Sulfur Containing Hetero Ring (e.g., Thioxane, Etc.) Patents (Class 544/145)
  • Patent number: 9901636
    Abstract: The present invention relates to novel chitosan-based conjugates, e.g. nanocarriers, comprising a derivative of the biocompatible polymer chitosan conjugated to a photosensitizing agent, and uses thereof in photochemical internalization (PCI) and photodynamic therapy (PDT). The invention also relates to the use of the novel conjugates of the invention in treatment or prevention of diseases, particularly cancer, and for vaccination purposes.
    Type: Grant
    Filed: May 14, 2013
    Date of Patent: February 27, 2018
    Assignee: PCI BIOTECH AS
    Inventors: Kristian Berg, Anders Hogset, Mar Masson, Vivek S. Gaware
  • Publication number: 20150034887
    Abstract: A novel photochromic compound which develops a color of a neutral tint (double peak characteristic) and has high color optical density, high fading speed and excellent durability. Like a compound represented by the following formula (20), the photochromic compound having a group (methylthio group in the following formula 20) which has a sulfur atom bonded to the 7-position carbon atom is a photochromic compound having high color optical density, high fading speed and excellent durability.
    Type: Application
    Filed: March 11, 2013
    Publication date: February 5, 2015
    Applicant: TOKUYAMA CORPORATION
    Inventors: Shinobu Izumi, Yasutomo Shimizu, Junji Momoda
  • Patent number: 8691352
    Abstract: Disclosed is a photopolymerizable composition which contains a photopolymerization initiator (A) that has a partial structure represented by the following Formula (1) and a polymerizable compound (B). In General formula (1), R3 and R4 each independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group or an alkoxy group; R3 and R4 may form a ring with each other; and X represents OR5, SR6, or NR17R18. The photopolymerizable composition is capable of forming a cured film that has high sensitivity, excellent intra-membrane curability and excellent adhesion to a support. The cured film is able to maintain a patterned shape even during post-heating after development and has good pattern formability, while coloring due to heating with passage of time being suppressed.
    Type: Grant
    Filed: August 10, 2010
    Date of Patent: April 8, 2014
    Assignee: FUJIFILM Corporation
    Inventor: Masaomi Makino
  • Publication number: 20140054520
    Abstract: A novel photochromic compound which develops a color of a neutral tint and has high color optical density, high fading speed and excellent durability. The present invention is a chromene compound having an indeno(2,1-f)naphtho(1,2-b)pyran structure as the basic skeleton in which a hetero ring having two hetero atoms including at least one sulfur atom is directly bonded to the 6-position and the 7-position of the indeno(2,1-f)naphtho(1,2-b)pyran structure via the hetero atom like the compound represented by the following formula (18).
    Type: Application
    Filed: March 7, 2012
    Publication date: February 27, 2014
    Applicant: TOKUYAMA CORPORATION
    Inventors: Junji Takenaka, Junji Momoda, Kazuhiro Teranishi, Toshiaki Takahashi, Mitsuyoshi Sando, Shinobu Izumi
  • Publication number: 20120231392
    Abstract: A salt represented by the formula (I) and a resist composition containing the salt are provided, wherein Q1, Q2, L1, ring W1, Re1, Re2, Re3, Re4, Re5, Re6, Re7, Re8, Re9, Re10, Re11, Re12, Re13 and Z are defined in the specification.
    Type: Application
    Filed: March 7, 2012
    Publication date: September 13, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Satoshi YAMAGUCHI, Koji ICHIKAWA
  • Patent number: 8227495
    Abstract: The present disclosure provides 2,4-disubstituted thiazoles of the general structure shown below that are agonists of G-protein coupled receptor (IC-GPCR2). Also, provided are compositions comprising these compounds as well as methods for using these compounds in a variety of applications including diabetes and metabolic disorders.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: July 24, 2012
    Assignee: Metabolex Inc.
