Chalcogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/445)
  • Publication number: 20110288052
    Abstract: The class compounds of the present invention may be represented by Formula (I), wherein X may be O, S, or N. R1 and R2 are independently either H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl. R3 and R4 are independently either H, an aryl group, a heteroaryl group, and a heterocyclic ring group having 4 to 6 carbon atoms, wherein the aryl, heteroaryl, and heterocyclic moieties are optionally substituted with one or more of a first substitution group defined herein. In a further embodiment, R3 and R4 along with the atoms and bonds to which they are attached, form an optionally substituted 5-7 membered ring having at least one nitrogen atom within the ring structure.
    Type: Application
    Filed: June 2, 2009
    Publication date: November 24, 2011
    Inventors: Craig A. Townsend, Kandasamy Subburaj, Jill Marie McFadden
  • Publication number: 20110268822
    Abstract: Compounds having the general formula (I): wherein X is S, Se or NH, and stereoisomers thereof, and de-O-sulfonated analogues of all of the foregoing, but excluding naturally occurring kotalanol and de-O-sulfonated kotalanol, and methods for synthesizing same. The compounds are useful as glycosidase inhibitors, and may be used in the treatment of diabetes. The synthetic compounds may also be used as standards in the calibration or grading of natural or herbal remedies produced from natural sources of glycosidase inhibitors such as kotalanol.
    Type: Application
    Filed: March 25, 2009
    Publication date: November 3, 2011
    Applicant: SIMON FRASER UNIVERSITY
    Inventors: Brian Mario Pinto, Jayakanthan Kumarasamy, Ravindranath Nasi, Sankar Mohan
  • Publication number: 20110263691
    Abstract: Non-human animals which overexpress PPARd or which express transgenic PPARd are useful as models for inflammatory skin conditions such as psoriasis. Test substances can be screened to assess their suitability for the treatment of inflammatory skin conditions such as psoriasis. Methyl 3-({[2-(methoxy)-4-phenyl]amino}sulfonyl)-2-thiophenecarboxylate can be administered topically for the prevention or treatment of psoriasis.
    Type: Application
    Filed: July 31, 2009
    Publication date: October 27, 2011
    Inventors: Colin Palmer, John Foerster, Nainamalai Sitheswaran
  • Patent number: 8039496
    Abstract: Disclosed herein is a compound of the formula. Therapeutic methods, compositions, and medicaments for the treatment of glaucoma or ocular hypertension related thereto are also disclosed.
    Type: Grant
    Filed: January 22, 2008
    Date of Patent: October 18, 2011
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20110250254
    Abstract: An agent comprising the compound according to general formula (I) wherein R1, R2, R3 and R4 are each independently H or a substituent, and wherein at least one of R1, R3 and R4 is halogen, cyano, cyanate, thiocyanate or C1-C6 haloalkyl.
    Type: Application
    Filed: October 9, 2009
    Publication date: October 13, 2011
    Inventors: Anne Aamdal Scheie, Tore Benneche, Jessica Lonn-Stensrud, Jan Skramstad
  • Patent number: 8030327
    Abstract: The present invention relates to a compound represented by the Formula [I]: Wherein: the A ring is a 5-membered aromatic heterocyclic group containing at least one hetero atom selected from a nitrogen atom, and the like; A1 and A2, are each a nitrogen atom, and the like; X2, X3, X4, and X5 are all carbon atoms, or alternatively any one of X2, X3, X4, and X5 is a nitrogen atom and the rest are all carbon atoms; R1 is a hydrogen atom, or the like; R2, R3, R4, and R5, are each a hydrogen atom, or the like; R6 and R6?, are each a hydrogen atom, and the like; R7 is an aryl group and the like; and R8 is an amino group or a hydroxy group, or a pharmaceutically acceptable salt or ester thereof.
    Type: Grant
    Filed: November 7, 2005
    Date of Patent: October 4, 2011
    Assignee: MDS K.K.
