Chalcogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/445)
  • Publication number: 20100152256
    Abstract: The present invention relates to novel (2R)-2-phenylpropanamides bearing a 4-sulfonylamino substituent on the 4 position of the phenyl group and to pharmaceutical compositions containing them, which are used as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells, and which are useful in the treatment of various ELR+CXC chemokine-mediated disorders. In particular, the compounds of the invention are useful in the treatment and control of specific CXCR2 dependent pathologies such as BOS, COPD, angiogenesis and melanoma.
    Type: Application
    Filed: December 15, 2009
    Publication date: June 17, 2010
    Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Andrea Aramini, Alessio Moriconi
  • Publication number: 20100143404
    Abstract: Compounds of formula (I), compositions, methods and kits are provided. The compounds and compositions may be particularly useful for modulating immunological responses. Formula (I) wherein, R1 is alkyl, aryl, or heterocyclyl; R2 is H, alkyl, aryl, heterocyclyl, OR3 or N(R3)2, R3 is H, alkyl, aryl, or heterocyclyl; R4 is H, CN, halogen, CF3, CO2R3, or C(O)N(R3)2; X is S, SO2, O, or NR3; and Y is S, O, or NR3.
    Type: Application
    Filed: December 29, 2004
    Publication date: June 10, 2010
    Inventors: Li-An Yeh, Gregory D. Cuny, Melissa Call, Kai Wucherpfennig, Ross L. Stein
  • Publication number: 20100119525
    Abstract: The present invention relates to a method for prolonging longevity using and NPC1L1 antagonist. The present invention also provides a method for reducing weight in an individual who consumes a high-fat diet using an NPC1L1 antagonist.
    Type: Application
    Filed: August 1, 2006
    Publication date: May 13, 2010
    Applicant: MOUNT SINAI SCHOOOL OF MEDICINE OF NEW YORK UNIVERSITY
    Inventor: Yiannis Ioannou
  • Publication number: 20100120901
    Abstract: A pharmaceutical composition comprising a pharmaceutical diluent and a compound of formula IV wherein R21=H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, —CH2OR25, —C(O)R25, —CO(O)R25, —C(O)NR25R26, —CH2C(O)R25, or —CH2C(O)NHR25, where R25 and R26 are each independently H, C1-C10 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing one or more halogen atoms. R22=—OH, —OR27, —OCH2C(O)R27, —OCH2C(O)NHR27, —OC(O)R27, —OC(O)OR27, —OC(O)NHNH—R5, or —OC(O)NR27R28, where R27 and R28 are each independently H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, and where R27 and R28 can each optionally contain halogen atoms; R23 and R24, the same or different from each other, are C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl. Methods of using such formulations for the treatment of cancer, to effect weight loss, to treat microbially-based infections, to inhibit neuropeptide-Y and/or fatty acid synthase, and to stimulate CPT-1.
    Type: Application
    Filed: January 13, 2010
    Publication date: May 13, 2010
    Applicants: FASGEN,INC, THE JOHNS HOPKINS UNIVERSITY
    Inventors: Francis P. Kuhajda, Susan M. Medghalchi, Jill M. McFadden, Jagan Thupari, Craig A. Townsend
  • Publication number: 20100099683
    Abstract: Methods for treating cancer using compounds that inhibit human DNA ligases. Methods for using compounds that inhibit human DNA ligases to provide insights into the reaction mechanisms of human DNA ligases, for example to identify the human DNA ligase involved in different DNA repair pathways. Screening methods for compounds that inhibit human DNA ligases.
    Type: Application
    Filed: October 9, 2009
    Publication date: April 22, 2010
    Inventors: Alan E. TOMKINSON, Xi CHEN, Barbara DZIEGIELEWSKA, Alexander D. MACKERELL, Shijun ZHONG, Gerald M. Wilson
  • Patent number: 7696244
    Abstract: The invention provides compositions, including pharmaceutical preparations, which comprise one or more substituted thiophene, benzofuran, pyrimidinetrione, dihydropyridine, tetrahydrocarbazol or anthraquinone compounds. The invention also features methods of use of such compositions in increasing activity of mutant-cystic fibrosis transmembrane conductance regulator protein in a cell, e.g. by increasing ion transport in a mutant-CFTR.
