Alicyclic Ring Containing Patents (Class 564/57)
  • Patent number: 6127575
    Abstract: A process is disclosed for preparing N,N'-disubstituted urea by reacting an amine and CO/O.sub.2 mixture gas in the presence of a catalyst system comprising at least one selenium compound selected from SeO.sub.2, (CH.sub.3 O)Se(O)(OH) and (CH.sub.3 CH.sub.2 O)Se(O)(OH), and M.sub.2 CO.sub.3 (M=alkali metal) as a co-catalyst. The process enables less active aromatic amine with a low reactivity as well as an aliphatic amine to be easily transformed into disubstituted urea avoiding the use of expensive precious metal catalysts.
    Type: Grant
    Filed: September 13, 1999
    Date of Patent: October 3, 2000
    Assignee: Korea Institute of Science and Technology
    Inventors: Hoon Sik Kim, Yong Jin Kim, Hyun Joo Lee, Moon Jo Chung, Sang Deuk Lee
  • Patent number: 6028112
    Abstract: There is provided novel spirocyclopropyl fluorene derivatives having the general Formula I ##STR1## wherein R, R.sup.1 and X are as defined herein which are useful as melatonergic agents.
    Type: Grant
    Filed: July 31, 1998
    Date of Patent: February 22, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Karen L. Leboulluec, Katherine S. Takaki
  • Patent number: 6008410
    Abstract: Aliphatic tetraketimine of the present invention are a novel class of compounds represented by the formula: ##STR1## wherein Et is ethyl, Me is methyl, and R is a residue of an aliphatic diisocyanate. The tetraketimine is made by condensing a novel ketimine with a diisocyanate. The ketimine has a free secondary amine after a polyamine selected from the group consisting of:______________________________________ H2N--C2H4--NH--C2H4--NH2, H2N--C2H4--NH--C2H4--NH--C2H4--NH2, H2N--(CH2)6--NH--(CH2)6--NH2, or tris(2-aminoethyl)amine ______________________________________is reacted with a ketone.
    Type: Grant
    Filed: December 17, 1997
    Date of Patent: December 28, 1999
    Assignee: The Boeing Company
    Inventor: Larry K. Olli
  • Patent number: 5961878
    Abstract: The invention relates to non-crystallising, amine-blocked polyisocyanates, to the preparation thereof and to their in one-component polyurethane stoving compositions, in particular for coil-coating applications.
    Type: Grant
    Filed: September 2, 1998
    Date of Patent: October 5, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Eberhard Konig, Karl-Ludwig Noble, Christian Fussel
  • Patent number: 5932595
    Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.
    Type: Grant
    Filed: December 18, 1996
    Date of Patent: August 3, 1999
    Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.
    Inventors: Steven Lee Bender, Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Lawrence Emerson Fisher, Robert Than Hendricks, Keshab Sarma
  • Patent number: 5912314
    Abstract: A Polyaddition product, containing uretdione groups, which is obtainable by reaction of (A) a diisocyanate mixture which contains uretdione groups and comprises (1) at least 40 mol % to not more than 80 mol % of isophorone diisocyanate containing uretdione groups and (2) not more than 60 mol % and not less than 20 mol % of hexamethylene diisocyanate containing uretdione groups, with (B) a disecondary diamine, in an NCO/NH ratio of 1:0.5 to 1:0.9 at room temperature to 60.degree. C. in a solvent which is inert towards isocyanates.
    Type: Grant
    Filed: March 17, 1997
    Date of Patent: June 15, 1999
    Assignee: Huels Aktiengesellschaft
    Inventor: Elmar Wolf
  • Patent number: 5902899
    Abstract: Process for preparing 1,3-disubstituted urea of the formula: ##STR1## wherein R.sup.5 is the same as or different from R.sup.6, and each of R.sup.5 and R.sup.6 is independently linear or branched, alkyl of 1-20 carbon atoms, alkenyl group having 2 to 20 carbon atoms or alkynyl group having 2 to 20 carbon atoms, which may have phenoxy, alkoxy of 1-13 carbon atoms, monocycloalkyl of 3-8 carbon atoms, bicycloalkyl of 6-12 carbon atoms, aryl of 6-13 carbon atoms, furyl, pyridyl, or aralkyl of 7-20 carbon atoms, comprising reacting cyclic carbonic acid ester with an amine using alkali metal alkoxide or trialkylamine as base, in safety and high yield.
    Type: Grant
    Filed: December 4, 1997
    Date of Patent: May 11, 1999
    Assignee: Sumika Fine Chemicals Co., Ltd.
    Inventors: Taketo Hayashi, Junichi Yasuoka
  • Patent number: 5872294
    Abstract: Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful as phase transfer catalysts and the reaction of alkali metal salts of dihydroxyaromatic compounds with substituted imides to form polyetherimides or their intermediates.
    Type: Grant
    Filed: January 11, 1996
    Date of Patent: February 16, 1999
    Assignee: General Electric Company
    Inventors: Joseph John Caringi, Gary Ray Faler, Peter David Phelps, Thomas Link Guggenheim, Larry Ivis Flowers, Daniel Joseph Brunelle, Roy Ray Odle
  • Patent number: 5840977
    Abstract: A method of producing a pantothenic acid derivative of formula (I): ##STR1## wherein each of R.sup.1 and R .sup.2 is different, and is a branched aliphatic hydrocarbon group having 3 to 5 carbon atoms, or a phenyl group; or a straight chain aliphatic hydrocarbon group having 5 to 10 carbon atoms, is provided, including methods of producing the starting materials for producing the same and novel amine derivative that can be used for the production of the pantothenic acid derivative.
    Type: Grant
    Filed: August 6, 1997
    Date of Patent: November 24, 1998
    Assignee: Fujirebio Inc.
    Inventors: Hiroshi Ikawa, Hajime Matsumoto
  • Patent number: 5783593
    Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: April 29, 1996
    Date of Patent: July 21, 1998
    Assignee: Abbott Laboratories
    Inventors: William R. Baker, Saul H. Rosenberg, Anthony K. L. Fung, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, Stephen J. O'Connor, Rajnandan N. Prasad, Wang Shen, David M. Stout, Gerard M. Sullivan
  • Patent number: 5782966
    Abstract: Resins and waxes made by reacting selected nucleophiles, including alcohols and/or amines, with an isocyanate are disclosed. The order of addition of the isocyanate and the different nucleophiles can tailor the distribution of di-urethane, mixed urethane/urea, and/or di-urea molecules in the final resin product. The isocyanate-derived resin and wax materials are useful as ingredients as phase change ink carrier compositions used to make phase change ink jet inks.
    Type: Grant
    Filed: June 28, 1996
    Date of Patent: July 21, 1998
    Assignee: Tektronix, Inc.
    Inventors: Loc V. Bui, Clifford R. King, Jeffery H. Banning, Donald R. Titterington
  • Patent number: 5739398
    Abstract: A process for preparing N-alkenylureas of the general formula I ##STR1## where R.sup.1 and R.sup.2 are hydrogen, C.sub.1 - to C.sub.40 -alkyl, C.sub.2 - to C.sub.40 -alkenyl, C.sub.3 - to C.sub.20 -cycloalkyl, C.sub.4 - to C.sub.20 -alkylcyc1oalkyl, C.sub.4 - to C.sub.20 -cycloalkylalkyl, aryl, C.sub.7 - to C.sub.20 -alkylaryl or C.sub.7 - to C.sub.20 -aralkyl, or aryl, C.sub.7 - to C.sub.20 -alkylaryl or C.sub.7 - to C.sub.20 -aralkyl which are mono- to pentasubstituted by C.sub.1 - to C.sub.8 -alkyl, C.sub.1 - to C.sub.8 -alkoxy or halogen, together are a C.sub.2 - to C.sub.10 -alkylene chain which is unsubstituted or mono- to hexasubstituted by C.sub.1 - to C.sub.8 -alkyl, andR.sup.3 and R.sup.4 are hydrogen or C.sub.1 - to C.sub.8 -alkyl,by reaction of ureas of the general formula II ##STR2## where R.sup.1 and R.sup.2 have the abovementioned meanings, with an alkenyl carboxylate of the general formula III ##STR3## where R.sup.3 and R.sup.4 have the abovementioned meanings and R.sup.5 is hydrogen, C.sub.