    Inventors: Xin Chen, Peng Cheng, L. Edward Clemens, Jeffrey D. Johnson, Jingyuan Ma, Alison Murphy, Imad Nashashibi, Christopher J. Rabbat, Jiangao Song, Maria E. Wilson, Yan Zhu, Zuchun Zhao
  • Publication number: 20120176571
    Abstract: Disclosed is a photopolymerizable composition which contains a photopolymerization initiator (A) that has a partial structure represented by the following Formula (1) and a polymerizable compound (B). In General formula (1), R3 and R4 each independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group or an alkoxy group; R3 and R4 may form a ring with each other; and X represents OR5, SR6, or NR17R18. The photopolymerizable composition is capable of forming a cured film that has high sensitivity, excellent intra-membrane curability and excellent adhesion to a support. The cured film is able to maintain a patterned shape even during post-heating after development and has good pattern formability, while coloring due to heating with passage of time being suppressed.
    Type: Application
    Filed: August 10, 2010
    Publication date: July 12, 2012
    Applicant: FUJIFILM CORPORATION
    Inventor: Masaomi Makino
  • Patent number: 8101605
    Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
    Type: Grant
    Filed: December 3, 2010
    Date of Patent: January 24, 2012
    Assignee: Aquinox Pharmaceuticals Inc.
    Inventors: Lloyd Mackenzie, Tom MacRury, Curtis Harwig, Jeremy Pettigrew, Noor Aini Bhatti, Sam Place, Paul Bird, Vladimir Khlebnikov, Rudong Shan
  • Publication number: 20110212954
    Abstract: The present invention concerns an enantiomer R of a compound of Formula (I), wherein X is —NH—R1 or of Formula (V) or (VI), R1 is —(CH2)n—R2, R2 is a linear, branched or cyclic C1C6 aliphatic group, —O—(CH2)n—CH3, —NH—CO—(CH2)n—CH3, a 5- or 6-membered aliphatic or aromatic ring optionally comprising a heteroatom, a 5- or 6-membered aromatic ring substituted by one or two substituents, said substituents being selected from the group consisting of —OH, —O(alkyl C1C3) and —OCO(alkyl C1C3), or of Formula (V), R3 is H or a C1-C3 aliphatic group and R4 is a linear C1-C3 or a branched C3-C12 aliphatic group, or R3 is a C1-C3 aliphatic group and R4 is a linear C1-C12 aliphatic group, Y is O, CH—(CH2)n—CH3 or N(CO)(CH2)n—CH3, and n is an integer from O to 6.
    Type: Application
    Filed: November 6, 2009
    Publication date: September 1, 2011
    Inventors: Mario Brufani, Ilaria Medici, Rinaldo Marini Bettolo, Luisa Maria Migneco, Rolando Marzella, Rocco Figliola, Angela La Bella
  • Publication number: 20110171569
    Abstract: Compounds of the formula (I), wherein R1, R2 and R3 for example are hydrogen, halogen, CN, C1-C18alkyl, C1-C10 haloalkyl, (CO)R8, (CO)OR4, or (CO)NR5R6; Y is O, S or CO; D2, D3 and D4 for example are a direct bond, O, S, NR7, CO, O(CO), (CO)O, S(CO), (CO)S, NR7(CO), (CO)NR7, SO, SO2, or OSO2, C1-C18alkylene, C3-C30cycloalkylene, C2-C12alkenylene, C4-C30cycloalkenylene, Ar1; Ar1, Ar2 and Ar3 are for example phenylene, R4, R5, R6, R7 and R8 are for example hydrogen, C3-C30-cycloalkyl, C1-C18alkyl, C1-C10haloalkyl, C2-C12alkenyl, C4-C30cycloalkenyl, phenyl-C1C3-alkyl; X? is Formulae (IA), (IB) or (IC); R10 is for example C1-C18alkyl, C1-C10haloalkyl, camphoryl, phenyl-C1-C3alkyl, C3-C30cycloalkyl; and R11, R12, R13, R14 and R15 are for example C1-C10haloalkyl; are useful as polymerizable photolatent acids.
