Halogen Attached Indirectly To The Thiocarbonyl By Nonionic Bonding Patents (Class 564/29)
  • Publication number: 20150080580
    Abstract: ?-Chymotrypsin inhibitors of thiourea class are reported that could be potent inhibitors of proteases, elastases, proteasomes, NS3 and NS4 serine protease of hepatitis C virus, dengue virus, etc. Compounds 1-22, which are belong to thiourea class, showed good inhibition. Their kinetics study and cytotoxicity profiles showed all type of inhibition except uncompetitive-type inhibition and no cytotoxicity except few compounds. Competitive type of inhibitors could inhibit other ?-chymotrypsin-like serine proteases, which are therapeutics target.
    Type: Application
    Filed: September 18, 2013
    Publication date: March 19, 2015
    Inventors: Atta-ur Rahman, Bishnu P. Marasini, Muhammad Iqbal Choudhary, Khalid M. Khan, Farzana Sheikh, Atia-tul- Wahab
  • Publication number: 20140171313
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171315
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Patent number: 8629299
    Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.
    Type: Grant
    Filed: May 20, 2013
    Date of Patent: January 14, 2014
    Assignee: Hammersmith Imanet Limited
    Inventors: Erik Arstad, Matthias Eberhard Glaser
  • Patent number: 8445721
    Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: May 21, 2013
    Assignee: Hammersmith Imanet Limited
    Inventors: Erik Arstad, Matthias Eberhard Glaser
  • Patent number: 8148575
    Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.
    Type: Grant
    Filed: April 20, 2007
    Date of Patent: April 3, 2012
    Assignee: Hammersmith Imanet Limited
    Inventors: Erik Arstad, Matthias Eberhard Glaser
  • Publication number: 20100234503
    Abstract: A polymer composite includes a polymer matrix and an alkyl-substituted carbon nanotube. A polymer composite also includes a polymer matrix and a fluorinated carbon nanotube reacted with urea, thiourea, or guanidine. A method of functionalizing a carbon nanotube includes heating a fluorinated carbon nanotube urea, thiourea, or guanidine. A substituted carbon nanotube includes a fluorinated carbon nanotube and amino silane compounds The amino silane compounds covalently link to the fluorinated nanotube through the amino functional group. Polymer composites, ceramics and surface coating materials may be constructed from these substituted carbon nanotubes.
    Type: Application
    Filed: August 10, 2007
    Publication date: September 16, 2010
    Inventors: Valery N. Khabashesku, Merlyn X. Pulikkathara
  • Publication number: 20100093864
    Abstract: The present application discloses thiourea compounds for use in the treatment of infections. The thiourea compounds have formula (I) wherein X1 and X2 each designate one or more substituents; and Z is —(CHR)—, —(CHR)2—, —O—(CHR)2—, —NH—(CHR)2—, or —S—(CHR)2—; including salts thereof.
    Type: Application
    Filed: October 12, 2007
    Publication date: April 15, 2010
    Applicant: LICA PHARMACEUTICALS
    Inventors: Simon Feldbaek Nielsen, Arsalan Kharazmi, Mogens Larsen
  • Patent number: 7696249
    Abstract: The invention relates to novel specifically trifluoromethyl and halogen substituted 1,3-diphenyl ureas and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects like the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: April 13, 2010
    Assignee: ARPIDA AG
    Inventors: Ralf Loewe, Sergio Lociuro, Stephen Hawser, Laurent Schmitt
  • Patent number: 7674827
    Abstract: Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds for combating animal pests The present invention relates to Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds of formula I wherein the variables R1 to R4 are as in the description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection.
    Type: Grant
    Filed: November 15, 2006
    Date of Patent: March 9, 2010
    Assignee: BASF SE
    Inventors: Markus Kordes, Christopher Koradin, Deborah L. Culbertson
  • Patent number: 7632970
    Abstract: The present invention relates to a production method of asymmetric compound (IV) which includes conjugately adding nucleophilic reagent (III) to compound (II) in the presence of asymmetric urea compound (I). The present invention provides a non-metallic asymmetric catalyst capable of realizing a highly stereoselective asymmetric conjugate addition reaction in a high yield, and an advantageous production method of an asymmetric compound by an asymmetric conjugate addition reaction using the asymmetric catalyst.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: December 15, 2009
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Yoshiji Takemoto
  • Publication number: 20090005452
    Abstract: The invention relates to novel specifically trifluoromethyl and halogen substituted 1,3-diphenyl ureas and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects like the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.
