Nitrogen Or Additional Chalcogen Attached Indirectly To The Chalcogen By Acyclic Nonionic Bonding Patents (Class 548/264.4)
  • Publication number: 20150119571
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: September 4, 2014
    Publication date: April 30, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20150044233
    Abstract: Methods for determining the presence of cancer stem cells by detecting GD2 expression. Also provided are methods for reducing proliferation of cancer stem cells by contacting the cells with a GD2 targeting agent, such as an anti-GD2 antibody or a GD3 synthase inhibitor. GD3 synthase inhibitor compounds are also provided.
    Type: Application
    Filed: February 27, 2013
    Publication date: February 12, 2015
    Inventors: Venkata Battula, Michael Andreeff, Sendurai A. Mani, Tapasree Roy Sarkar
  • Publication number: 20140371222
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Kowalczyk-Prezewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Paul Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
  • Publication number: 20140288301
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Inventors: Dinesh U. Chimmanamada, Joseph A. Burlison, Weiwen Ying, Lijun Sun, Stefan M. Schweizer, Shijie Zhang, Zachary Demko, David James, Teresa Kowalczyk-Przewloka
  • Publication number: 20140242135
    Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Method of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: April 25, 2012
    Publication date: August 28, 2014
    Applicant: Vanderbilt University
    Inventors: Laurence Zwiebel, Gregory M. Pask, David C. Rinker, Ian M. Romaine, Gary A. Sulikowski, Paul R. Reid, Alex G. Waterson, Kwangho Kim, Patrick L. Jones, Robert W. Taylor
  • Publication number: 20140221658
    Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.
    Type: Application
    Filed: February 3, 2014
    Publication date: August 7, 2014
    Applicant: University of South Florida
    Inventors: Said M. Sebti, Srikumar Chellappan, Nicholas James Lawrence
  • Publication number: 20140148472
    Abstract: Disclosed are compounds able to modulate the activity of the GPR17 receptor in a highly specific way, which are useful in the treatment and diagnosis of diseases or dysfunctions involving the activation of said receptor. In particular, the compounds according to the invention can be used for neuroprotective and/or reparatory purposes, in cerebral, cardiac and renal ischaemia, in cerebral trauma, in chronic neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS), and in demyelinating diseases such as multiple sclerosis.
    Type: Application
    Filed: November 2, 2011
    Publication date: May 29, 2014
    Applicant: CENTRO CARDIOLOGICO MONZINO SpA
    Inventors: Mariapia Abbracchio, Ivano Eberini, Chiara Parravicini, Claudia Martini, Maria Letizia Trincavelli, Simona Daniele
  • Publication number: 20140100242
    Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
    Type: Application
    Filed: September 17, 2013
    Publication date: April 10, 2014
    Applicant: THE TRUSTEES OF PRINCETON UNIVERSITY
    Inventors: Bonnie Bassler, Lee Swem
  • Publication number: 20140005136
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: July 30, 2013
    Publication date: January 2, 2014
    Applicant: Ardea Biosciences, Inc.
    Inventors: Barry D. QUART, Jean-Luc GIRARDET, Esmir GUNIC, Li-Tain YEH
  • Publication number: 20130059852
    Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).
    Type: Application
    Filed: April 8, 2011
    Publication date: March 7, 2013
    Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
  • Publication number: 20130040907
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: May 4, 2012
    Publication date: February 14, 2013
    Applicant: Ardea Biosciences Inc.
    Inventors: Esmir GUNIC, Jean-Luc GIRARDET, Jean-Michel VERNIER, Martina E. TEDDER, David A. PAISNER
  • Publication number: 20130012557
    Abstract: Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.
    Type: Application
    Filed: May 12, 2012
    Publication date: January 10, 2013
    Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: Brian Clem, Sucheta Telang, John Trent, Jason Chesney, Pooran Chand, Gilles Tapolsky
  • Publication number: 20120283301
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Application
    Filed: July 18, 2012
    Publication date: November 8, 2012
    Applicant: Ardea Biosciences Inc.
