The Five-membered Hetero Ring And Phosphorus Are Both Bonded Directly To The Same Nitrogen Patents (Class 548/115)
  • Publication number: 20130281708
    Abstract: A process for the production of fluorinated compound represented by the formula (I): or salts thereof wherein R1 and R2 are the same or different and each is selected from the group consisting of a hydrogen atom, a carbonyl group, a sulfonyl group and a phosphoryl group.
    Type: Application
    Filed: March 4, 2011
    Publication date: October 24, 2013
    Applicant: TAKEDA CALIFORNIA, INC.
    Inventor: Matthew Neil Mattson
  • Publication number: 20100233123
    Abstract: Provided herein are phosphothiophene and phosphothiazole compounds, for example, of any of Formulae I, IA, IIA, IIIA, IVA, VA, VIA, VIIA, IB, IIB, IIIB, IVB, VB, VIIB and VIIB disclosed herein, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host infected with HCV.
    Type: Application
    Filed: March 3, 2010
    Publication date: September 16, 2010
    Applicant: Idenix Pharmaceuticals, Inc.
    Inventors: Cyril Dousson, Claire Pierra, Jean-Francois Griffon, Frederic Leroy, Jean-Laurent Paparin, David Dukhan, Dominique Surleraux
  • Patent number: 7192968
    Abstract: The invention relates a compound represented by the formula (1): Q1-Q2-C(?O)—N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 represent H or the like; Q1 represents an aromatic ring, heterocyclic ring or the like; Q2 represents a single bond, aromatic ring, heterocyclic ring or the like; Q3 represents a group or the like, Q4 represents an aromatic ring, heterocyclic ring or the like; and T1 represents —CO— or —SO2—, and a medicine which comprises the compound and is useful for thrombosis and embolism.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: March 20, 2007
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Toshiharu Yoshino, Tsutomu Nagata, Noriyasu Haginoya, Kenji Yoshikawa, Hideyuki Kanno, Masatoshi Nagamochi
  • Patent number: 5958905
    Abstract: Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: ##STR1## in which A, B, R.sup.1 and R.sup.2 are as described are provided. Also provided are methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these compounds or prodrugs thereof. Methods for elucidating the physiological and pathophysiological roles of endothelin, as well as isolating endothelin receptors are also provided.
    Type: Grant
    Filed: March 26, 1996
    Date of Patent: September 28, 1999
    Assignee: Texas Biotechnology Corporation
    Inventors: Ming Fai Chan, Erik Joel Verner
  • Patent number: 5424303
    Abstract: The present invention relates to novel aminophosphonate derivatives substituted in .alpha. position by phenol groups, of formula (I): ##STR1## in which: X.sup.1, X.sup.2, X.sup.3, R.sup.1, R.sup.2, A, B, Z and n are defined in claim 1, as well as their preparations and the pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 26, 1993
    Date of Patent: June 13, 1995
    Assignee: Symphar SA
    Inventors: Hieu T. Phan, Lan M. Nguyen, Eric Niesor, Yves Guyon-Gellin, Craig L. Bentzen
  • Patent number: 5254546
    Abstract: Substituted imidazoles such as ##STR1## which are useful as angiotensin II receptor inhibitors. These compounds have activity in treating hypertension and congestive heart failure.
    Type: Grant
    Filed: June 18, 1992
    Date of Patent: October 19, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Robert J. Ardecky, David J. Carini, John Jonas V. Duncia, Pancras C. Wong
  • Patent number: 4851422
    Abstract: The compound represented by the formula: ##STR1## where R.sup.1 stands for amino or an organic residue bonded through nitrogen; R.sup.2 stands for carboxyl or a group derivable therefrom; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 independently stand for hydrogen or an organic residue, including the case where R.sup.5 or R.sup.6 forms a chemical bond or a ring with R.sup.7 or R.sup.8 ; X stands for hydrogen, methoxy or formylamino; or a salt thereof, produceable by the present method, exhibits excellent antimicrobial activity, and is utilized as antimicrobial agents.
    Type: Grant
    Filed: April 30, 1986
    Date of Patent: July 25, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideaki Natsugari, Yasuhiko Kawano, Akira Morimoto, Kouichi Yoshioka
  • Patent number: 4826993
    Abstract: 4-Substituted 1-(optionally substituted)diazolidinones are intermediates to 7-substituted bicyclic pyrazolidinone antimicrobials.