    Type: Application
    Filed: December 8, 2006
    Publication date: January 1, 2009
    Applicant: ARIPIDA AG
    Inventors: Ralf Loewe, Sergio Lociuro, Stephen Hawser, Laurent Schmitt
  • Patent number: 7094807
    Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.
    Type: Grant
    Filed: November 18, 2003
    Date of Patent: August 22, 2006
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Dawei Chen, Milind Deshpande, Andrew Thurkauf, Avinash Phadke, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
  • Patent number: 6866833
    Abstract: A substituted thiourea having the general formula characterized in that each of R1 and R2 independently comprises an alkyl, alkaryl or aryl group or a substituted derivative thereof, and contains at least one fluorine atom, and in that each of R3 and R4 is selected from the group which consists of H, alkyl, alkaryl and aryl and substituted derivatives thereof, including fluorine-containing derivatives. A method for producing the substituted thiourea is disclosed, and a method for extracting a noble metal such as gold from a matrix by treating the matrix with the substituted thiourea is also disclosed.
    Type: Grant
    Filed: February 8, 2000
    Date of Patent: March 15, 2005
    Assignee: University College Cork
    Inventors: Jeremy Denis Glennon, Jane Harris, Stephen John Harris
  • Patent number: 6794541
    Abstract: This invention provides combinatorial chemistry libraries containing thiourea and urea compounds. In addition, the invention relates to methods for constructing combinatorial chemistry libraries containing thiourea and urea compounds. Furthermore, this invention relates to methods for the identification of bioactive thiourea and urea compounds as well as compositions and therapeutic methods for treating cancer.
    Type: Grant
    Filed: September 19, 2001
    Date of Patent: September 21, 2004
    Assignee: Parker Hughes Institute
    Inventors: Zhaohai Zhu, Chen Mao, Rama K. Narla, Fatih M. Uckun
  • Patent number: 6743790
    Abstract: The present invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5, R6, A, X, m and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, for example as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Grant
    Filed: June 6, 2001
    Date of Patent: June 1, 2004
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Otmar Klingler, Manfred Schudok, Hans-Peter Nestler, Hans Matter, Herman Schreuder
  • Patent number: 6380422
    Abstract: Compounds of the formula I and disulfides thereof and salts thereof are important intermediate products for the preparation of compounds having a microbicidal and plant-immunizing action, of the formula III In the compounds of the formulae I and III: X is halogen, n is 0, 1, 2 or 3; Z is CN, CO—A or CS—A, A is hydrogen, halogen, OR1, SR2 and N(R3)R4; R1 to R4 are hydrogen, a substituted or unsubstituted, open-chain, saturated or unsaturated hydrocarbon radical containing not more than 8 carbon atoms, a substituted or unsubstituted cyclic, saturated or unsaturated hydrocarbon radical containing not more than 10 carbon atoms, substituted or unsubstituted benzyl or phenethyl, a substituted or unsubstituted alkanoyl group containing not more than 8 carbon atoms, a substituted or unsubstituted benzoyl group or a substituted or unsubstituted heterocyclyl radical; or R3 and R4, together with the nitrogen atom to which they are bonded, are a 5- or 6-membered, subs
    Type: Grant
    Filed: February 26, 1999
    Date of Patent: April 30, 2002
    Assignee: Syngenta Investment Corportion
    Inventors: Walter Kunz, Beat Jau
  • Patent number: 6271261
    Abstract: Novel IL-8 receptor antagonists and methods of using them are provided.
    Type: Grant
    Filed: December 17, 1998
    Date of Patent: August 7, 2001
    Assignee: SmithKline Beecham Corporation
    Inventor: Katherine L Widdowson
  • Patent number: 6255349
    Abstract: Compounds having the formula:  wherein  R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W—Y—(CH2)n—Z provided that at least one of R1-R5 is not hydrogen; or R2 and R3or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl;  R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl;  R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or  R7 an
    Type: Grant
    Filed: November 22, 1999
    Date of Patent: July 3, 2001
    Assignee: American Home Products Corporation
    Inventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Stanley Lang, Emily Norton, Adma Ross, Bryan O'Hara
  • Patent number: 5952386
    Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.