    Type: Grant
    Filed: May 14, 2004
    Date of Patent: April 13, 2010
    Assignee: The Regents of the University of California
    Inventors: Alan Verkman, Luis J. V. Galietta, R. Kiplin Guy
  • Patent number: 7691884
    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 determining ?-amyloid levels in a subject are described.
    Type: Grant
    Filed: March 16, 2005
    Date of Patent: April 6, 2010
    Assignees: Wyeth, ArQule, Inc.
    Inventors: Anthony Frank 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: 20100081652
    Abstract: Disclosed is an extracellular matrix genetranscription inhibitor composition or the like characterized by containing a cinnamoyl compound represented by the formula (I) below: and an inert carrier.
    Type: Application
    Filed: March 2, 2006
    Publication date: April 1, 2010
    Inventors: Hiroaki Shiraki, Kiyoshi Higashi, Yoshitaka Tomigahara, Junya Takahashi
  • Patent number: 7678790
    Abstract: Novel compounds of formula (I) to (VI), 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)-(VI), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 23, 2005
    Date of Patent: March 16, 2010
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles Marlowe
  • Publication number: 20100048666
    Abstract: A compound represented by the formula (1) or a salt thereof ( represents a single bond, or a double bond; R1 represents hydrogen atom, or an alkyl group; R2 and R3 represent hydrogen atom, or an alkyl group; R4 and R5 represent hydrogen atom, hydroxy group, an alkoxyl group, a halogen atom, or a mono- or di-alkyl-substituted amino group; R6 represents hydrogen atom, cyano group, an alkoxycarbonyl group, or carboxy group; R7 represents one or two of substituents on the benzene ring (the substituents are selected from hydrogen atom, a halogen atom, nitro group, cyano group, hydroxy group, amino group, an alkyl group, and an alkoxyl group); A represents a 5-membered or 6-membered non-aromatic heterocyclic ring containing one or two contiguous sulfur atoms (the sulfur atoms may independently form oxide); W represents oxo group, hydrogen atom, an alkyl group, hydroxy group, an alkoxyl group, or a halogen atom; and X represents oxygen atom, or sulfur atom), or a salt thereof, which has a superior suppressing action
    Type: Application
    Filed: September 10, 2007
    Publication date: February 25, 2010
    Applicant: FUJI YAKUHIN CO., LTD.
    Inventors: Hideo Kato, Osamu Nagata, Yoshiyuki Iwabuchi, Takahiro Sato, Junichiro Uda, Tutomu Inoue, Hiroshi Nakamura, Nobuhide Kawasaki, Ippei Tanaka, Naoki Kurita, Tomohiko Ishikawa
  • Publication number: 20100048684
    Abstract: The present invention relates to agents and methods for growth-factor receptor activation by modulating the G-protein mediated signal transduction pathway.
    Type: Application
    Filed: November 3, 2009
    Publication date: February 25, 2010
    Applicant: Max-Planck-Gesellschaft zur Forderung der Wissenschaften e.V.
    Inventors: Axel Ullrich, Norbert Prenzel, Esther Zwick-Wallasch, Henrik Daub
  • Publication number: 20100029752
    Abstract: A pharmaceutical composition containing a pharmaceutical diluent and a compound of formula II: wherein: R8?H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, —C(O)R4, where R4 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms, or —OH, —OR7 or —NR7, where R7 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms; R9=—OR5, —NR5, —NH—NH—R5 where R5 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl, optionally containing halogen atoms; R10?H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, or —CH2C(O)R6, where R6 is OR7 and NR7, where R7?H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl and can optionally contain halogen atoms. Also included in the invention are methods of using the pharmaceutical compositions and the chemical compounds used in the compositions.
    Type: Application
    Filed: July 26, 2006
    Publication date: February 4, 2010
    Inventors: Francis P. Kuhajda, Craig A. Townsend, Susan M. Medghalchi, Jill M. McFadden
  • Publication number: 20100029719
    Abstract: The present invention relates to sulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are useful in the treatment of neuronal disorders, autoimmune diseases, cancer and cardiovascular diseases. Furthermore, said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and -3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation.