    Inventors: Jean-Luc Girardet, Yung-Hyo Koh, Martha De La Rosa, Esmir Gunic, Zhi Hong, Stanley Lang, Woo-Hong Kim
  • Publication number: 20120220610
    Abstract: The present invention relates to a method of reducing the production of glutamate from glutamine by glutaminase C in a cell or tissue. The method involves inhibiting glutaminase C activity in the cell or tissue under conditions effective to reduce production of glutamate from glutamine. Compounds for carrying out this method are also disclosed.
    Type: Application
    Filed: March 25, 2010
    Publication date: August 30, 2012
    Applicant: CORNELL UNIVERSITY
    Inventors: Richard A. Cerione, Jon W. Erickson, Kristin Wilson Cerione, Jianbin Wang
  • Publication number: 20120189614
    Abstract: Organic compounds showing the ability to inhibit viral glycoprotein (GP)-mediated entry of a filovirus into a host cell are disclosed. The disclosed filovirus entry inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by filovirus including the type species Marburg virus (MARV) and Ebola virus (EBOV). Preferred inhibitors of the invention provide therapeutic agents for combating the Ivory Coast, Sudan, Zaire, Bundibugyo, and Reston Ebola virus strains.
    Type: Application
    Filed: July 10, 2010
    Publication date: July 26, 2012
    Applicant: Crobiotix, Inc.
    Inventors: Arnab Basu, Debra M. Mills, Norton P. Peet, John D. Williams
  • Publication number: 20120088662
    Abstract: The present invention relates to fungicidal mixtures comprising, as active components, 1) azolylmethyloxiranes of the general formula I in which the variables have the meanings described in the application, and 2) a fungicidal compound II, where the compounds II of component 2 are selected from among the compounds described in the application, and to the use of the fungicidal mixtures for controlling phytopathogenic fungi and to the compositions comprising them.
    Type: Application
    Filed: June 11, 2010
    Publication date: April 12, 2012
    Applicant: BASF SE
    Inventors: Jochen Dietz, Egon Haden, Jens Renner, Sarah Ulmschneider, Alice Glättli, Marianna Vrettou-Schultes, Silke Stolz
  • Publication number: 20120088771
    Abstract: This invention relates generally to the field of mineralization, and specifically to the role of TNAP in regulating the levels of extracellular inorganic pyrophosphate. The invention provides methods for modulating the activity of TNAP activity; methods for screening for modulators of TNAP activity; modulators of TNAP activity; and methods for treating pathologic conditions known of suspected to be affected by modulation of TNAP activity.
    Type: Application
    Filed: October 11, 2011
    Publication date: April 12, 2012
    Inventor: Jose Luis Millan
  • Publication number: 20120077981
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having N-(?-mercaptoacetyl) p amino benzoic acid derivatives. are provided, where Q is CO2H, or a salt or ester thereof, or a C(O) N-linked amino acid. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Application
    Filed: December 6, 2011
    Publication date: March 29, 2012
    Applicant: Ardea Biosciences Inc.
    Inventors: Jean-Luc Girardet, Yung-hyo Koh, Martha de la Rosa, Zhi Hong, Stanley Lang
  • Publication number: 20120077676
    Abstract: The present invention relates to novel triazole compounds of the formulae I and II as defined below which carry a sulfur substituent, to agricultural compositions containing them, to their use as fungicides and to intermediate compounds used in the method of producing them.
    Type: Application
    Filed: June 11, 2010
    Publication date: March 29, 2012
    Applicant: BASF SE
    Inventors: Jochen Dietz, Thomas Grote, Egon Haden, Bernd Mueller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Alice Glaetli, Marianna Vrettou-Schultes, Wassilios Grammenos
  • Publication number: 20110313157
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Application
    Filed: June 30, 2011
    Publication date: December 22, 2011
    Applicant: ARDEA BIOSCIENCES INC.
    Inventors: Jean-Luc Girardet, Yung-Hyo Koh, Martha De La Rosa, Esmir Gunic, Zhi Hong, Stanley Lang, Woo-Hong Kim
  • Publication number: 20110293719
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: June 30, 2011
    Publication date: December 1, 2011
    Applicant: Ardea Biosciences, Inc.
    Inventors: Barry D. Quart, Jean-Luc Girardet, Esmir Gunic, Li-Tain Yeh
  • Publication number: 20110257211
    Abstract: Small molecule choline kinase inhibitors having the following formula: are provided herein. Also provided herein are pharmaceutical compositions containing Formula I compounds, together with methods of treating cancer, methods of inhibiting choline kinase enzymatic activity, and methods of treating tumors by administering an effective amount of a Formula I compound.