    Type: Application
    Filed: June 2, 2009
    Publication date: July 14, 2011
    Inventors: Yuichi Nishimae, Toshikage Asakura, Hitoshi Yamato
  • Patent number: 7973030
    Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.
    Type: Grant
    Filed: February 25, 2005
    Date of Patent: July 5, 2011
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Takehiko Sasahara, Mitsunobu Mohri, Ken-Ichi Kasahara
  • Publication number: 20110152255
    Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J, B, Y, and A are as described in claims 1-13. Methods, compositions, and medicaments related thereto are also disclosed, for treating baldness, glaucoma or inflammatory bowel diseases.
    Type: Application
    Filed: April 21, 2009
    Publication date: June 23, 2011
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Patent number: 7960378
    Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y, A, R1, R2, Z, and G are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: June 14, 2011
    Assignee: Allergan, Inc.
    Inventors: Mark Holoboski, Robert M. Burk, Mari Posner
  • Publication number: 20110136802
    Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
    Type: Application
    Filed: December 3, 2010
    Publication date: June 9, 2011
    Applicant: Aquinox Pharmaceuticals Inc.
    Inventors: Lloyd Mackenzie, Tom MacRury, Curtis Harwig, Jeremy Pettigrew, Noor Aini Bhatti, Sam Place, Paul Bird, Vladimir Khlebnikov, Rudong Shan
  • Publication number: 20110098469
    Abstract: The present invention provides a 1-thio-D-glucitol compound of the following formula, which shows the action of inhibiting the activity of SGLT2, a pharmaceutically acceptable salt of the compound, or a hydrate of the compound or the salt; and a pharmaceutical comprising such a compound as an active ingredient, especially, a pharmaceutical for preventing or treating diabetes, diabetes-related disease, or diabetic complication. The invention also provides a method for producing the 1-thio-D-glucitol compound and its intermediate.
    Type: Application
    Filed: December 30, 2010
    Publication date: April 28, 2011
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Hiroyuki KAKINUMA, Yuko Hashimoto, Takahiro Ol, Hitomi Takahashi
  • Patent number: 7834001
    Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.
    Type: Grant
    Filed: November 8, 2005
    Date of Patent: November 16, 2010
    Assignee: Piramal Life Sciences Limited
    Inventors: Bansi Lal, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More
  • Patent number: 7803797
    Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein G, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: April 22, 2009
    Date of Patent: September 28, 2010
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Patent number: 7799824
    Abstract: Quaternary salt compounds of Formula (I) or pharmaceutically acceptable forms thereof, which are CCR2 antagonists and are useful in preventing, treating or ameliorating CCR2 mediated inflammatory syndromes, disorders or diseases in a subject in need thereof.
    Type: Grant
    Filed: June 22, 2005
    Date of Patent: September 21, 2010
    Assignee: OraPharma, Inc.
    Inventors: Bharat Lagu, Michael Wachter
  • Publication number: 20100190766
    Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.
    Type: Application
    Filed: December 10, 2009
    Publication date: July 29, 2010
    Applicant: Achaogen, Inc.
    Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
  • Patent number: 7642254
    Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 together form, along with the nitrogen atom to which they are attached, an optionally substituted nitrogen containing heterocyclic ring having from 4 to 8 ring atoms; and R3 is selected from hydroxy and —NRN1RN2, where RN1 and RN2 are independently selected from hydrogen, optionally substituted C1-7 alkyl groups, optionally substituted C3-20 heterocyclyl groups and optionally substituted C5-20 aryl groups, or together form, along with the nitrogen atom to which they are attached, an optionally substituted nitrogen containing heterocyclic ring having from 4 to 8 ring atoms, and its use in inhibiting ATM.
