Plural Chalcogens Bonded Directly To Ring Carbons Of The Five-membered Hetero Ring (e.g., Phthalimide, Etc.) Patents (Class 514/417)
  • Publication number: 20100160405
    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: Application
    Filed: December 3, 2009
    Publication date: June 24, 2010
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Publication number: 20100152271
    Abstract: A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and ORa; R2 is selected from H, OH, and (C?O)(C1-7)alkyl; Ra is (C1-7)alkyl or (C?O)(C1-7)alkyl; or a derivative of the compound selected from N-oxide derivatives, prodrug derivatives, protected derivatives, isomers, and mixtures of isomers of the compound; or a pharmaceutically acceptable salt or solvate of the compound or the derivative. Compounds of formula I and II and pharmaceuticals compositions thereof are also presented.
    Type: Application
    Filed: July 6, 2007
    Publication date: June 17, 2010
    Applicant: UNIVERSIT OF MEDICINE AND DENISTRY OF NEW JERSEY
    Inventors: William J. Welsh, Nina Ching Y. Wang, Ni Ai
  • Patent number: 7674817
    Abstract: The antimicrobial acid-catalyzed coating composition of the invention is an acid-catalyzed coating composition formulated with at least one antimicrobial agent to provide antimicrobial activity to the coating composition and an article coated therewith.
    Type: Grant
    Filed: May 12, 2005
    Date of Patent: March 9, 2010
    Assignee: Akzo Nobel Coatings International B.V.
    Inventor: James H. Bray, III
  • Patent number: 7662847
    Abstract: The invention encompasses novel N-alkyl-hydroxamic acid-isoindolyl compounds, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions for treatment or prevention of various diseases and disorders, for example, diseases associated with PDE4.
    Type: Grant
    Filed: May 9, 2005
    Date of Patent: February 16, 2010
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, George W. Muller
  • Publication number: 20100035958
    Abstract: The invention relates to novel compounds containing a carboxylic acid head group. The invention further provides compositions containing the novel compounds, a particulate solid and an organic medium or water.
    Type: Application
    Filed: September 7, 2007
    Publication date: February 11, 2010
    Applicant: LUBRIZOL LIMITED
    Inventor: Dean Thetford
  • Patent number: 7659302
    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: February 8, 2008
    Date of Patent: February 9, 2010
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Patent number: 7659303
    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 4, 2008
    Date of Patent: February 9, 2010
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Publication number: 20100016387
    Abstract: Method of preventing or treating myocardial ischemia by inhibiting DGAT1 enzyme with a DGAT1 inhibitor compound.
    Type: Application
    Filed: December 10, 2007
    Publication date: January 21, 2010
    Inventors: Avirup Bose, Thomas Edward Hughes
  • Patent number: 7645781
    Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.
    Type: Grant
    Filed: September 21, 2006
    Date of Patent: January 12, 2010
    Assignee: Pfizer Inc
    Inventors: Richard C. Thomas, Toni-Jo Poel, Michael R. Barbachyn, Mikhail F. Gordeev, Gary W. Luehr, Adam Renslo, Upinder Singh, Vara Prasad Venkata Negandra Josyula
  • Publication number: 20090291970
    Abstract: The invention provides compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
    Type: Application
    Filed: July 27, 2009
    Publication date: November 26, 2009
    Inventors: James P. Beck, Matthew Drowns, Martha A. Warpehoski
  • Publication number: 20090291991
    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: August 4, 2009
    Publication date: November 26, 2009
    Inventors: George W. MULLER, Hon-Wah Man
  • Publication number: 20090275556
    Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, X, Z, R2, X1, Ar, n, R3 and R4 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR8 and accordingly are useful for the treatment of a variety of inflammatory and allergic disorders.
    Type: Application
    Filed: August 27, 2008
    Publication date: November 5, 2009
    Inventors: Mingshi Dai, Bing Guan, Roert A. Bennett, Douglas F. Burdi, Shomir Ghosh, Gang Li, Charles Minor, Tracy J. Jenkins
  • Publication number: 20090269408
    Abstract: Liquid formulations of imidoalkanepercarboxylic acids, in the form of aqueous dispersions comprising, in percentages by weight relative to the total weight of the composition: A) from ?7% to 40% and preferably from 10% to 20% of imidoalka-nepercarhoxylic acids having the general formula (I), the said imidoalkanepercarboxylic acids being in the ? form and having a dissolution time, determined via the test of the rate of dissolution at a temperature of 40° C. or 18° C., of not more than 5 minutes when determined at 40° C. or 15 minutes when determined at 18° C., for an amount of dissolved acid equal to 99% of the theoretical amount; B) from 0.001% to 0.9% of a nonionic surfactant; the said dispersions having a viscosity of not more than 2000 mPa·sec at 25° C. by applying a shear rate of 20 s?1; in which the dissolution time of the component A), determined via the test of the rate of dissolution at a temperature of 40° C. or 18° C., is not more than 5 minutes when determined at 40° C.