    Type: Application
    Filed: December 22, 2010
    Publication date: October 20, 2011
    Applicants: ADVANCED CANCER THERAPEUTICS, LLC, UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: Pooran Chand, Jason A. Chesney, Brian F. Clem, Gilles H. Tapolsky, Sucheta Telang, John O. Trent
  • Publication number: 20110212994
    Abstract: Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.
    Type: Application
    Filed: June 28, 2010
    Publication date: September 1, 2011
    Inventors: BRIAN CLEM, SUCHETA TELANG, JOHN TRENT, JASON CHESNEY, POORAN CHAND, GILLES TAPOLSKY
  • Publication number: 20110112151
    Abstract: There is provided a compound of formula R1—CO—X—Y—Z—R2 wherein X and Z are each optional groups that are, independently, saturated or unsaturated carbon chains having a length of 1 to 3 carbons; Y is SO, S, SO2, CH?CH, CH2CH2 or O; R1 is wherein denotes the point of attachment; R2 is a heteroaryl group comprising an optionally substituted 5 or 6 membered ring, which ring contains only carbon and at least one nitrogen, or contains only carbon, and at least two nitrogens and at least one sulfur; and wherein (i) when R1 is and —CO—X—Y—Z— is CO—CH2—SO, CO—CH2—S, or CO—CH2—SO2, R2 is other than and; (ii) when R1 is and —CO—X—Y—Z— is —CO—CH2—O—, R2 is other than
    Type: Application
    Filed: February 25, 2009
    Publication date: May 12, 2011
    Inventors: Nigel Vicker, Xiangdong Su, Fabienne Pradaux-Caggiano, Barry Victor Lioyd Potter
  • Publication number: 20100317515
    Abstract: The present invention relates to triazolylmethyloxiranes of the formula I in which the variables A, B and D have the meanings described in the claims and the description.
    Type: Application
    Filed: December 12, 2008
    Publication date: December 16, 2010
    Applicant: BASF SE
    Inventors: Jochen Dietz, Thomas Grote, Bernd Mueller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Alice Glaettli, Marianna Vrettou
  • Publication number: 20100311581
    Abstract: The present invention relates to triazolylmethyloxiranes of the formula I in which the variables D and B have the meanings as defined in the description and the claims.
    Type: Application
    Filed: December 15, 2008
    Publication date: December 9, 2010
    Applicant: BASF SE
    Inventors: Jochen Dietz, Thomas Grote, Bernd Mueller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Alice Glaettli, Marianna Vrettou
  • Publication number: 20100273651
    Abstract: The present invention relates to azolylmethyloxiranes of the formula I in which the variables A, B and D have the meanings as defined in the description and the claims.
    Type: Application
    Filed: December 15, 2008
    Publication date: October 28, 2010
    Applicant: BASF SE
    Inventors: Jochen Dietz, Thomas Grote, Bernd Mueller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Alice Glaettli, Marianna Vrettou
  • Publication number: 20100137590
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having N-(?-mercaptoacetyl) p amino benzoic acid derivatives. are provided, where Q is CO2H, or a salt or ester thereof, or a C(O) N-linked amino acid. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Application
    Filed: February 2, 2010
    Publication date: June 3, 2010
    Applicant: Ardea Biosciences, Inc.
    Inventors: Jean-Luc Girardet, Yung-hyo Koh, Martha De La Rosa, Zhi Hong, Stanley Lang
  • Publication number: 20100056464
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: September 3, 2009
    Publication date: March 4, 2010
    Applicant: Ardea Biosciences
    Inventors: Esmir Gunic, Jean-Luc Girardet, Jean-Michel Vernier, Martina E. Tedder, David A. Paisner
  • Publication number: 20100056465
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: September 4, 2009
    Publication date: March 4, 2010
    Applicant: Ardea Biosciences
    Inventors: Esmir Gunic, Jean-Luc Girardet, Jean-Michel Vernier, Martina E. Tedder, David A. Paisner
  • Publication number: 20090197825
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: November 26, 2008
    Publication date: August 6, 2009
    Applicant: ARDEA BIOSCIENCES, INC.