    Type: Application
    Filed: September 24, 2009
    Publication date: February 4, 2010
    Applicant: LABORATOIRES SERONO S.A.
    Inventors: Thomas RUECKLE, Jean-Pierre Gotteland, Russel J. Thomas, Marco Biamonte
  • Publication number: 20100022601
    Abstract: The sulfoneamide compounds having the following Formula (1), which can be used as an effective component of a CaSR antagonizing agent useful for prophylaxis and/or treatment of bone disorders including osteoporosis and etc., are provided. The compounds have an excellent activity of promoting PTH secretion. In addition, the compounds are useful as an effective component of a medicament for the prophylaxis and/or treatment of bone disorders such as osteoporosis, bone fracture, hypoparathyroidism and the like.
    Type: Application
    Filed: June 2, 2009
    Publication date: January 28, 2010
    Applicant: ASAHI KASEI PHARMA CORPORATION
    Inventors: Masami OGAWA, Kazuhiko KITAGAWA, Hiromitsu SHIRAHASHI, Satomi KURIBAYASHI
  • Publication number: 20100022594
    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 9, 2009
    Publication date: January 28, 2010
    Applicants: Wyeth, ArQule, Inc.
    Inventors: Anthony F. Kreft, Derek Cecil Cole, Kevin R. Woller, Joseph R. Stock, George Diamantidis, Dennis M. Kubrak, Kristina M. Kutterer, William J. Moore, David S. Casebier
  • Publication number: 20100022520
    Abstract: Compounds characterized by thiolactone or thiomorpholino cores display useful antibiotic and radioprotective properties. The latter properties are believed to arise from an ability of the compounds to inhibit proteins involved in apoptosis.
    Type: Application
    Filed: May 22, 2009
    Publication date: January 28, 2010
    Inventor: Alexander Doemling
  • Patent number: 7649012
    Abstract: A pharmaceutical composition comprising a pharmaceutical diluent and a compound of formula IV wherein R21=H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, —CH2OR25, —C(O)R25, —CO(O)R25, —C(O)NR25R26, —CH2C(O)R25, or —CH2C(O)NHR25, where R25 and R26 are each independently H, C1-C10 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing one or more halogen atoms. R22=—OH, —OR27, —OCH2C(O)R27, —OCH2C(O)NHR27, —OC(O)R27, —OC(O)OR27, —OC(O)NHNH—R5, or —OC(O)NR27R28, where R27 and R28 are each independently H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, and where R27 and R28 can each optionally contain halogen atoms; R23 and R24, the same or different from each other, are C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl. Methods of using such formulations for the treatment of cancer, to effect weight loss, to treat microbially-based infections, to inhibit neuropeptide-Y and/or fatty acid synthase, and to stimulate CPT-1.
    Type: Grant
    Filed: July 9, 2003
    Date of Patent: January 19, 2010
    Assignees: FASgen, Inc., Johns Hopkins University
    Inventors: Francis P. Kuhajda, Susan M. Medghalchi, Jill M. McFadden, Jagan Thupari
  • Patent number: 7612108
    Abstract: The present invention relates to a 2-phenylthiophene derivative or a salt thereof, wherein the thiophene ring is substituted with a carboxyl group or the like and the benzene ring has an electron-withdrawing group such as a cyano group and an electron-donating group such as a substituted alkoxy group at the same time. Since the compound of the invention has good xanthine oxidase-inhibitory action and uric acid-lowering action and does not have a structure derived from nucleic acid, the compound has advantages of high safety and excellent effects as compared with conventional compounds and is useful as a therapeutic or preventive agent for hyperuricemia, gout, inflammatory bowel diseases, diabetic kidney diseases, diabetic retinopathy, or the like.
    Type: Grant
    Filed: August 26, 2005
    Date of Patent: November 3, 2009
    Assignee: Astellas Pharma Inc.