    Type: Grant
    Filed: September 24, 1997
    Date of Patent: September 14, 1999
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
  • Patent number: 5723075
    Abstract: A near-infrared absorbent is obtained by heating a dimerized thiourea derivative of Formula ?1! or ?2! and a copper compound: ##STR1## The near-infrared absorbent is used to obtain a near-infrared absorbent resin material having a wide absorption in the near-infrared region, and the absorbent does not substantially decompose at a molding temperature of the resin. Typical examples of the dimerized thiourea derivative are 4,4'-di(benzylthiocarbamoyl)-aminodiphenylmethane, 4,4'-di(benzylthiocarbamoyl)-aminodiphenylhexafluoropropane, and 1,4'-di(dibenzoylthiocarbamoylamino)-2,5-dimethylbenzene, and typical examples of the copper compound are copper stearate and copper .beta.-acryloyloxypropylhydrogenphthalate.
    Type: Grant
    Filed: April 19, 1996
    Date of Patent: March 3, 1998
    Assignee: Nippon Paper Industries Co., Ltd.
    Inventors: Hideki Hayasaka, Toshiyuki Takano, Toshimi Satake
  • Patent number: 5624937
    Abstract: A compound of the formula I in which ##STR1## Z is O or S; R.sup.11 is a halogen atom;R.sup.12 is a halogen atom or a trifluoromethyl group; andX is S, SO, SO.sub.2, O or NH;R.sup.4 is naphthyl, quinolinyl, benzimidazolyl, pyridyl, pyradazinyl, benzoxazolyl or benzothiazolyl, unsubstituted or substituted by one or two substituents selected from a halogen atom, (1-4C)alkyl, (1-4C)alkoxy, nitro, (1-4C)alkoxycarbonyl, halo(1-4C)alkyl, and phenyl;or a pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of amyloid beta-protein production.
    Type: Grant
    Filed: March 2, 1995
    Date of Patent: April 29, 1997
    Assignee: Eli Lilly and Company
    Inventors: Jon K. Reel, Richard L. Simon, Celia A. Whitesitt
  • Patent number: 5567411
    Abstract: Dendritic derivatives of 3,5-bis(aminomethyl)benzene and aminomethyl benzene core groups are disclosed. In each derivative, termed an "amplifier" because the dendritic structure on each molecule terminates with multiple termini to each of which an "active group" can be attached, the desired effect of the active group per mole is amplified compared to conventional compounds having only one active group per molecule. Amplifier molecules can include a targeting group permitting the molecules to preferentially attach to a particular anatomical or physiological situs. Active groups are any of various pharmacologically or therapeutically active moieties, including moieties useful for magnetic-resonance contrast enhancement. The dendritic structures comprise linkers and branch groups covalently bonded to each other in any of various structural combinations. The amplifiers can be prepared as a solution or mixture with a physiologically compatible carrier for administration to a warm-blooded animal subject.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: October 22, 1996
    Assignee: State of Oregon Acting by and Through the State Board of Higher Education on Behalf of the University of Oregon
    Inventors: John F. W. Keana, Vladimir Martin, William H. Ralston
  • Patent number: 5384425
    Abstract: Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## wherein, R.sup.1 and R.sup.2 are the same or different, and each represents C.sup.1 -10 alkyl group, a C.sup.3 -18 cycloalkyl group, or a lower alkyl group substituted by cycloalkyl radical(s);R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and each represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, hydrocarbyl aralkyl group, a pyridyl group, or an unsubstituted or substituted phenyl group, the substituents of the phenyl group being selected from a group consisting of lower alkyl radical, halogen atom-substituted lower alkyl radical, halogen atom, nitro radical, amino radical, mono- or di-lower alkylamino radical, lower acylamino radical, hydroxyl radical, lower alkoxy radical and lower acyloxy radical;X represents an oxygen atom or a sulfur atom, and n.sup.1 and n.sup.2 represent an integer of 1 to 6; and wherein at least one of R.sup.3 -R.sup.