    Inventors: Barry D. QUART, Jean-Luc GIRARDET, Esmir GUNIC, Li-Tain YEH
  • Publication number: 20090142347
    Abstract: This invention relates generally to the field of mineralization, and specifically to the role of TNAP in regulating the levels of extracellular inorganic pyrophosphate. The invention provides methods for modulating the activity of TNAP activity; methods for screening for modulators of TNAP activity; modulators of TNAP activity; and methods for treating pathologic conditions known of suspected to be affected by modulation of TNAP activity.
    Type: Application
    Filed: September 29, 2005
    Publication date: June 4, 2009
    Applicant: THE BURNHAM INSTITUTE FOR MEDICAL RESEARCH
    Inventor: José Luis Millan
  • Publication number: 20080319201
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having N-(?-mercaptoacetyl) p amino benzoic acid derivatives. are provided, where Q is CO2H, or a salt or ester thereof, or a C(O) N-linked amino acid. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Application
    Filed: August 18, 2008
    Publication date: December 25, 2008
    Applicant: Ardea Biosciences, Inc., a California Corporation
    Inventors: Jean-Luc Girardet, Yung-hyo Koh, Martha de la Rosa, Zhi Hong, Stanley Lang
  • Publication number: 20080249131
    Abstract: Various carbonyl amides are employed in vitro and in vivo as non-nucleoside inhibitors of a reverse transcriptase, and particularly of HIV reverse transcriptase. Therefore, contemplated compounds may be employed in the treatment of HIV infected patients. Further contemplated aspects include pharmaceutical compositions comprising therapeutically effective amounts of contemplated compounds.
    Type: Application
    Filed: May 2, 2008
    Publication date: October 9, 2008
    Applicant: Ardea Biosciences, Inc.
    Inventors: Jean-Luc Girardet, Zhijun Zhang, Robert Hamatake, Martha A. De La Rosa, Esmir Gunic, Zhi Hong, Hong Woo Kim, Yung-hyo Koh, Shahul Nilar, Stephanie Shaw, Nanhua Yao
  • Publication number: 20080242715
    Abstract: The present invention relates to novel compounds of formula (IC) or a salt thereof: wherein: p is an integer ranging from 0 to 4; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R5; m1, m2, m3, and m4 are 0; m5, m6 and m7 are each independently 0, 1 or 2 wherein the sum of m5, m6 and m7 is 1 or 2; R6 is C1-6alkyl; R7 is halogen, C1-6alkyl or haloC1-6alkyl; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is S or —CH2—; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R5 is isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl or 2-pyrrolidinonyl,
    Type: Application
    Filed: August 18, 2006
    Publication date: October 2, 2008
    Inventors: Anna Marie Capelli, Elettra Fazzolari, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20080167357
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl and indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R5; each R2 is independently hydrogen or C1-4alkyl; n is 2, 3, 4 or 5; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl and SF5; R5 is selected from a group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl and 2-pyrrolidinonyl, and such a grou
    Type: Application
    Filed: April 13, 2006
    Publication date: July 10, 2008
    Inventors: Dieter Hamprecht, Caterina Mazzoni, Fabrizio Micheli
  • Patent number: 7166607
    Abstract: The present invention relates to substituted indoles of formula (I) useful as pharmaceutical compounds for treating respiratory disorders
    Type: Grant
    Filed: May 27, 2003
    Date of Patent: January 23, 2007
    Assignee: AstraZeneca AB
    Inventors: Roger Bonnert, Stephen Brough, Tony Cook, Mark Dickinson, Rukhsana Rasul, Hitesh Sanganee, Simon Teague
  • Patent number: 7067656
    Abstract: A sulfamoyl compound of the general formulae (1): wherein R1 and R2 are each independently C1-4 alkyl, or R1 and R2 together are C4-6 alkylene or C4-6 alkyleneoxy, Y is H, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylthio, C1-8 haloalkyl, C1-8 haloalkoxy or C1-8 haloalkylthio, A is a predetermined heterocyclic group, B is a predetermined heterocyclic group which is identical with or different from A, W is a chemical bond or O, V is O or S, D, E, F and G are each independently N, CR7, CR8, CR9 or CR10, and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are each independently predetermined group such as H, or an unsubstituted or substituted aliphatic, aromatic or heterocyclic group. The sulfamoyl compound is useful as an agricultural and horticultural fungicide.
    Type: Grant
    Filed: July 9, 2003
    Date of Patent: June 27, 2006
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Toshiaki Takeyama, Toshimasa Hamada, Hiroaki Takahashi, Junichi Watanabe, Kazuhiro Yamagishi, Masanori Nishioka, Hiroyuki Suzuki
  • Patent number: 6927230
    Abstract: A compound of the formula (I): wherein R1 is lower alkyl which is optionally substituted with halogen, cyano, N,N-di(lower)alkylcarbamoyl, phenyl optionally substituted with halogen, or heterocyclic group, cyclo(lower)alkyl, lower alkynyl, or N,N-di(lower)alkylcarbamoyl; R2 is lower alkyl, lower alkoxy, cyano, or 1H-pyrrol-1-yl; R3 is lower alkyl, lower alkoxy, or cyano; X is O, S, SO or SO2; Y and Z are each CH or N; and m is 0 or 1; or salts thereof, which are useful as a medicament.
    Type: Grant
    Filed: October 30, 2002
    Date of Patent: August 9, 2005
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Satoshi Aoki, Toshiya Nakagawa, Nobukiyo Konishi, Katsuya Nakamura, Hiroki Omori, Ariyoshi Kubota, Norio Hashimoto
  • Patent number: 6696456
    Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where R1, R2, R3, R4, R5, R6, G and Z have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: February 24, 2004
    Assignee: The Procter & Gamble Company
    Inventors: Stanislaw Pikul, Norman Eugene Ohler, Kelly Michelle Solinsky, Neil Gregory Almstead, Biswanath De, Michael George Natchus
  • Patent number: 6693124
    Abstract: Bisimino-substituted phenyl compounds of the formula I where the substituents have the following meanings: X is a group A or B  where # denotes the bond with the phenyl ring and Ra is halogen, alkyl or alkoxy; Y is halogen, alkyl, haloalkyl or alkoxy; n is 0, 1 or 2, it being possible for the radicals Y to be different if n=2; R1 is alkyl; R2 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl; R3 is hydrogen, alkyl, haloalkyl or substituted or unsubstituted phenyl; R4 is ═CRbRc or ═N—ORd where Rb, Rc independently of one another are hydrogen, alkyl or substituted or unsubstituted phenyl; and Rd is one of the radicals mentioned under R2. Processes and intermediates for their preparation, and their use.
    Type: Grant
    Filed: December 6, 1999
    Date of Patent: February 17, 2004
    Assignee: BASF Aktiengesellschaft
    Inventors: Wassilios Grammenos, Herbert Bayer, Thomas Grote, Hubert Sauter, Andreas Gypser, Reinhard Kirstgen, Bernd Müller, Arne Ptock, Franz Röhl, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
  • Publication number: 20030162771
    Abstract: The present invention relates to compounds of formula: 1
    Type: Application
    Filed: June 12, 2002
    Publication date: August 28, 2003
    Inventors: Michel Geslin, Danielle Gully, Jean-Pierre Maffrand, Pierre Roger
  • Patent number: 6610631
    Abstract: The invention relates to novel substituted aryl ketones of the general formula (I) in which n, A, R1, R2, R3, R4 and Z are each as defined in the description, to processes for their preparation and to their use as herbicides.
    Type: Grant
    Filed: March 27, 2002
    Date of Patent: August 26, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus-Helmut Müller, Stefan Lehr, Otto Schallner, Hans-Georg Schwarz, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Patent number: 6605631
    Abstract: Compounds of the general formula I where the index and the substituents have the following meanings: n is 0 or 1 to 4; X is O or S; Y is a five-membered heteroaromatic ring; R1 is nitro; cyano; halogen; alkyl; haloalkyl; alkoxy; haloalkoxy; alkylthio; phenyl or phenoxy; R2 is hydrogen; alkyl, alkenyl or alkynyl; or a saturatedy,or unsaturated ring which, in addition to carbon atoms, can also contain hetero atoms as ring members are described.