    Inventors: Junji Miyata, Masaki Yokota, Ryo Naito, Akio Kamikawa, Masakatsu Kawakami, Kazuyuki Hattori
  • Publication number: 20090227667
    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: Application
    Filed: May 5, 2009
    Publication date: September 10, 2009
    Applicant: Wyeth
    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: 20090215775
    Abstract: Compounds of formula (I) are disclosed for treatment of cancer.
    Type: Application
    Filed: May 16, 2006
    Publication date: August 27, 2009
    Inventors: Huw David Lewis, Timothy Harrison, Mark Steven Shearman
  • Publication number: 20090181932
    Abstract: A synthetic compound characterized by having the structure of formula I or II or a pharmaceutically acceptable salt and/or hydrate thereof is provided. Formula I and formula II are defined as follows. wherein R1 is substituted aryl or substituted heteroaryl; R2 and R3 are independently selected from the group consisting of CF3, substituted phenyl, C1-C4 alkyl, substituted C1-C4 alkyl, (CF3)nC1-C4alkyl, (CF3)n(substituted C1-C4 alkyl), provided that when R2 or R3 is CF3, the other is not an unsubstituted alkyl; R4 and R4? are independently selected from the group consisting of M, C1-C4 alkyl, phenyl, and benzyl, wherein M is a metal ion is selected from the group consisting of sodium, lithium, calcium, magnesium and potassium, or R4 and R4? are taken together to form a cyclic structure. Methods of making such compounds and uses thereof are also provided.
    Type: Application
    Filed: January 7, 2009
    Publication date: July 16, 2009
    Applicant: Wyeth
    Inventors: David Zenan LI, Dane Springer, Sayed Elmarakby, Appavu Chandrasekaran, Anthony F. Kreft, III
  • Publication number: 20090176762
    Abstract: This invention relates to the use of a JNK inhibitor for treating and/or preventing skin diseases selected from psoriasis and dermatitis.
    Type: Application
    Filed: June 1, 2007
    Publication date: July 9, 2009
    Applicant: LABORATOIRES SERONO SA
    Inventors: Chiara Ferrandi, Jean-Pierre Gotteland, Christoph H. Ladel, Paola Zaratin
  • Patent number: 7553868
    Abstract: The invention relates to thiophene carboxamides of formula (I) wherein Ar, R1, R2, R3, R4, R5, m and n are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: January 13, 2004
    Date of Patent: June 30, 2009
    Assignee: AstraZeneca AB
    Inventors: Andrew David Morley, Jeffrey Philip Poyser
  • Publication number: 20090156611
    Abstract: The disclosure relates to compositions for and methods of inhibiting the mammalian Hedgehog signaling pathway.
    Type: Application
    Filed: November 10, 2006
    Publication date: June 18, 2009
    Applicant: Licentia Ltd.
    Inventors: Antti Oinas, Jussi Taipale, Juhani Lahdenperä
  • Patent number: 7547725
    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(substituted alkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substituted phenyl), 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: June 15, 2007
    Date of Patent: June 16, 2009
    Assignee: Wyeth
    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
  • Patent number: 7534811
    Abstract: Cyclic onium compounds reresented by the following structural formula (I), glucosidase inhibitors using such compounds, and antidiabetic drugs or food containing such glucosidase inhibitor. wherein A? is an aniom; m is an interger between 1 and 6, n is 0 or 1, X+ is S+ or N+Q (where Q is H or an alkyl of 1 to 4 carbon atoms).
    Type: Grant
    Filed: May 31, 2004
    Date of Patent: May 19, 2009
    Assignees: Kinki University, Diabetym Co., Ltd.
    Inventors: Osamu Muraoka, Masayuki Yoshikawa, Genzoh Tanabe, Hisashi Matsuda
  • Publication number: 20090124684
    Abstract: This invention provides methods and compositions for inducing weight loss and maintaining optimum weight comprising administering an agent that stimulates carnitine palmitoyl transferase-1 (CPT-1) activity to the patient in need, including human patients. These methods do not require inhibition of fatty acid synthesis. In particular, this invention provides methods for development of therapeutics that selectively enhance fatty acid oxidation, increase energy production, and reduce adiposity while preserving lean mass, through the pharmacological stimulation of CPT-1 activity. In a preferred mode, the agent is administered in an amount sufficient to increase fatty acid oxidation. In another preferred mode, the agent is administered in an amount sufficient to antagonize malonyl CoA inhibition of CPT-1. In yet another preferred mode, the agent is administered in an amount sufficient to increase malonyl CoA level.