    Type: Grant
    Filed: July 3, 1996
    Date of Patent: April 14, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Jochem Henkelmann, Marc Heider, Thomas Ruhl
  • Patent number: 5681858
    Abstract: The present invention provides a novel N-hydroxyurea compound of chemical formula (I) wherein R.sup.1 and R.sup.2 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl; Ar is phenyl or mono-, di- or trisubstituted phenyl; A is a valence bond or a C.sub.1 -C.sub.6 alkylene chain, optionally having one double bond or one triple bond in the chain, and optionally having one or more C.sub.1 -C.sub.4 alkyl groups attached to the chain: X is oxygen or sulfur, n is an integer of 3 to 6; M is hydrogen, pharmaceutically acceptable cation or a metabolically cleavable group: and X and A may be attached at any available position on the ring. These compounds are useful for treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.
    Type: Grant
    Filed: October 3, 1995
    Date of Patent: October 28, 1997
    Assignee: Pfizer Inc.
    Inventors: Rodney William Stevens, Takashi Mano, Yoshiyuki Okumura, Masami Nakane
  • Patent number: 5648515
    Abstract: Urea- and urethane-containing monomers for contact lens materials are disclosed.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: July 15, 1997
    Assignee: Bausch & Lomb Incorporated
    Inventor: Yu-Chin Lai
  • Patent number: 5648523
    Abstract: The invention relates to fullerene derivatives which are capable of scavenging free radicals. The derivatives have the formula F(--X).sub.m (--Y--Z).sub.n, in which F is a fullerene core; each X is independently --CO.sub.2.sup.-, --SO.sub.3.sup.-, --SH, or the like; each --Y--Z is independently (C.sub.3-30 alkyl ether).sub.50 --CH.sub.2 --CO.sub.2.sup.-, (C.sub.3-30 alkyl ester).sub.50 --CH.sub.2 --SO.sub.3.sup.-, (C.sub.3-30 alkyl amide).sub.50 --CH.sub.2 --SH, or the like; m is 0-30; n is 0-30; and the sum of m and n is 2-30.
    Type: Grant
    Filed: October 26, 1995
    Date of Patent: July 15, 1997
    Inventor: Long Y. Chiang
  • Patent number: 5639908
    Abstract: Urea- and urethane-containing monomers for contact lens materials are disclosed.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: June 17, 1997
    Assignee: Bausch & Lomb Incorporated
    Inventor: Yu-Chin Lai
  • Patent number: 5637769
    Abstract: The present invention provides: a urea-modified carbodiimide represented by the following general formula ##STR1## (wherein each R is a C.sub.1 -C.sub.12 alkyl group or a C.sub.3 -C.sub.10 cycloalkyl group; each Z is a C.sub.1 -C.sub.12 alkylene group, a C.sub.3 -C.sub.10 cycloalkylene group, a C.sub.4 -C.sub.16 alkylene group having a cyclic or non-cyclic structure, or a C.sub.8 -C.sub.16 alkylene group having an aromatic ring; n is an integer of 1-50; and each m is an integer of 1 or 2), and a process for producing the above urea-modified carbodiimide, which comprises (1) reacting an organic aliphatic diisocyanate represented by the following general formulaO.dbd.C.dbd.N--Z--N.dbd.C.dbd.
    Type: Grant
    Filed: June 27, 1995
    Date of Patent: June 10, 1997
    Assignee: Nisshinbo Industries, Inc.