    Inventors: Yoshiyuki Sato, Hideki Kurihara, Kaori Kamijo, Yu Onozaki, Toshiaki Tsujino, Tetsuya Sugimoto, Akiko Watanabe, Morihiro Mitsuya, Hideya Komatani
  • Publication number: 20110237525
    Abstract: A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of lipid soluble, hydrophobic active compounds having a chemical structure: wherein R1 is an aromatic backbone and R2 is a sulfur containing ligand. Through formation of disulfide linkages other moieties can be attached to R2 converting the hydrophobic base into a water soluble entity, for ease of delivery, which can be reconverted back to the original compound by biochemical reduction in the blood stream.
    Type: Application
    Filed: June 18, 2010
    Publication date: September 29, 2011
    Inventors: Boyd E. Haley, Niladri Narayan Gupta
  • Publication number: 20110201609
    Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds.
    Type: Application
    Filed: June 30, 2009
    Publication date: August 18, 2011
    Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South Florida
    Inventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
  • Patent number: 7985769
    Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.
    Type: Grant
    Filed: January 26, 2005
    Date of Patent: July 26, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constanin Yannopoulos
  • Publication number: 20110172298
    Abstract: Indication of use of erdosteine as antidote in a large number of intoxications, especially in heavy metals like lead or mercury, and paracetamol. Indication of use of erdosteine as prophylaxis for intoxications. Erdosteine can be administered per os or intravenous, using a solution obtained with sodium hydrogen carbonate and bidistilled water.
    Type: Application
    Filed: August 13, 2009
    Publication date: July 14, 2011
    Inventors: Marco Peretto, Cristina Sarbulescu, Victor Voicu
  • Publication number: 20110152341
    Abstract: Methods and means for the identification of meprin-? and meprin-? as novel ?-secretases and antagonists thereof for use in the treatment of amyloidosis.
    Type: Application
    Filed: December 22, 2010
    Publication date: June 23, 2011
    Applicant: PROBIODRUG AG
    Inventors: Stephan Schilling, Dagmar Schlenzig, Hans-Ulrich Demuth
  • Publication number: 20110152318
    Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.
    Type: Application
    Filed: July 2, 2009
    Publication date: June 23, 2011
    Applicant: Amorepacific Corporation
    Inventors: Byoung Young Woo, Sun-Young Kim, Yeonjoon Kim, Song Seok Shin, Jin Kwan Kim, Ki-Wha Lee, Dong Hyun Kim, Kyung Min Lim, Joo-Hyun Moh, Yeon Su Jeong, Jin Kyu Choi, Hyun Ju Koh, Jeongho Lee, Hyuk Kim, Jeong Hoon Yoon, Funan Li, Jee-Suk Kim, Young-Ger Suh
  • Publication number: 20110136827
    Abstract: The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: December 7, 2010
    Publication date: June 9, 2011
    Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • Publication number: 20110105544
    Abstract: The invention provides novel compounds of formula (I), wherein: R1 is a radical derived from one of the known ring systems; R2 is a phenyl radical optionally substituted; Xn represents a birradical selected from the group consisting of: —(CH2)1-4—, (C2-C4)-alkenyl, (C2-C4)alkynyl, —S—(CH2)1-3—#, and —(CH2)1-3—O—#; wherein the symbol # indicates the position at which Xn is attached to R1; Yn is a birradical selected from the group consisting of: —(CH2)2-4—, —S—(CH2)1-3#, and —O—(CH2)1-3—#; wherein the symbol # indicates the position at which Yn is attached to R2; and R3 is a radical selected from the group consisting of: —OR4. The compounds of formula (I) are useful in the treatment of cancer.
    Type: Application
    Filed: December 18, 2008
    Publication date: May 5, 2011
    Inventors: Juan Aymami Bofarull, Franck Camille Nicolas Chevalier, Montserrat Soler Lopez, Maria Teresa Luque Garrofe, Marc Martinell Pedemonte
  • Publication number: 20110105597
    Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;
    Type: Application
    Filed: December 28, 2007
    Publication date: May 5, 2011
    Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
  • Patent number: 7932283
    Abstract: The present invention relates to N-cyclopropyl-sulfonylamide derivatives of formula (I) wherein the substituents are cyclic groups, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions:
    Type: Grant
    Filed: April 5, 2007
    Date of Patent: April 26, 2011
    Assignee: Bayer Cropscience AG
    Inventors: Hans-Georg Schwarz, Sandra Gassmann, Karl-Heinz Kuck, Peter Dahmen, Ulrike Wachendorff-Neumann, Stéphane Carbonne, Stéphanie Gary, Christopher Steele, Alain Villier, Jean-Pierre Vors
  • Patent number: 7928037
    Abstract: The present invention relates to novel 3-biphenyl-substituted, 3-substituted 4-keto-lactams and -lactones of the formula (I) in which A, B, Q, G, W, X, Y and Z are as defined in the disclosure, to processes for their preparation, and to their use as pesticides and/or microbicides and/or herbicides.
    Type: Grant
    Filed: October 23, 2007
    Date of Patent: April 19, 2011
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Mark Wilhelm Drewes, Christoph Erdelen, Angelika Lubos-Erdelen, legal representative, Dieter Feucht, Udo Reckmann, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann
  • Publication number: 20110082148
    Abstract: The invention provides a method for treating, preventing or ameliorating a hyperproliferative disease and/or disorder such as cancer (e.g. leukemia) in a mammal comprising administering a therapeutically effective amount of one or more compounds selected from the group consisting of compounds of Formula (I), quinolones and fluoroquinolones; or a pharmaceutically acceptable salt thereof to said mammal: wherein R1 comprises a structural moiety represented by X—C(O)—CH—NH(X?O or S). The invention also provides a combination therapy method using such compounds in combination with other cancer fighting chemicals. The invention exhibits merits such as none or minimal side effect associated with chemotherapy.
    Type: Application
    Filed: October 7, 2010
    Publication date: April 7, 2011
    Inventor: Gilles Klopman
  • Publication number: 20110077290
    Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Application
    Filed: June 26, 2009
    Publication date: March 31, 2011
    Applicant: Nissan Chemical Industries Limited
    Inventors: Shingo OWADA, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
  • Publication number: 20110071199
    Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R1, R2 and n are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
    Type: Application
    Filed: March 16, 2010
    Publication date: March 24, 2011
    Inventor: John E. Starrett, JR.
  • Publication number: 20110052732
    Abstract: A mineral absorption accelerator, and an anemia improving agent, food and drink or food and drink material containing the mineral absorption accelerator are provided, the mineral absorption accelerator including: an ?-glucosidase inhibitory component.
    Type: Application
    Filed: April 3, 2009
    Publication date: March 3, 2011
    Applicant: FUJIFILM Corporation
    Inventor: Fumitaka Ueda
  • Publication number: 20110053890
    Abstract: Bacterial quorum-sensing molecule analogs having the following structures: and methods of reducing bacterial pathogenicity, comprising providing a biological system comprising pathogenic bacteria which produce natural quorum-sensing molecule; providing a synthetic bacterial quorum-sensing molecule having the above structures and introducing the synthetic quorum-sensing molecule into the biological system comprising pathogenic bacteria. Further is provided a method of targeted delivery of an antibiotic, comprising providing a synthetic quorum-sensing molecule; chemically linking the synthetic quorum-sensing molecule to an antibiotic to produce a quorum-sensing molecule-antibiotic conjugate; and introducing the conjugate into a biological system comprising pathogenic bacteria susceptible to the antibiotic.
    Type: Application
    Filed: September 1, 2009
    Publication date: March 3, 2011
    Applicant: Los Alamos National Security, LLC.
    Inventors: Rashi Iyer, Kumkum Ganguly, Louis A. Silks
  • Publication number: 20110046195
    Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.
    Type: Application
    Filed: June 24, 2010
    Publication date: February 24, 2011
    Inventors: Helen E. BLACKWELL, Christine E. McInnis
  • Publication number: 20110034513
    Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's disease and Down's syndrome are described.
    Type: Application
    Filed: October 19, 2010
    Publication date: February 10, 2011
    Applicants: Wyeth LLC, ArQule, Inc.
    Inventors: Anthony F. Kreft, Derek C. Cole, Kevin R. Woller, Joseph R. Stock, George Diamantidis, Dennis M. Kubrak, Kristina M. Kutterer, William J. Moore, David S. Casebier
  • Publication number: 20110028463
    Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.
    Type: Application
    Filed: July 2, 2008
    Publication date: February 3, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo
  • Publication number: 20110020232
    Abstract: Provided are methods for treating cancer in a patient, comprising administering to a patient in need thereof a therapeutically effective regimen, the regimen comprising administering a gamma-secretase inhibitor, wherein the regimen results in a reduction in the cancer cell population in the patient. In some embodiments of the methods, the therapeutically effective regimen stabilizes, reduces or eliminates the cancer stem cell population. Also provided are compounds of the formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, and X are as herein described.
    Type: Application
    Filed: March 25, 2010
    Publication date: January 27, 2011
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Charles Eberhart, Xing Fan, Anirban Maitra
  • Publication number: 20110002875
    Abstract: Therapeutic compounds and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is inhibited by the administration to a subject of an effective amount of a therapeutic compound comprising an anionic group and a carrier molecule, or a pharmaceutically acceptable salt thereof, such that an interaction between an amyloidogenic protein and a basement membrane constituent is inhibited. Preferred anionic groups are sulfonates and sulfates. Preferred carrier molecules include carbohydrates, polymers, peptides, peptide derivatives, aliphatic groups, alicyclic groups, heterocyclic groups, aromatic groups and combinations thereof.
    Type: Application
    Filed: June 8, 2010
    Publication date: January 6, 2011
    Applicant: Bellus Health (International) Limited
    Inventors: Robert Kisilevsky, Walter Szarek, Donald Weaver
  • Patent number: 7858658
    Abstract: Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: December 28, 2010
    Assignee: Wyeth LLC
    Inventors: Anthony Frank Kreft, Lynn Resnick, Scott Christian Mayer, George Diamantidis, Derek Cecil Cole, Boyd Lynn Harrison, Minsheng Zhang, Molly Hoke, Tingzhong Wang, Rocco John Galante
  • Publication number: 20100324093
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: August 26, 2010
    Publication date: December 23, 2010
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
  • Publication number: 20100317677
    Abstract: The invention relates to methods and compositions for treating a microbial infection. In the present invention, RNase-L activity has been shown to play an integral role in innate immunity and for defense against invading microbes. The present invention is drawn to exploiting the role of RNase-L in innate immunity for methods of treating a microbial infection. The present invention is also drawn to exploiting the role of RNase-L in innate immunity for methods of treating an immune related disease or disorder.
    Type: Application
    Filed: September 10, 2008
    Publication date: December 16, 2010
    Inventors: Bret A. Hassel, Alan S. Cross, Xiao-Ling Li, Tae Jin Kang
  • Publication number: 20100311711
    Abstract: Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases.
    Type: Application
    Filed: October 10, 2008
    Publication date: December 9, 2010
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Daniele Piomelli, Giorgio Tarzia, Marco Mor, Andrea Duranti, Andrea Tontini
  • Patent number: 7842718
    Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's disease and Down's syndrome are described.
    Type: Grant
    Filed: October 9, 2009
    Date of Patent: November 30, 2010
    Assignees: Wyeth LLC, ArQule, Inc.
    Inventors: Anthony Frank Kreft, Derek Cecil Cole, Kevin R. Woller, Joseph Raymond Stock, George Diamantidis, Dennis Michael Kubrak, Kristina Martha Kutterer, William J. Moore, David S. Casebier
  • Publication number: 20100298347
    Abstract: Substituted 2-naphthoic acids of structural formula are effective as antagonists of the biological activity of GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and conditions associated with the Metabolic Syndrome.