    Type: Grant
    Filed: February 9, 2006
    Date of Patent: January 5, 2010
    Assignee: Kudos Pharmaceuticals Limited
    Inventors: Marc Geoffrey Hummersone, Keith Allan Menear, Laurent Jean Martin Rigoreau, Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Roger John Griffin
  • Publication number: 20090218039
    Abstract: An dye compound of the following formula (1): wherein D represents a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group; L represents ?CR2—, ?N—, or ?N—NH—; R1 represents a monovalent substituent; R2 represents a hydrogen atom or a cyano group; n indicates an integer of from 0 to 4; when n is 2 or more, then plural R1's may be the same or different.
    Type: Application
    Filed: February 27, 2009
    Publication date: September 3, 2009
    Applicant: FUJIFILM Corporation
    Inventors: Yoshihiko FUJIE, Tetsuya WATANABE, Hisashi MIKOSHIBA
  • Patent number: 7534791
    Abstract: The present invention relates to benzo[b]furane and benzo[b]thiophene derivatives of the general formula IV as the free base or salts thereof and their use.
    Type: Grant
    Filed: June 14, 2006
    Date of Patent: May 19, 2009
    Assignee: H. Lundbeck A/S
    Inventors: Jan Kehler, Karsten Juhl, Morten Bang Norgaard
  • Publication number: 20090054427
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
    Type: Application
    Filed: August 22, 2008
    Publication date: February 26, 2009
    Inventors: Emmanuelle Briard, Rainer Martin Lueoend, Rainer Machauer, Henrik Moebitz, Olivier Rogel, Jean-Michel Rondeau, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra
  • Publication number: 20090043091
    Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and RN1 is selected from hydrogen, an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, an optionally substituted C5-20 aryl group, an acyl group, an ester group and an amido group, and its use as a pharmaceutical.
    Type: Application
    Filed: September 19, 2008
    Publication date: February 12, 2009
    Applicant: KUDOS PHARMACEUTICALS LIMITED
    Inventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Laurent Jean Martin Rigoreau, Marc Geoffrey Hummersone, Roger John Griffin
  • Patent number: 7429667
    Abstract: The invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted-3-hydroxy-5-arylamino-isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones.
    Type: Grant
    Filed: January 20, 2006
    Date of Patent: September 30, 2008
    Assignee: Ardea Biosciences, Inc.
    Inventors: Hassan Abdellaoui, Robert Tam, Huanming Chen, Varaprasad Chamakura, Dinesh Barawkar, Andreas Maderna, Zhi Hong, Stanley Lang
  • Patent number: 7429660
    Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and RN1 is selected from hydrogen, an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, an optionally substituted C5-20 aryl group, an acyl group, an ester group and an amido group, and its use as a pharmaceutical.
    Type: Grant
    Filed: August 13, 2004
    Date of Patent: September 30, 2008
    Assignee: Kudos Pharmaceuticals Limited
    Inventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Laurent Jean Martin Rigoreau, Marc Geoffrey Hummersone, Roger John Griffin
  • Patent number: 7405212
    Abstract: Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein Y, A, B, R1 and R2 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing the same, are neurokinin (tachykinin) antagonists. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening such libraries to identify biologically active members.
    Type: Grant
    Filed: May 3, 2005
    Date of Patent: July 29, 2008
    Assignee: Myriad Genetics, Inc.
    Inventors: Vincent Huber, Jan Urban, Hiroshi Nakanishi, Masakatsu Eguchi, Jessymol Mathew, Min Sang Lee
  • Patent number: 7208491
    Abstract: Mono-acylated o-phenylendiamines derivatives of formula I wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone deacetylase, such as cancer.
    Type: Grant
    Filed: February 3, 2004
    Date of Patent: April 24, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
  • Patent number: 7202242
    Abstract: The invention relates to substituted 1 and 2 naphthol Mannich bases, a method for the production thereof, medicaments containing said compounds and the use of said compounds in the production of medicaments.