    Type: Grant
    Filed: May 14, 1986
    Date of Patent: May 2, 1989
    Assignee: Eli Lilly and Company
    Inventors: Richard E. Holmes, Louis N. Jungheim
  • Patent number: 4784993
    Abstract: The present invention provides diphosphonates of the general formula: ##STR1## wherein Het is 1,2,3-triazole, or 1,2,4-triazole radical, which is optionally substituted by alkyl, alkoxy, halogen, hydroxyl, carboxyl, an amino group optionally substituted by alkyl or acyl radicals or is a benzyl radical optionally substituted by alkyl, nitro, amino or aminoalkyl, A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 carbon atoms, X is a hydrogen atom, optionally substituted by acyl, or an amino group optionally substituted by alkyl or acyl radicals and R is a hydrogen atom or an alkyl radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these diphosphonates and pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 23, 1987
    Date of Patent: November 15, 1988
    Assignee: Boehringer Mannheim GmbH
    Inventors: Elmar Bosies, Rudi Gall
  • Patent number: 4770688
    Abstract: A 1-aryl-pyrazole of the formula ##STR1## in which R represents cyano or nitro,Ar represents in each case optionally substituted phenyl or pyridyl,X represents an azido group, or represents the radical ##STR2## and R.sup.1, R.sup.2 and R.sup.3 each independently represents alkyl, alkenyl, alkinyl, halogenoalkyl, alkoxy, alkoxyalkyl, cycloalkyl or cycloalkyloxy, or represents in each case optionally substituted aryl, aryloxy, aralkyl or aralkyloxy,but wherein, in the case where R represents cyano and X simultaneously represents an azido group, Ar does not represent unsubstituted phenyl and does not represent 5-nitro-2-pyridyl. The compounds exhibit herbicidal and plant growth-regulating activity.
    Type: Grant
    Filed: December 16, 1986
    Date of Patent: September 13, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhold Gehring, Markus Lindig, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
  • Patent number: 4695308
    Abstract: Herbicidally active substituted 5-amino-1-aryl-pyrazoles of the formula ##STR1## in which R represents hydrogen, cyano, nitro or alkoxycarbonyl,R.sup.1 represents hydrogen or alkyl,R.sup.2 and R.sup.3 independently of one another in each case represent alkyl, alkenyl, alkinyl, halogenoalkyl, alkoxyalkyl, cycloalkyl, alkoxy or cycloalkoxy, or represent in each case optionally substituted aryl, aryloxy, aralkyl or aralkyloxy,X represents oxygen or sulphur andAr represents in each case optionally substituted phenyl or pyridyl,or salts thereof.
    Type: Grant
    Filed: October 30, 1986
    Date of Patent: September 22, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhold Gehring, Markus Lindig, Otto Schallner, Hans-Joachim Santel, Robert R. Schmidt, Jorg Stetter
  • Patent number: 4687767
    Abstract: The present invention provides diphosphonates of the general formula: ##STR1## wherein Het is an imidazole, oxazole, isoxazole, thiazole, pyridine, 1,2,3-triazole, 1,2,4-triazole or benzimidazole radical, which is optionally substituted by alkyl, alkoxy, halogen, hydroxyl, carboxyl, an amino group optionally substituted by alkyl or alkanoyl radicals or a benzyl radical optionally substituted by alkyl, nitro, amino or aminoalkyl, A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 carbon atoms, X is a hydrogen atom, optionally substituted by alkanoyl, or an amino group optionally substituted by alkyl or alkanoyl radicals and R is a hydrogen atom or an alkyl radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these diphosphonates and pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 26, 1985
    Date of Patent: August 18, 1987
    Assignee: Boehringer Mannheim GmbH
    Inventors: Elmar Bosies, Rudi Gall
  • Patent number: 4654422
    Abstract: The invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is phosphono, dihalophosphoryl, di(lower) alkoxyphosphoryl, O-lower alkylphosphono, diaminophosphoryl, (amino) (hydroxy) phosphoryl or (lower alkoxy) (morpholino) phosphoryl,R.sup.2 is lower alkyl or lower alkenyl,R.sup.3 is a group of the formula: ##STR2## wherein X is hydrogen, halogen or lower alkoxy, or a group of the formula: ##STR3## wherein R.sup.4 is lower alkyl, and Y is N or CH; and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: October 9, 1985
    Date of Patent: March 31, 1987
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Tsutomu Teraji, Kazuo Sakane, Jiro Goto
  • Patent number: 4522647
    Abstract: Substituted phenoxyalkanediones and intermediates therefor, and the use of said compounds for the control of weeds.
    Type: Grant
    Filed: June 29, 1983
    Date of Patent: June 11, 1985
    Assignee: Zoecon Corporation
    Inventors: Richard J. Anderson, Shy-Fuh Lee
  • Patent number: 4188382
    Abstract: Thiazolinyl (thiazolyl) phosphonamidates and phosphoramidates of the formula: ##STR1## wherein R is a C.sub.1 -C.sub.4 -alkyl, a halo-C.sub.1 -C.sub.4 -alkyl, a C.sub.1 -C.sub.4 alkoxy; R' is a C.sub.1 -C.sub.4 -alkoxy, phenoxy, a halophenoxy, a C.sub.1 -C.sub.4 -alkyl-amino, dialkylamino or thiazolinyl-2-amino; X is oxygen or sulphur; Z is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH-- group which comprise an active principle for insecticidal, acaricidal and herbicidal compositions.
    Type: Grant
    Filed: February 25, 1977
    Date of Patent: February 12, 1980
    Assignee: Vsesojuzny Nauchno, et al.
    Inventors: Nikolai N. Melnikov, Artur F. Grapov, Ljudmila V. Razvodovskaya, Petr V. Popov, Aelita S. Sedykh, Galina K. Shapovalova, Galina M. Abelentseva, Tamara A. Siforova, Tatyana A. Nikolaeva, Valentina V. Galitsina, Leonid D. Stonov, Ljudmila A. Bakumenko