    Type: Application
    Filed: November 6, 2008
    Publication date: May 14, 2009
    Applicant: The Johns Hopkins University School of Medicine Licensing and Technology Development
    Inventors: Jagan N. Thupari, Leslie E. Landree, Gabrielle Ronnett, Francis P. Kuhajda
  • Publication number: 20090124664
    Abstract: The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
    Type: Application
    Filed: November 24, 2006
    Publication date: May 14, 2009
    Inventors: Marcello Allegretti, Alessio Moriconi, Andrea Aramini, Maria Candida Cesta, Andrea Beccari, Riccardo Bertini
  • Publication number: 20090105218
    Abstract: Compounds of formula (I) are useful in the treatment of disease responsive to modulation of CRTH2 receptor activity, wherein: A represents a carboxyl group —COOH, or a carboxyl bioisostere; L1 is a bond, —CH2—, —OCH2—, —CH2CH2— or —CH?CH—; L2 is CONH—, —NHCO—, SO2NR1—, —NR1SO2 wherein R1 is hydrogen or C1-C3 alkyl, or a divalent radical of formula (X) or (Y), wherein ring Q is a non aromatic heterocyclic ring containing 5 to 7 ring atoms, including the nitrogen shown; L3 is a divalent linker radical of formula -(Alk1)m-(Z)n-(Alk2)p as defined in the description; ring Ar1 is an optionally substituted divalent phenyl radical or divalent 5- or 6-membered monocyclic heteroaryl radical, in which L1 and the H[B]sL3L2Ar2CONH-radical are linked to adjacent ring carbon atoms; ring Ar2 is an optionally substituted 1,3-phenylene radical, or an optionally substituted divalent 5- or 6-membered monocyclic heteroaryl radical, in which AL1Ar1NHCO-radical and the H[B]sL3L2-radical are linked to ring carbon atoms which are not
    Type: Application
    Filed: May 30, 2005
    Publication date: April 23, 2009
    Applicant: 7TM PHARMA A/S
    Inventors: Trond Ulven, Thomas Frimurer, Oystein Rist, Evi Kostenis, Thomas Hogberg
  • Patent number: 7521473
    Abstract: Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted thiophene compounds such as, for example, 2-carboxyl, 3-carboxymethoxy, 5-aryl substituted thiophenes, can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.
    Type: Grant
    Filed: February 23, 2005
    Date of Patent: April 21, 2009
    Assignee: Wyeth
    Inventors: Jinbo Lee, Zhao-Kui Wan, Douglas P. Wilson, Bruce C. Follows, Steven J. Kirincich, Michael J. Smith, Jun-Jun Wu, Kenneth W. Foreman, David V. Erbe, Yan-Ling Zhang, Weixin Xu, Steve Y. Tam
  • Publication number: 20090093536
    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: Application
    Filed: August 6, 2008
    Publication date: April 9, 2009
    Applicant: Chungbuk National University Industry Academic Cooperation Foundation
    Inventors: Jin Tae Hong, Jung Ok Ban, Heon-Sang Jeong, Dae Joong Kim
  • Publication number: 20090093530
    Abstract: The present invention relates to novel (2R)-2-phenylpropanamides bearing a 4-sulfonylamino substituent on the 4 position of the phenyl group and to pharmaceutical compositions containing them, which are used as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells, and which are useful in the treatment of various ELR+CXC chemokine-mediated disorders. In particular, the compounds of the invention are useful in the treatment and control of specific CXCR2 dependent pathologies such as BOS, COPD, angiogenesis and melanoma.