    Type: Grant
    Filed: January 15, 2004
    Date of Patent: April 10, 2007
    Assignee: Gruenenthal GmbH
    Inventors: Matthias Gerlach, Corinna Maul
  • Patent number: 7105518
    Abstract: The present invention provides compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein R1 and R2 are independently hydrogen, an option ally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and R3 is an optionally substituted C3-20 heterocyclyl or C5-20 aryl group, and their use as pharmaceuticals, particularly in treating diseases which are retroviral mediated or ameliorated by the inhibition of DNA-PK,
    Type: Grant
    Filed: August 14, 2002
    Date of Patent: September 12, 2006
    Assignee: Cancer Research Technology Limited
    Inventors: Niall Morrison Barr Martin, Graeme Cameron Murray Smith, Roger John Griffin, Bernard Thomas Golding, Ian Robert Hardcastle, Laurent Jean Martin Rigoreau, David Richard Newell, Hilary Alan Calvert, Nicola Jane Curtin, Paul Workman, Florence Irene Raynaud, Bernard Paul Nutley
  • Patent number: 7067516
    Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: June 27, 2006
    Assignee: Tularik Limited
    Inventors: Sarah Elizabeth Lively, Martin James Harrison, Neil Jason Naylor, Christopher Neil Farthing, Bohdan Waszkowycz
  • Patent number: 7049313
    Abstract: The application concerns a compound of formula I: wherein one of P and Q is O, and the other of P and Q is CH, where there is a double bond between whichever of Q and P is CH and the carbon atom bearing the R3 group; Y is either O or S; R1 and R2 are independently hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; R3 is a phenyl or pyridyl group, attached by a first bridge group selected from —S—, —S(?O)—, —S(?O)2—, —O—, —NRN— and CRC1RC2— to an optionally substituted C5-20 carboaryl group, the phenyl or pyridyl group and optionally substituted C5-20 carboaryl group being optionally further linked by a second bridge group, so as to form an optionally substituted C5-7 ring, the phenyl or pyridyl group being further optionally substituted.
    Type: Grant
    Filed: February 24, 2003
    Date of Patent: May 23, 2006
    Assignee: Kudos Pharmaceuticals Ltd.
    Inventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Stephen Philip Jackson, Mark James O'Connor, Alan Yin Kai Lau, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Laurent Jean Martin Rigoreau, Marc Geoffery Hummersone, Roger John Griffin
  • Patent number: 6972292
    Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: December 6, 2005
    Assignee: Novartis AG
    Inventors: Frederick Ray Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
  • Patent number: 6849658
    Abstract: The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R1 is CH3, —CH2—O—R6, —OR6 or —COR7; R2 is —OR8, —SR8 or a polyether radical if in the latter case R4 is C1-C20alkyl and is in ortho or meta position relative to X—Ar; R3 is alkyl or R2 and R3 together form a cycle optionally interrupted by O or S; R4 is aryl radical; R5 is H, halogen, C1-C20 alkyl or —OR8; R6 is H, alkyl or —COR9; R7 is H, alkyl, —N(r?)(r?) or —OR10; R8 is H, alkyl or —COR9; R9 is alkyl; R10 is H, C1-C20 alkyl, alkenyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aralkyl or a sugar residue, r? and r? are H, alkyl mono- or polyhydroxyalkyl, aryl, an amino acid or sugar residue or together form a heterocycle, X represents a radical of formula (d) or (e) in which R11 is H or —OR6; R12 is H or alkyl; or R11 and R12 form an oxo radical, and the salts, optical and geometrical isomers of the compounds of formula (I).
    Type: Grant
    Filed: October 31, 2001
    Date of Patent: February 1, 2005
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Simon Trouille
  • Patent number: 6849733
    Abstract: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.
    Type: Grant
    Filed: August 22, 1997
    Date of Patent: February 1, 2005
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Yufeng Hong, Vlad Edward Gregor, Anthony Lai Ling, Eileen Valenzuela Tompkins
  • Publication number: 20040180883
    Abstract: This invention relates to compounds of formula (I) wherein R2 to R10, —X—Y—, A, —W—, n and p have the values defined in claim 1, their preparation and use as pharmaceuticals.