    Type: Application
    Filed: December 23, 2004
    Publication date: October 29, 2009
    Applicant: SOLVAY SOLEXIS S.P.A.
    Inventors: Ugo Piero Bianchi, Roberto Garaffa
  • Publication number: 20090215814
    Abstract: The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75NTR common neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve growth factor to p75NTR comprises, particularly when bound to nerve growth factor, at least two of the following: (1) a first electronegative atom or functional group positioned to interact with Lys34 of nerve growth factor; (2) a second electronegative atom or functional group positioned to interact with Lys95 of nerve growth factor; (3) a third electronegative atom or functional group positioned to interact with Lys88 of nerve growth factor; (4) a fourth electronegative atom or functional group positioned to interact with Lys32 of nerve growth factor; and (5) a hydrophobic moiety which interacts with the hydrophobic region formed by Ile31, Phe101 and Phe86 of nerve growth factor.
    Type: Application
    Filed: April 28, 2009
    Publication date: August 27, 2009
    Inventors: Gregory M. Ross, Igor L. Shamovsky, Sandra Marone, Donald F. Weaver, Richard J. Riopelle
  • 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
  • Patent number: 7560459
    Abstract: The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.
    Type: Grant
    Filed: November 2, 2005
    Date of Patent: July 14, 2009
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Ahmed Abdel-Magid, Cynthia Maryanoff, Steven Mehrman, Allen B. Reitz, Bruce Maryanoff
  • Patent number: 7553872
    Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Grant
    Filed: February 13, 2006
    Date of Patent: June 30, 2009
    Assignee: Emisphere Technologies, Inc.
    Inventors: Donald J. Sarubbi, Evgueni Barantsevitch
  • Publication number: 20090155186
    Abstract: The present invention relates to compositions containing signal transduction modulator compounds, to methods for treating or preventing inflammation, or promoting healthy joints, using the compounds and to kits for the same.
    Type: Application
    Filed: June 13, 2006
    Publication date: June 18, 2009
    Applicant: SIGNUM BIOSCENCES, INC.
    Inventors: Jeffry B. Stock, Joel Gordon, Maxwell Stock, Gregory Stock
  • Publication number: 20090149415
    Abstract: The invention relates to compounds for modulating the glycolosis enzyme complex and the transaminase complex, to pharmaceutical compositions containing said compounds, and to the uses of said compounds for the production of pharmaceutical compositions for treating different diseases.
    Type: Application
    Filed: December 6, 2004
    Publication date: June 11, 2009
    Applicant: Schebo.Biotech AG
    Inventor: Hans Scheefers
  • 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
  • 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
  • Publication number: 20090082377
    Abstract: The present invention relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding preparation processes, pharmaceutical formulations and methods for use as inhibitors of matrix metallproteinase enzymes (MMPs).
    Type: Application
    Filed: November 7, 2008
    Publication date: March 26, 2009
    Inventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
  • Patent number: 7507759
    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: June 29, 2007
    Date of Patent: March 24, 2009
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Patent number: 7507836
    Abstract: The present invention is directed to compounds which are allosteric modulators of metabotropic glutamate receptors, including the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: March 22, 2004
    Date of Patent: March 24, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Mark E. Duggan, Craig W. Lindsley, David D. Wisnoski
  • 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: 20090069328
    Abstract: The present invention relates to ?-alkyl substituted N-acyltryptophanols of the formula I in which R1, R2, R3, R4, R5, R6, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
    Type: Application
    Filed: August 14, 2008
    Publication date: March 12, 2009
    Inventors: Lars Wortmann, Marcus Koppitz, Hans Peter Muhn, Anna Schrey, Ronald Kuehne
  • Publication number: 20090048236
    Abstract: Specific phenylalanine derivatives or pharmaceutically acceptable salts thereof have an antagonistic effect on the ?4 integrins and, therefore, are usable as therapeutic agents or preventive agents for diseases in which ?4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.
    Type: Application
    Filed: October 16, 2008
    Publication date: February 19, 2009
    Applicant: AJINOMOTO CO. INC
    Inventors: Nobuyasu SUZUKI, Toshihiko Yoshimura, Hiroyuki Izawa, Kazuyuki Sagi, Shingo Makino, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
  • Publication number: 20090036512
    Abstract: Active compound combinations comprising an oxime ether derivative of the formula (I) and captan and their use as fungicides are described.
    Type: Application
    Filed: December 4, 2006
    Publication date: February 5, 2009
    Inventors: Isolde Hauser-Hahn, Peter Dahmen, Albert Witzenberger, Ulrike Wachendorff-Neumann
  • Publication number: 20090029949
    Abstract: Disclosed are pharmacophores for developing and screening compounds having G-protein-coupled receptor antagonist activity, including LPA1, LPA2, LPA3 and S1P antagonists. These compositions have therapeutic benefit in the fields of cancer chemotherapy, cardiovascular disease prevention, and fertility protective agents during radiation and chemotherapy.
    Type: Application
    Filed: May 25, 2007
    Publication date: January 29, 2009
    Inventors: Abby L. Parrill-Baker, Gabor J. Tigyi, Donna Hope Perygin, James I. Fells
  • Publication number: 20090023714
    Abstract: The invention relates to pharmaceutical preparations which contain a combination of a thiazide diuretic and a low-dose loop diuretic and which are particularly useful for treating hypertension and heart failure. It is not only the overall natriuretic/diuretic effects which are increased due to said combination of thiazide diuretic and loop diuretic, but the undesired secondary effects regarding potassium and magnesium losses are significantly reduced as well. As a result, the desired hypocalciuric effect of the thiazide is maintained despite the presence of the loop diuretic.
    Type: Application
    Filed: August 29, 2006
    Publication date: January 22, 2009
    Inventors: Heinrich Knauf, Ernst Mutschler
  • Publication number: 20080318881
    Abstract: The present invention includes a fast-drying liquid composition comprising at least one fungicide and at least one insecticide. The present invention further includes a method for treating plant propagation materials, especially cut seeds, including tubers, against pests, a method for promoting suberization in cut seeds, a method for decreasing the drying time of a liquid pesticide on cut seeds, and a method for selectively loading a pesticide onto the skin side of a cut seed.
    Type: Application
    Filed: June 28, 2006
    Publication date: December 25, 2008
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Marlene Torrent-Parker, Kiran Shetty
  • 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
  • Publication number: 20080306134
    Abstract: Thalidomide analog compounds having a general structure are described. R1 is selected from a group comprising of hydroxy, hydrogen, and amino. Also described is a method for treating vascular abnormalities, such as neovascularization and vascular leakage. A therapeutically effective amount of a composition containing the thalidomide analog compound is administered to a patient. The composition may further include agents, such as solubilizing agents, inert fillers, diluents, excipients, or flavoring agents.
    Type: Application
    Filed: June 8, 2007
    Publication date: December 11, 2008
    Inventor: Danyang Chen
  • 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
  • Publication number: 20080280967
    Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF? and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.