    Type: Application
    Filed: May 17, 2007
    Publication date: April 9, 2009
    Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Andrea Aramini, Alessio Moriconi
  • Publication number: 20090047365
    Abstract: The present invention relates to a pharmaceutical composition, a kit, a method of treating cancer and/or a method of inhibiting angiogenesis comprising a sulfonamide compound in combination with a platinum complex, a DNA-topoisomerase I inhibitor, an antimetabolite, a microtubule inhibitor or an antibiotic.
    Type: Application
    Filed: February 28, 2006
    Publication date: February 19, 2009
    Applicant: Eisai R & D Management Co., Ltd.
    Inventors: Takashi Owa, Yoichi Ozawa, Taro Semba, Naoko Hata
  • Publication number: 20090029903
    Abstract: The present invention is related to carboxylic acids of Formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of carboxylic acids of Formula (I) to modulate, notably to inhibit the activity of PTPs.
    Type: Application
    Filed: March 29, 2005
    Publication date: January 29, 2009
    Inventors: Dominique Swinnen, Catherine Jorand-Lebrun, Patrick Gerber, Jerome Gonzalez, Agnes Bombrun
  • Patent number: 7482376
    Abstract: The present invention is directed to conjugated complement cascade inhibitors, and a method of treating a patient using a conjugated complement cascade inhibitor.
    Type: Grant
    Filed: June 16, 2004
    Date of Patent: January 27, 2009
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Nalin Subasinghe, Ehab Khalil, Farah Ali, Heather Rae Hufnagel, Shelley Ballentine, Jeremy M. Travins, Kristi A. Leonard, Roger F. Bone
  • Publication number: 20090023801
    Abstract: Novel sulfonamide compounds useful in the treatment of conditions related to the production of beta-amyloid are described, as are routes to their preparation. The sulfonamide compounds are of the following structure, wherein R1-R3 are defined herein. Also provided are pharmaceutical compositions containing these compounds and/or prodrugs of these compounds and a physiologically compatible carrier. These compounds are specifically useful for inhibiting beta amyloid production, and treating Alzheimer's Disease, amyloid angiopathy, cerebral amyloid angiopathy, systemic amyloidosis, hereditary cerebral hemorrhage with amyloidosis of the Dutch type, inclusion body myositis, mild cognitive impairment (MCI) and Down's syndrome.
    Type: Application
    Filed: July 14, 2008
    Publication date: January 22, 2009
    Applicant: Wyeth
    Inventors: Thomas J. Caggiano, Koi M. Morris, Boyd L. Harrison, Anthony F. Kreft, III, Dennis M. Kubrak, Dane M. Springer
  • Publication number: 20090018169
    Abstract: This present invention is related to sulfonamide derivatives of Formula (I), pharmaceutical composition thereof, methods of preparation thereof and to their use for the treatment and/or prophylaxis of bacterial infections such as tuberculosis.
    Type: Application
    Filed: February 9, 2007
    Publication date: January 15, 2009
    Applicant: Laboratoires Serono SA
    Inventors: Jerome Gonzalez, Dominique Swinnen, Agnes Bombrun, Rob Hooft Van Huijsduijnen, Timothy Wells
  • Publication number: 20090012127
    Abstract: Compounds of Formula (I) wherein E, A and R1 are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.
    Type: Application
    Filed: June 26, 2006
    Publication date: January 8, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Thomas R. Simpson, Michael Balestra, Dean G. Brown, Cathy L. Dantzman, Glen E. Ernst, William Frietze, Christopher R. Holmquist, James Kang, Frances M. McLaren, Reed W. Smith, JR., James M. Woods
  • Publication number: 20090005435
    Abstract: A pharmaceutical composition comprising a pharmaceutical diluent and a compound of formula (II), wherein R1 and R2, the same or different from each other, are H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, —CH2CORS, —CH2C(O)NRS, —C(O)R5, or —CH2OR5, and can optionally contain halogen atoms, where R5 is a C1-C12 alkyl group. R3 and R4, the same or different from each other, are H, C1-C20 alkyl cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl.
    Type: Application
    Filed: May 25, 2005
    Publication date: January 1, 2009
    Inventors: Jill M. Sturdivant, Craig Townsend, Susan Medghalchi
  • Publication number: 20080312313
    Abstract: A compound of formula (I), wherein the residues have various meanings, useful as pharmaceuticals.