    Type: Application
    Filed: December 12, 2003
    Publication date: September 16, 2004
    Inventors: Jeremy Gilmore, Carlos Lamas-Peteira, Maria Alicia Torrado Varela
  • Publication number: 20040157841
    Abstract: Mono-acylated o-phenylendiamines derivatives of formula I 1
    Type: Application
    Filed: February 3, 2004
    Publication date: August 12, 2004
    Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
  • Publication number: 20040152698
    Abstract: Compounds of general formula (I), in which Het represents a five or six membered saturated, partially unsaturated or aromatic ring containing between one and six heteroatoms of the group N, O, S, in which the heterocycle is substituted in an adjacent manner with -P-Qi-T-Q2, -GZ and Y, such that the substituant -GZ is adjacent to both, the other substituants being as defined in the description, process for preparing this compound, fungicidal composition comprising this compound, method for treating plants by applying this compound or composition.
    Type: Application
    Filed: April 1, 2004
    Publication date: August 5, 2004
    Inventors: Stephanie Gary, Tim Lange, Benoit Muller, Christopher Richard Steele, Geoffrey Gower Briggs, Joseph Perez, Alain Villier, Brian Hill
  • Patent number: 6756372
    Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.
    Type: Grant
    Filed: November 2, 2001
    Date of Patent: June 29, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Michel Jose Emmanuel, Weimin Liu, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward
  • Patent number: 6730671
    Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.
    Type: Grant
    Filed: February 13, 2003
    Date of Patent: May 4, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
  • Patent number: 6730670
    Abstract: A compound of the formula Compounds of formula I have a good affinity to the A2A receptor and are useful for the treatment of diseases mediated by this receptor.
    Type: Grant
    Filed: December 10, 2002
    Date of Patent: May 4, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Alexander Flohr
  • Publication number: 20040077854
    Abstract: The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation.
    Type: Application
    Filed: October 10, 2003
    Publication date: April 22, 2004
    Inventors: Serge Halazy, Dennis Church, Stephen J. Arkinstall, Marco Biamonte, Montserrat Camps, Jean-Pierre Gotteland, Thomas Rueckle
  • Publication number: 20040058923
    Abstract: Compounds of formula (I) wherein: R1 represents C1-16 alkyl, C2-6alkenyl, C2-6alkynyl, C2-6alkynyl-Y1—, aryl-Y1—, heteroaryl-Y1—, aryl-(O)t-aryl-Y1—, aryl-(O)t-heteroaryl-Y1—, heteroaryl-(O)t-aryl-Y1—, heteroaryl-(O)t-heteroaryl-Y1—, C2-6 alkenyl-Y1—, aryl-O—Y1—, heteroaryl-O—Y1—, C1-16 alkyl-SO2—Y1—,M—Y1—,J2-Y1—, —CN or C3-8 cycloalkyl-Y1— or C3-8 cycloalkenyl-Y1—, which cycloalkyl or cycloalkenyl may be optionally substituted by one or more hydroxyl or C1-16 Alkyl groups; R2 represents hydrogen or C1-16 alkyl; X represents ethylene or a group of formula CReRf wherein Re and Rf independently represent hydrogen or C1-14 alkyl or Re and Rf may together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R3 and R4 independently represent hydrogen or C1-14 alkyl; Z represents a bond, CO, SO2, CR9R6(CH2)n, (CH2)nCR9R6, CHR6(CH2)nO, CHR6(CH2)nS, CHR6(CH2)nOCO, CHR6(CH2)n
    Type: Application
    Filed: August 15, 2003
    Publication date: March 25, 2004
    Inventors: Rachael Anne Ancliff, Caroline Mary Cook, Colin David Eldred, Paul Martin Gore, Lee Andrew Harrison, Simon Teanby Hodgson, Duncan Bruce Judd, Suzanne Elaine Keeling, Xiao Qing Lewell, Graeme Michael Robertson, Stephen Swanson
  • Patent number: 6703416
    Abstract: The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R1 is CH3, —CH2—O—R6, —OR6 or —COR7; R2 is —OR8, —SR8 or a polyether radical if in the latter case R4 is C1-C20alkyl and is in ortho or meta position relative to X—Ar; R3 is alkyl or R2 and R3 together form a cycle optionally interrupted by O or S; R4 is aryl radical; R5 is H, halogen, C1-C20 alkyl or —OR8; R6 is H, alkyl or —COR9; R7 is H, alkyl, —N(r′)(r″) or —OR10; R8 is H, alkyl or —COR9; R9 is alkyl; R10 is H, C1-C20 alkyl, alkenyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aralkyl or a sugar residue, r′ and r″ are H, alkyl mono- or polyhydroxyalkyl, aryl, an amino acid or sugar residue or together form a heterocycle, X represents a radical of formula (d) or (e) in which R11 is H or —OR6; R12 is H or alkyl; or R11 and R12 form an oxo radical, and the salts, optical and geometrical isomers of
    Type: Grant
    Filed: October 31, 2001
    Date of Patent: March 9, 2004
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Simon Trouille
  • Publication number: 20040030131
    Abstract: A compound of the formula in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholino group, said group being optionally substituted with 1 to 3 substituents selected from C1-4 alkyl, hydroxymethyl, C1-4 alkoxymethyl and amido, R3 is a naphthyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; and m is 0 or 1, provided that when m is 1 then n is 1; or a salt or ester thereof.
    Type: Application
    Filed: September 3, 2003
    Publication date: February 12, 2004
    Inventors: Martine Keenan, Vincent Patrick Rocco, Kumiko Takeuchi, David Edward Tupper, Vincent Vivien
  • Publication number: 20040029914
    Abstract: Novel compounds are useful as chemotherapeutic, chemopreventative, and antiangiogenic agents are provided. The compounds are flavanoids, including flavanones, flavanols, and chalcones.
    Type: Application
    Filed: April 18, 2003
    Publication date: February 12, 2004
    Inventors: Nurulain Zaveri, Wan-Ru Chao
  • Patent number: 6686467
    Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines
    Type: Grant
    Filed: October 8, 2002
    Date of Patent: February 3, 2004
    Assignee: Zeneca Limited
    Inventors: Dearg S Brown, George R Brown, Philip Cohen
  • Publication number: 20040019084
    Abstract: The invention concerns novel lipoic acid derivatives, which have an inhibiting action with respect to NO-synthase enzymes producing nitrogen monoxide NO and/or are agents enabling the regeneration of antioxidants or entities trapping reactive oxygen species (ROS) and intervening in a more general manner in the redox status of thiol groups. The invention also concerns methods for preparing them, pharmaceutical compositions containing them and their use for therapeutic purposes, particularly their use as NO-synthase inhibitors and/or as agents acting more generally in the redox status of thiol groups.
    Type: Application
    Filed: April 21, 2003
    Publication date: January 29, 2004
    Applicant: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATION SCIENTIFIQUES (S.C.R.A.S)
    Inventors: Jeremiah Harnett, Michel Auguet, Pierre-Etienne Chabrier de Lassauhyere
  • Publication number: 20030232827
    Abstract: This invention to antagonists that inhibit transporters and receptors. The invention also relates to partial inhibitors of transporters and receptors that allow partial transport or partial binding of a compound to the transporter or receptor. The invention also relates to compounds that differentially prevent transport or binding through a transporter or to a receptor. The invention also relates to the use of these compounds for treating certain diseases and disorders.
    Type: Application
    Filed: February 10, 2003
    Publication date: December 18, 2003
    Inventors: Peter C. Meltzer, Bertha K. Madras, Paul Blundell, Shanghao Lui
  • Publication number: 20030232819
    Abstract: The present invention provides novel tropane compounds and methods for their use.
    Type: Application
    Filed: March 27, 2003
    Publication date: December 18, 2003
    Inventors: Paul Blundell, Peter C. Meltzer, Bertha K. Madras