    Type: Grant
    Filed: September 30, 1999
    Date of Patent: August 12, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Kirstgen, Wassilios Grammenos, Herbert Bayer, Reinhard Doetzer, Hartmann Koenig, Klaus Oberdorf, Hubert Sauter, Horst Wingert, Gisela Lorenz, Eberhard Ammermann, Volker Harries
  • Patent number: 6579892
    Abstract: Triazole compounds of the following formula where R1, R2, A and B have the meanings given in the description are described. The compounds according to the invention possess a high affinity for the dopamine D3 receptor and can therefore be used for treating diseases which respond to the influence of dopamine D3 ligands.
    Type: Grant
    Filed: July 11, 2001
    Date of Patent: June 17, 2003
    Assignee: Abbott Laboratories
    Inventors: Dorothea Starck, Hans-Jörg Treiber, Liliane Unger, Barbara Neumann-Schultz, Kai Blumbach, Dietmar Schöbel
  • Patent number: 6545161
    Abstract: Novel herbicidal and defoliant substituted aniline derived compounds represented by general structure (I) are described. W, X, Y, Z, and Q are as defined in the disclosure. Also described are the processes for the manufacture of these compounds and agriculturally suitable compositions containing these as active ingredients which are useful as herbicides for general or selective pre-emergent or post-emergent control of undesired plant species and defoliants at very low concentrations of these biologically active compounds.
    Type: Grant
    Filed: August 16, 2001
    Date of Patent: April 8, 2003
    Assignee: Isk Americas Incorporated
    Inventors: Sandeep Gupta, Shao-Yong Wu, Masamitsu Tsukamoto, David A. Pulman, Bai-Ping Ying
  • Patent number: 6472414
    Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X,  are as defined herein.
    Type: Grant
    Filed: May 18, 1999
    Date of Patent: October 29, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
  • Patent number: 6465650
    Abstract: The invention provides a processes for the preparation of a compound of Formula I, or a salt thereof wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH2, O, or NH; and B′ is a base customary in nucleotide chemistry. The processes include reacting a compound of Formula (II) with a compound of Formula (III) a compound of Formula (V) B′—CH2—CO—R2  (V), a monohaloacetic acid derivative in a suitable solvent with an auxiliary base, or a compound of Formula (VII) B′—CH2—CO—R3  (VII), and converting the resulting compounds to that of Formula I.
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: October 15, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Breipohl, Eugen Uhlmann, Jochen Knolle
  • Patent number: 6461997
    Abstract: New herbicidal compounds are provided having the formula wherein Y is oxygen or sulfur; R1 and R2 are each independently a C1-4 hydrocarbyl group, unsubstituted or substituted with one or more halogen, haloalkyl, hydroxy, alkoxy, carboxy, amido, cyano or amino groups; or R1 and R2, together with the carbamoyl nitrogen atom to which they are attached, form a nitrogen-containing five or six membered ring, the ring being optionally interrupted by an ethereal oxygen atom and unsubstituted or substituted with one or more hydroxy, amido, cyano, amino or C1-8 alkyl, alkenyl, alkynyl, cycloalkyl, arylalkyl, alkoxy, aminoalkyl or haloalkyl groups; and R3 is hydrogen, halogen, or an alkyl, cycloalkyl, alkenyl, cycloalkenyl, cycloalkylalkenyl, aryl, arylalkyl, alkylthio or arylalkylthio group that is unsubstituted or substituted with one or more halo, hydroxy, alkoxy, acetyloxy, benzoyloxy, alkoxycarbonyl, silyl or alkylsilyl groups; or an agronomically acceptable acid addition salt or metal complex of
    Type: Grant
    Filed: January 13, 2000
    Date of Patent: October 8, 2002
    Assignee: Monsanto Technology LLC
    Inventors: Shridhar G. Hegde, Martin D. Mahoney
  • Patent number: 6414007
    Abstract: Novel oxiranyl-triazolinethiones of the formula in which R1, R2 and R3 are each as defined in the description, a process for preparing the novel substances and their use as microbicides in crop protection and in the protection of materials.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: July 2, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Stefan Hillebrand, Manfred Jautelat, Astrid Mauler-Machnik, Klaus Stenzel, Martin Kugler, Otto Exner