    Type: Application
    Filed: December 22, 2006
    Publication date: December 18, 2008
    Inventors: Jose M. Carballido Herrera, Herbert Jaksche, Philipp Lehr, Gudrun Werner, Anthony Winiski
  • Publication number: 20080300295
    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: Application
    Filed: December 22, 2006
    Publication date: December 4, 2008
    Inventors: Jose M. Carballido Herrera, Herbert Jaksche, Philipp Lehr, Gudrun Werner, Anthony Winiski
  • Patent number: 7459479
    Abstract: The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.
    Type: Grant
    Filed: March 8, 2007
    Date of Patent: December 2, 2008
    Assignee: Biolipox AB
    Inventors: Ronald W. Lauener, David L. Burgoyne, Patrick J. Rebstein, Lloyd F. Mackenzie, Yuanlin Zhou, Yaping Shen
  • Publication number: 20080286282
    Abstract: The present invention relates to a pharmaceutical composition, a kit and a method for treating cancer and/or a method for inhibiting angiogenesis, comprising a sulfonamide compound in combination with Bevacizumab.
    Type: Application
    Filed: February 28, 2006
    Publication date: November 20, 2008
    Applicant: Eisai R & D Management Co., Ltd.
    Inventors: Taro Semba, Naoko Hata, Yoichi Ozawa, Takashi Owa
  • Publication number: 20080255108
    Abstract: Disclosed are compounds for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade. Said compounds are of Formula I or a solvate, hydrate, pharmaceutically acceptable salt, or prodrug thereof; wherein Ra, Rb, and Rc are defined in the specification, as are A Z, Q, R1 and R2.
    Type: Application
    Filed: April 3, 2008
    Publication date: October 16, 2008
    Inventors: Nalin L. Subasinghe, Shelley Ballentine, Jeremy M. Travins, Ehab M. Khalil, Farah Ali, Kristi A. Leonard, Joan M. Gushue, Michael Peter Winters, Heather Hufnagel, Maxwell David Cummings
  • Publication number: 20080200499
    Abstract: The present invention relates to the use of selective insecticidal and/or acaricidal compositions, characterized in that they comprise an effective amount of an active compound combination comprising (a) at least one substituted cyclic dicarbonyl compound of the formula (I) in which W, X, Y and Z are as defined in the description and CDC is one of the dicarbonyl radicals mentioned in the description, and (b) at least one crop plant compatibility-improving compound from the group of compounds given in the description. for controlling insects and/or arachnids, and also to a method for controlling insects and/or arachnids using the compositions.
    Type: Application
    Filed: July 18, 2005
    Publication date: August 21, 2008
    Inventors: Reiner Fischer, Udo Reckmann, Chris Rosinger, Erich Sanwald, Christian Arnold
  • Publication number: 20080194597
    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: August 20, 2007
    Publication date: August 14, 2008
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: ROBERT M. SCARBOROUGH, Wolin Huang, Charles K. Marlowe, Kim A. Kane-Maguire
  • Patent number: 7375131
    Abstract: The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I?B. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-?B in which diseases excessive activation of NF-?B is implicated.
    Type: Grant
    Filed: May 29, 2003
    Date of Patent: May 20, 2008
    Assignee: SmithKlineBeecham Corp.
    Inventors: James F. Callahan, Yue Hu Li
  • Patent number: 7358376
    Abstract: The invention relates to heteroaromatic carboxamides of formula (I), wherein A, R1, R2 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: February 7, 2001
    Date of Patent: April 15, 2008
    Assignee: AstraZeneca AB
    Inventors: Andrew Baxter, Stephen Brough, Alan Faull, Craig Johnstone, Thomas McInally
  • Patent number: 7351825
    Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.
    Type: Grant
    Filed: December 15, 2004
    Date of Patent: April 1, 2008
    Assignee: Japan Tobacco Inc.
    Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
  • Patent number: 7351841
    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: Grant
    Filed: December 6, 2005
    Date of Patent: April 1, 2008
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa