abstract: 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: GrantFiled: March 1, 2006Date of Patent: June 24, 2008Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: John Cooke, Christopher Heeschen, Michael Weis
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Publication number: 20080145336Abstract: 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: ApplicationFiled: February 15, 2008Publication date: June 19, 2008Inventors: George W. Muller, Hon-Wah Man
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Publication number: 20080138295Abstract: 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: ApplicationFiled: February 11, 2008Publication date: June 12, 2008Inventor: Jerome B. Zeldis
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Patent number: 7378438Abstract: 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: GrantFiled: April 15, 2003Date of Patent: May 27, 2008Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventor: Abdullah Ibrahim Haj-Yehia
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Patent number: 7354948Abstract: 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: GrantFiled: November 6, 2003Date of Patent: April 8, 2008Assignee: Celgene CorporationInventor: Jerome B. Zeldis