    Type: Application
    Filed: December 1, 2008
    Publication date: November 25, 2010
    Applicant: MERCK FROSST CANADA LTD
    Inventors: Michel Belley, Denis Deschenes, Rejean Fortin, Jean-Francois Fournier, Sebastien Gagne, Yves Gareau, Jacques Yves Gauthier, Lianhai Li, Joel Robichaud, Michel Therien, Geoffrey K. Tranmer, Zhaoyin Wang
  • Patent number: 7838550
    Abstract: Processes for preparing sulfonamide trifluoroalkyl substituted alcohol compounds are provided. Desirably, the compounds are heterocyclic sulfonamide trifluoroalkyl substituted alcohol compounds or phenyl sulfonamide trifluoroalkyl substituted alcohol compounds.
    Type: Grant
    Filed: February 15, 2007
    Date of Patent: November 23, 2010
    Assignee: Wyeth LLC
    Inventors: Anita Wai-Yin Chan, Jianxin Ren, Mousumi Ghosh, Panolil Raveendranath
  • Patent number: 7829564
    Abstract: ?-and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: December 7, 2007
    Date of Patent: November 9, 2010
    Assignee: G.D. Searle LLC
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
  • Publication number: 20100280074
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: December 3, 2009
    Publication date: November 4, 2010
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
  • Publication number: 20100273739
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: February 16, 2010
    Publication date: October 28, 2010
    Inventors: Wilhelm Amberg, Micheal Ochse, Udo Lange, Andreas King, Berthold Behl, Wilfried Hamberger, Maric Mezier, Charles W. Hutchins
  • Patent number: 7816397
    Abstract: The invention relates to compounds of general formula (1): in which R1, R2, R3, R4, R5, A, B, D and E are as defined in Claim 1, and also to the preparation process therefor and the therapeutic use thereof. These compounds can be used in the treatment of pathologies associated with hyperglycaemia.
    Type: Grant
    Filed: June 1, 2005
    Date of Patent: October 19, 2010
    Assignee: Merck Patent GmbH
    Inventors: Gérard Moinet, Gérard Botton, Micheline Kergoat
  • Publication number: 20100261675
    Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.
    Type: Application
    Filed: June 24, 2010
    Publication date: October 14, 2010
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
  • Publication number: 20100261735
    Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.
    Type: Application
    Filed: June 24, 2010
    Publication date: October 14, 2010
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
  • Publication number: 20100240708
    Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, methods for using the compounds and processes for making the compounds. More specifically, the disclosure relates to alpha-(N-benzenesulfonamido)cycloalkyl compounds that may inhibit one or both of: (i) the functioning of a ?-secretase enzyme; or (ii) the production of ?-amyloid. Such compounds may be beneficial in the treatment of Alzheimer's disease and other conditions. Representative compounds have the following formula I: wherein: A, R1, and R2 are described herein.
    Type: Application
    Filed: March 17, 2010
    Publication date: September 23, 2010
    Inventors: Dalton King, Zhaoxing Meng, Ivar M. McDonald, Richard E. Olson, John E. Macor
  • Publication number: 20100234350
    Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 14, 2009
    Publication date: September 16, 2010
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-McGuire, Hans-Michael Jantzen, David M. Sedlock
  • Patent number: 7786160
    Abstract: Combinations of certain analgesics with certain COX-II inhibitors, related pharmaceutical compositions, including advantageous galenical forms containing these combinations, and to the use thereof in methods of treatment, in particular for the treatment of pain.
    Type: Grant
    Filed: May 20, 2005
    Date of Patent: August 31, 2010
    Assignee: Gruenenthal GmbH
    Inventors: Klaus Schiene, Guenter Haase, Babette-Yvonne Koegel, Elmar Friderichs, Ulrich Jahnel
  • Patent number: 7759390
    Abstract: Compounds of formula I, wherein one of R1 and R2 is thienyl which is substituted by halogen and the other of R1 and R2 is substituted phenyl, wherein the substituents are as defined in the claims, with the proviso that the phenyl group is substituted by at least a cyano, carboxy or (C1-4)alkyloxycarbonyl group, are inhibitors of CCR9 activity and useful for therapeutic treatment.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: July 20, 2010
    Assignee: Novartis AG
    Inventors: Jose M. Carballido Herrera, Herbert Jaksche, Philipp Lehr, Gudrun Werner, Anthony Winiski
  • Patent number: 7759391
    Abstract: The present invention relates to an anti-cancer composition, which comprises a sulfur-containing compound thiacremonone as an active ingredient. The active ingredient induces the death of cancer cells by apoptosis through the action of specific inhibition of the activity of NF-?B. The composition can be effectively used in the treatment or prevention of cancer.
    Type: Grant
    Filed: August 6, 2008
    Date of Patent: July 20, 2010
    Assignee: Chungbuk National University Industry Academic Cooperation Foundation
    Inventors: Jin Tae Hong, Jung Ok Ban, Heon-Sang Jeong, Dae Joong Kim
  • Publication number: 20100173778
    Abstract: The present invention relates to novel 3-biphenyl-substituted, 3-substituted 4-ketolactams and -lactones of the formula (I) in which A, B, Q, G, W, X, Y and Z are as defined in the disclosure, to processes for their preparation, and to their use as pesticides and/or microbicides and/or herbicides.
    Type: Application
    Filed: October 23, 2007
    Publication date: July 8, 2010
    Inventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Mark Wilhelm Drewes, Christoph Erdelen, Angelika Lubos-Erdelen, Dieter Feucht, Udo Reckmann, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann
  • Publication number: 20100168218
    Abstract: A method of decreasing the food intake of a subject, comprising the administration of a compound which increases FAO, where the compound does not act in the central nervous system to decrease appetite, where the compound is not a fatty acid, or an NPY-inhibitor, or an FAS inhibitor.
    Type: Application
    Filed: July 26, 2006
    Publication date: July 1, 2010
    Inventor: Francis P. Kuhajda
  • Publication number: 20100168176
    Abstract: Compounds having the following general formula, pharmaceutical compositions comprising the compounds, and methods of treating cancer, obesity, and microbial infections using such compositions: wherein: R1=H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, cyanomethyl, —OCH3, OC(O)CH3 or OC(O)CF3 R2=-OCH2C(O)NHNH—R5, where R5 is (a) phenyl, optionally substituted with one or more of halogen, C1-C8 alkyl, optionally substituted with halogen, —OH, —OR6, where R6 is C1-C8 alkyl, optionally substituted with halogen, or (b) 2-, 3-, or 4-pyridyl, optionally substituted with halogen, —OH, —OR6, where R6 is C1-C8 alkyl, optionally substituted with halogen, or (c) a heterocycle selected from the group consisting of imidazole, thiazole, benzimidazole, benzoxazole, benzthiazole, tetrazole, triazole, and aminothiazole; or (d) —C(O)R7, where R7 is a C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, or a heterocycle selected from the group consisting of pyridyl, imidazole, thiazole, benzimi
    Type: Application
    Filed: November 8, 2007
    Publication date: July 1, 2010
    Applicants: FASGEN LLC, THE JOHNS HOPKINS UNIVERSITY
    Inventors: Craig Townsend, Francis Kuhajda, Kandasamy Subburaj, Jill Marie Sturdivant
  • Publication number: 20100168089
    Abstract: An in vitro method of screening for candidate compounds for the preventive or curative treatment of acne entails determination of the ability of a compound to inhibit the expression or the activity of TACE, and also to the administration of inhibitors of the expression or of the activity of this enzyme, in the treatment of acne.
    Type: Application
    Filed: December 17, 2009
    Publication date: July 1, 2010
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: JÉRÔME AUBERT, ISABELLE CARLAVAN, JOHANNES VOEGEL
  • Publication number: 20100160423
    Abstract: A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized. Analog and derivative molecules harbor a range of activities. The novel small molecule and most potent antagonist protects the eukaryote Caenorhabditis elegans from quorum-sensing-mediated killing by the bacterial pathogen Chromobacterium violaceum. The saving of C. elegans demonstrates the use of these molecules as small molecule antimicrobials.
    Type: Application
    Filed: December 21, 2009
    Publication date: June 24, 2010
    Inventors: Bonnie L. Bassler, Lee R. Swem, Scott M. Ulrich, Colleen T. O'Loughlin