    Type: Grant
    Filed: October 7, 1993
    Date of Patent: January 24, 1995
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
  • Patent number: 5312930
    Abstract: This invention relates to optical elements capable of second harmonic generation and novel compositions for use in such optical elements comprising polar molecules placed in noncentrosymmetric configuration wherein such optical element has an electron donor moiety linked through a conjugated bonding moiety to an electron acceptor moiety which consists of a selected fluorinated sulfone, fluorinated ketone, fluorinated vinyl sulfone or fluorinated alkyl vinyl sulfone.
    Type: Grant
    Filed: December 31, 1992
    Date of Patent: May 17, 1994
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Lap T. Cheng, Andrew E. Feiring, Wilson Tam
  • Patent number: 5264441
    Abstract: The invention provides new ureas and thioureas derivatives of general formula (I) ##STR1## and pharmaceutically acceptable salts thereof, which are useful as therapeutic agents such as for the prevention of coronary heart disease and as antidyslipidaemic agents.
    Type: Grant
    Filed: February 18, 1992
    Date of Patent: November 23, 1993
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Paolo Cozzi, Danielle Fancelli, Dino Severino, Augusto Chiari, Giancarlo Ghiselli
  • Patent number: 5227492
    Abstract: Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## Illustrative derivatives include 1,3-bis[[1-cycloheptyl-3-(3-pyridyl)ureido]-methyl]benzene, 1,3-bis[[1-cycloheptyl-3-(2-pyridyl)ureido]-methyl]benzene, and 1,3-bis[[1-cycloheptyl-3-(4-pyridyl)ureido]-methyl]benzene.The above compounds inhibit acyl-coenzyme A cholesterol acyltransferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.
    Type: Grant
    Filed: June 30, 1992
    Date of Patent: July 13, 1993
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
  • Patent number: 5187197
    Abstract: Novel substituted phenyl-thioureas, -isothioureas and -carbodiimides of formula I ##STR1## in which R.sub.1 is C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkyl mono- or poly-substituted by halogen and/or by C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl mono- or poly-substituted by C.sub.1 -C.sub.3 alkyl, or is C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 C.sub.4 alkyl; each of R.sub.2 and R.sub.3 is C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl or C.sub.5 -C.sub.6 cycloalkenyl; each of R.sub.4 and R.sub.5 is hydrogen or C.sub.1 -C.sub.4 alkyl; each R.sub.6 is halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 C.sub.4 haloalkoxy or a --CH.dbd.CH, --CH.sub.2 or --CH.sub.2 bridge in the 2,3-or 3,4-position; n is 0, 1 or 2; Z is --NH--CS--NH--, --N.dbd.C(SR.sub.7) --NH--or --N.dbd.C.dbd.N--, and R.sub.7 is C.sub.1 -C.sub.10 alkyl or C.sub.3 -C.sub.
    Type: Grant
    Filed: August 20, 1990
    Date of Patent: February 16, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Josef Ehrenfreund
  • Patent number: 5166429
    Abstract: Diurea Derivatives represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A chloresterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.
    Type: Grant
    Filed: September 24, 1991
    Date of Patent: November 24, 1992
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
  • Patent number: 5155127
    Abstract: Novel N-[substituted aryl]-N'-(substituted alkoxy)-urea and thiourea derivatives are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.
    Type: Grant
    Filed: January 18, 1990
    Date of Patent: October 13, 1992
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 5116848
    Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxphenyl-N'-diarylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis with urea and thiourea compounds.
    Type: Grant
    Filed: March 30, 1988
    Date of Patent: May 26, 1992
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 5107021
    Abstract: The invention relates to polyfluoroalkyl nitrogen compounds of general formula:R.sub.F --(CH.sub.2).sub.2 --Xin which X denotes an isothiocynate --N.dbd.C.dbd.S, carbodiimide --N.dbd.C.dbd.N(CH.sub.2).sub.2 --R'.sub.F or thiourea --NH--CS--A group, A denoting an optionally substituted amino group, and each of the symbols R.sub.F and R'.sub.F denotes a perfluoroalkyl radical.These compounds, prepared from the corresponding azides R.sub.F (CH.sub.2).sub.2 N.sub.3 or amines R.sub.F (CH.sub.2).sub.2 NH.sub.2, can be used as surface-active agents or precursors of such agents.
    Type: Grant
    Filed: April 12, 1991
    Date of Patent: April 21, 1992
    Assignee: Societe ATOCHEM
    Inventors: Eric Bollens, Francois Szonyi, Aime Cambon
  • Patent number: 5106873
    Abstract: This invention relates to novel compounds which are ACAT inhibitors rendering them useful in lowering blood cholesterol levels. The compounds contain two urea or thiourea, amide, or amine moieties or combinations of said moieties and have the following general formula: ##STR1## wherein m and n are zero or one, W and YNH and ##STR2## form the urea, thiourea, amide or amine moieties; and R.sub.1 and R .sub.2 are hydrogen or a hydrocarbon radical.
    Type: Grant
    Filed: June 26, 1990
    Date of Patent: April 21, 1992
    Assignee: Warner-Lambert Company
    Inventors: Patrick M. O'Brien, Drago R. Sliskovic, Michael W. Wilson
  • Patent number: 5063247
    Abstract: Novel diphenylurea derivatives represented by the following formula (I): ##STR1## wherein R.sub.1 is an alkyl group of 5 to 18 carbon atoms, each of R.sub.2 and R.sub.3 is independently an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, R.sub.4 is hydrogen atom, an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, and X is oxygen atom or sulfur atom, are provided.The compounds are potent in reducing the cholesterol level in serum, and useful for treating hyperlipemia and atherosclerosis.
    Type: Grant
    Filed: June 13, 1990
    Date of Patent: November 5, 1991
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Tetsuo Sekiya, Shinya Inoue, Masao Taniguchi, Kohei Umezu, Kazuo Suzuki
  • Patent number: 5030653
    Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.
    Type: Grant
    Filed: October 23, 1990
    Date of Patent: July 9, 1991
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 5026910
    Abstract: The invention relates to polyfluoroaklyl nitrogen compounds of general formula:R.sub.F --(CH.sub.2).sub.2 --Xin which X denotes an isothiocyanate --N.dbd.C.dbd.S, carbodiimide --N.dbd.C.dbd.N(CH.sub.2).sub.2 --R'.sub.F or thiourea --NH--CS--A group, A denoting an optionally substituted amino group, and each of the symbols R.sub.F and R'.sub.F denotes a perfluoroalkyl radical.these compounds, prepared from the corresponding axides R.sub.F (CH.sub.2).sub.2 N.sub.3 or amines R.sub.F(CH.sub.2).sub.2 NH.sub.2, can be used as surface-active agents or precursors of such agents.
    Type: Grant
    Filed: May 22, 1990
    Date of Patent: June 25, 1991
    Assignee: Societe Atochem
    Inventors: Eric Bollens, Francois Szonyi, Aime Cambon
  • Patent number: 5015644
    Abstract: Certain substituted urea, thiourea, carbamate, and thiocarbamate compounds are potent inhibitors of the enzyme acyl-CoA: cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol, and for lowering blood plasma cholesterol.
    Type: Grant
    Filed: June 1, 1989
    Date of Patent: May 14, 1991
    Assignee: Warner-Lambert Company
    Inventors: Bruce D. Roth, Bharat K. Trivedi
  • Patent number: 4977170
    Abstract: Novel isoprenoidamine compounds (I) which show antiulcer activity are provided.
    Type: Grant
    Filed: May 3, 1989
    Date of Patent: December 11, 1990
    Assignee: Shionogi & Co., Ltd.
    Inventors: Saichi Matsumoto, Masami Doteuchi, Takuji Mizui, Kentaro Hirai
  • Patent number: 4888043
    Abstract: The invention concerns compounds of the formula I ##STR1## wherein: Z is selected from hydrogen, alkyl, alkanoyl, sulfamoyl, carboxy and trifluoroacetamido;Y is selected from various carboxy or thiocarboxy groups, haloalkanoyl, alkylsulfonyl and haloalkylsulfonyl;R.sup.1 is selected from hydrogen, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl and alkynyl;R.sup.3 is selected from alkyl; andR.sup.4 is selected from hydrogen, alkyl, and alkoxycarbonyl.The compounds of the invention show herbicidal properties and plant growth regulating properties and in further embodiments and the invention provides processes for the preparation of compounds of formula I, intermediates useful in the preparation of the compounds of formula I, compositions containing as active ingredient a compound of formula I, and herbicidal and plant growth regulating processes utilizing compounds of formula I.
    Type: Grant
    Filed: June 20, 1986
    Date of Patent: December 19, 1989
    Assignee: ICI Australia Limited
    Inventors: Keith G. Watson, Craig G. Lovel
  • Patent number: 4877880
    Abstract: A process for the preparation of certain iminothiazolidines of the formula ##STR1## in which R is halo, nitro, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, pentahalomethyl, difluoromethyl, pentafluoroethyl, trifluoromethylthio, difluoromethoxy, trifluoromethoxy, tetrafluoroethoxy, methylsulfonyl, C.sub.1 -C.sub.4 alkyloxyiminomethyl, benzyloxyiminomethyl, 1-(C.sub.1 -C.sub.4)alkyl oxyiminoethyl or 1-benzyloxyiminoethyl; R.sub.1 is hydrogen or halo; R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 haloalkyl; and R.sub.3 and R.sub.4 are independently hydrogen, halo, nitro, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 fluoroalkoxy or C.sub.1 -C.sub.4 alkylthio, by reacting a thiourea with methanesulfonic acid or trifluoromethanesulfonic acid in an aprotic solvent for a period of time and at a temperature sufficient to achieve cyclization of the thiourea to form said iminothiazolidine.
    Type: Grant
    Filed: December 9, 1988
    Date of Patent: October 31, 1989
    Assignee: ICI Americas Inc.
    Inventor: Frank X. Woolard
  • Patent number: 4868210
    Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.
    Type: Grant
    Filed: March 30, 1988
    Date of Patent: September 19, 1989
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 4857556
    Abstract: Substituted benzylcycloalkenylurea derivatives of the formula (I) ##STR1## wherein X represents a halogen atom or a lower alkyl group, Y represents an oxygen atom or a sulfur atom,R.sup.1 represents a cycloalkenyl group andR.sup.2 represents a lower alkyl group, a cycloalkyl group, a benzyl group or a phenyl group optionally substituted by 1 to 5 substituents selected from the group consisting of a hydroxyl group or a lower alkoxy groupand their use as fungicides. They can be synthesized, for example, by reacting of a substituted benzyl-cycloalkenylamine with an isocyanate or by reacting of a carbamoyl halide with an amine. The starting material, the substituted benzyl-cycloalkenyl amines, are also new.
    Type: Grant
    Filed: December 8, 1987
    Date of Patent: August 15, 1989
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Yasuo Yamada, Junichi Saito, Tatsuo Tamura, Shinji Sakawa
  • Patent number: 4855478
    Abstract: An N,N-diaryl-N-alkylurea having the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are selected from the group consisting of hydrogen, halogen, cyano, trifluoromethyl, trifluoromethylthio, trifluoromethyl thionyl, trifluoromethane sulfonyl, sulfonamido, substituted phenoxy and substituted pyridyloxy groups wherein the substituent is any one of halogen, cyano, trifluoromethyl, trifluoromethylthio, trifluoromethyl thionyl, trifluoromethane sulfonyl, sulfonamido; andR.sub.5 is selected from the group consisting of alkyl, alkenyl, haloalkyl, haloalkenyl, hydroxyalkyl, hydroxylalkenyl, acetoxyalkyl, acetoxyalkenyl, mercaptoalkyl, and mercaptoalkenyl, wherein the alkyl or alkenyl group in each alkyl- or alkenyl-containing moiety has from 3 to 6 carbon atoms;X is oxygen or sulfur;and agriculturally acceptable salts thereof.Also disclosed is an herbicidal composition and method of treating weeds.
    Type: Grant
    Filed: November 30, 1987
    Date of Patent: August 8, 1989
    Assignee: ICI Americas Inc.
    Inventor: Frank X. Woolard
  • Patent number: 4564638
    Abstract: Fungicidally active novel benzylurea derivatives of the formula ##STR1## in which R.sup.1 is a halogen atom or a lower alkyl group,X is an oxygen or sulfur atom, andR.sup.2 is an alkyl group, a cycloalkyl group having 5 to 8 carbon atoms, or a phenyl group which may be substituted by at least one member of the class consisting of halogen atoms, lower alkyl groups, lower alkoxy groups and hydroxyl groups.
    Type: Grant
    Filed: June 10, 1983
    Date of Patent: January 14, 1986
    Assignee: Nihon Tokushu Boyaku Seizo K.K.
    Inventors: Yasuo Yamada, Junichi Saito, Tatsuo Tamura, Shinji Sakawa
  • Patent number: 4536341
    Abstract: Dihalo and haloalkyl, haloalkoxy or haloalkylthio-substituted anilines and aniline derivatives, e.g. isocyanates that are useful in the preparation of acyl ureas having insecticidal activity.
    Type: Grant
    Filed: August 3, 1983
    Date of Patent: August 20, 1985
    Assignee: The Dow Chemical Company
    Inventors: Raymond H. Rigterink, Ronald J. Sbragia
  • Patent number: 4518804
    Abstract: Novel N-aroyl N'-phenyl urea compounds having halogen substituents in the 2- and 5-position of the phenyl radical possess exceptional insecticidal activity.
    Type: Grant
    Filed: August 3, 1983
    Date of Patent: May 21, 1985
    Assignee: The Dow Chemical Company
    Inventors: Raymond H. Rigterink, Barat Bisabri-Ershadi
  • Patent number: 4487783
    Abstract: (Thio)-ureas of the formula ##STR1## in which R.sup.1 is an optionally alkyl-substituted cycloalkyl radical or a halogenoalkyl radical,R.sup.2 is an alkyl or cycloalkyl radical or an optionally substituted aryl radical,Ar is an optionally substituted aryl radical, at least one of the radicals R.sup.1, R.sup.2 and Ar carrying fluorine or a fluorine-containing substituent, andX is an oxygen or sulphur atom,which possess fungicidal activity. Novel intermediates are also disclosed.
    Type: Grant
    Filed: August 9, 1982
    Date of Patent: December 11, 1984
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Grohe, Volker Paul
  • Patent number: 4460602
    Abstract: A compound, or pharmaceutically acceptable salt thereof, having the formula: ##STR1## wherein X is O or S; wherein n=1 or 0; wherein R is C.sub.3 -C.sub.12 alkyl or aralkyl, branched or unbranched, aryl or haloaryl, or C.sub.3 -C.sub.22 alkenyl, branched or unbranched; wherein R.sub.1 is OCH.sub.3, and wherein R.sub.2 is OH. These urea derivatives have analgesic and anti-irritant activity when administered to humans and lower animals.
    Type: Grant
    Filed: May 25, 1982
    Date of Patent: July 17, 1984
    Assignee: The Procter & Gamble Company
    Inventors: Brian L. Buckwalter, Thomas R. LaHann
  • Patent number: 4328247
    Abstract: The invention relates to N-phenoxyphenylisothioureas of the formula ##STR1## wherein each R.sub.1, R.sub.2 and R.sub.3 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, trifluoromethyl or nitro, each of R.sub.4 and R.sub.5 is C.sub.2 -C.sub.4 alkyl, R.sub.6 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl or C.sub.3 -C.sub.5 alkynyl, R.sub.7 is C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.5 alkenyl or C.sub.3 -C.sub.6 cycloalkyl, and R.sub.8 is hydrogen or C.sub.1 -C.sub.10 alkyl. The invention further relates to the production of these compounds and their use in pest control, as well as to phenoxyphenylthioureas as intermediates for the production of the N-phenoxyphenylisothioureas of the invention.
    Type: Grant
    Filed: September 8, 1980
    Date of Patent: May 4, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Jozef Drabek, Manfred Boger
  • Patent number: 4289903
    Abstract: There are provided certain p-phenylalkoxy phenylurea and thiourea compounds useful for the control of undesirable plants in the presence of agronomic crops and to methods for the preparation of said phenylalkoxy phenylurea and thiourea compounds.
    Type: Grant
    Filed: June 25, 1979
    Date of Patent: September 15, 1981
    Assignee: American Cyanamid Company
    Inventors: David M. Spatz, Barrington Cross