    Type: Application
    Filed: January 16, 2008
    Publication date: November 13, 2008
    Inventors: Hon-Wah Man, George W. Muller, Shaei Y. Huang
  • Publication number: 20080269197
    Abstract: The invention provides compounds of formula (I): wherein A and B represent the groups —(CH2)m— and —(CH2)n— respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxy C1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR5R6, —SO2NR5R6, —(CH2)pNR5R6, —(CH2)pNR5COR6, optionally substituted aryl ring, optionally substituted heteroaryl ring or optionally substituted heterocyclyl ring; R3 represents optionally substituted aryl ring or optionally substituted heteroaryl ring; R4 represents hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, trifluoromethyl, trifluoromethoxy, halogen, —OSO2CF3, —(CH2)pC3-6cycloalkyl, —(CH2)qOC1-6alkyl or —(CH2)pOC3-6cycloalkyl; R5 and R6 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalky
    Type: Application
    Filed: June 24, 2008
    Publication date: October 30, 2008
    Inventors: Ian Thomson Forbes, Vincenzo Garzya, Andrew Derrick Gribble, Andrew Lightfoot, Andrew H. Payne, Graham Walker
  • Publication number: 20080261917
    Abstract: A compound of formula or a prodrug and/or a pharmaceutically acceptable salt thereof, wherein X is O, N or S; R1 is hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroaralkyl; R2 is hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; R3 is hydrogen, halo, hydroxy, substituted or unsubstituted alloy substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; and R4-R7, is used to represent groups R4, R5, R6 and R7 which are H, OH, alkyl, alkoxy, alkylamine, hydroxyalkyl, h
    Type: Application
    Filed: August 26, 2005
    Publication date: October 23, 2008
    Inventors: Hendrika Maria Gerarda Willems, Per Kallblad, Ian Robert Hardcastle, Robert John Griffin, Bernard Thomas Golding, John Lunec, Martin E.M. Noble, David R. Newell, Alan H. Calvert
  • Publication number: 20080261982
    Abstract: Stilbene derivatives exhibit killing and suppression of growth activity against a variety of cancer cells, and are effective at suppressing tumor growth in vivo. The stilbene derivatives may be used in the treatment of diseases characterized by cell hyperproliferation including human malignancies and non-malignant diseases such as liver cirrhosis. Stilbenes may also disrupt abnormal vessels in tumor to achieve vascular disrupting effect to suppress tumor growth. Water soluble pro-drug forms of stilbene derivatives are particularly useful in suppressing tumor growth in vivo.
    Type: Application
    Filed: April 23, 2007
    Publication date: October 23, 2008
    Inventors: Ruey-min Lee, Daniele Simoni
  • Publication number: 20080242712
    Abstract: Methods are provided for treating or prophylactically preventing metabolic disorders in humans without causing, promoting, or aggravating fluid retention, peripheral edema, pulmonary edema, or congestive heart failure, by administration of a therapeutically effective amount of a compound sufficient to partially or fully activate peroxisome proliferator activated receptors (PPARs) and partially or fully inhibit, antagonize or block the activity of angiotensin II type 1 receptors. Metabolic disorders that can be treated or prevented include but are not limited to type 2 diabetes, the metabolic syndrome; prediabetes, and other insulin resistance syndromes.
    Type: Application
    Filed: June 3, 2008
    Publication date: October 2, 2008
    Applicant: Bethesda Pharmaceuticals
    Inventor: Harrihar A. Pershadsingh
  • Publication number: 20080242719
    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: Application
    Filed: April 4, 2008
    Publication date: October 2, 2008
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Publication number: 20080234359
    Abstract: Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use 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: Application
    Filed: March 27, 2008
    Publication date: September 25, 2008
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge, Jean Xu
  • 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: 20080207730
    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: Application
    Filed: February 8, 2008
    Publication date: August 28, 2008
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • 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
  • Patent number: 7396852
    Abstract: A compound including at least one type of an optionally substituted indolocarbazole moiety and at least one divalent linkage.
    Type: Grant
    Filed: November 16, 2005
    Date of Patent: July 8, 2008
    Assignee: Xerox Corporation
    Inventors: Yuning Li, Beng S. Ong, Yiliang Wu, Ping Liu
  • Publication number: 20080153816
    Abstract: Indole compounds corresponding to the formula (I): as defined in the claims, pharmaceutically acceptable addition salts of such compounds, pharmaceutical compositions containing such compounds, the process for their preparation, and their use as pharmacologically active substances, especially in the treatment of hypertriglyceridemia, hyperlipidemia, hypercholesterolemia, diabetes, endothelial dysfunction, cardiovascular disease, inflammatory disease and neurodegeneration.
    Type: Application
    Filed: February 28, 2008
    Publication date: June 26, 2008
    Applicant: Laboratoires Fournier S.A.
    Inventors: Jean BINET, Benaissa Boubia, Pierre Dodey, Christiane Legendre, Martine Barth, Olivia Poupardin-Olivier
  • Publication number: 20080153823
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: December 13, 2007
    Publication date: June 26, 2008
    Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert Sibley
  • Patent number: 7358272
    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: June 28, 2005
    Date of Patent: April 15, 2008
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • 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
  • Patent number: RE40360
    Abstract: The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis. Importantly, these compounds can be administered orally.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: June 3, 2008
    Assignee: The Children's Medical Center Corporation
    Inventor: Robert J. D'Amato