    Inventors: Yasuo Imashiro, Ikuo Takahashi, Naofumi Horie, Takeshi Yamane
  • Patent number: 5620977
    Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 15, 1997
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
  • Patent number: 5614522
    Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: July 24, 1995
    Date of Patent: March 25, 1997
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Kathryn L. Reed
  • Patent number: 5610190
    Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV Protease.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 11, 1997
    Assignee: G. D. Searle & Co.
    Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Ko-Chung Lin, Michael L. Vazquez, Richard A. Mueller, Kathryn L. Reed, Robert M. Heintz, Michael Clare, John N. Freskos, Eric T. Sun
  • Patent number: 5602275
    Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: February 11, 1997
    Assignee: American Cyanamid Company
    Inventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
  • Patent number: 5538997
    Abstract: The invention relates to compounds of formula I ##STR1## wherein the substituents have various significances. They can be prepared by conventional methods, e.g. coupling, substitution, deprotection or protection reactions.They possess interesting pharmacological properties and are thus indicated for use in the treatment of retroviral infections, particularly as HIV proteinase inhibitors.
    Type: Grant
    Filed: January 3, 1994
    Date of Patent: July 23, 1996
    Assignee: Sandoz Ltd.
    Inventors: Andreas Billich, Brigitte Charpiot, Peter Ettmayer, Hubert Gstach, Philipp Lehr, Dieter Scholz
  • Patent number: 5510349
    Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 23, 1996
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Ko-Chung Lin, Michael L. Vazquez, Richard A. Mueller, Kathryn L. Reed, Robert M. Heintz, Michael Clare, John N. Freskos, Eric T. Sun
  • Patent number: 5482947
    Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: November 15, 1993
    Date of Patent: January 9, 1996
    Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Ko-Chung Lin, Michael L. Vazquez, Richard A. Mueller, Kathryn L. Reed, Robert M. Heintz, Michael Clare, John N. Freskos, Eric T. Sun
  • Patent number: 5475027
    Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: November 8, 1993
    Date of Patent: December 12, 1995
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Daniel P. Getman, Ko-Chung Lin, Gary A. DeCrescenzo, Donald J. Rogier, Jr., John N. Freskos
  • Patent number: 5389682
    Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.
    Type: Grant
    Filed: September 13, 1993
    Date of Patent: February 14, 1995
    Assignee: Warner-Lambert Company
    Inventors: Bradley D. Tait, Michael W. Wilson
  • 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: 5312831
    Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.
    Type: Grant
    Filed: May 12, 1993
    Date of Patent: May 17, 1994
    Assignee: American Cyanamid Company
    Inventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
  • Patent number: 5294582
    Abstract: As a curing catalyst of epoxy resins, superacid salts of an N,N'-di- or N,N',N'-trisubstitued urea, the urea component of which is produced by reacting an organic isocyanate and a primary or secondary amine, at least one of which is monofunctional, are soluble in conventional organic solvents compatible with epoxy resins and catalyze the cationic polymerization reaction of epoxy resins at room temperature.
    Type: Grant
    Filed: June 14, 1993
    Date of Patent: March 15, 1994
    Assignee: Nippon Paint Co., Ltd.
    Inventors: Tadafumi Miyazono, Koji Tabuchi
  • Patent number: 5248755
    Abstract: Process for the preparation of asymmetrically substituted ureas, carbamates, thiocarbamates or substituted isocyanates by reaction of an adduct of isocyanic acid and a tertiary amine with a primary and secondary amine, an alcohol, a thiol or a compound having one or two non-cumulated olefinic double bonds, and a process for the preparation of N-mono- or N,N-disubstituted ureas by reaction of ammonium isocyanate with a primary or secondary amine in a diluent.
    Type: Grant
    Filed: October 9, 1992
    Date of Patent: September 28, 1993
    Assignee: Chemie Linz Gesellschaft m.b.H.
    Inventors: Martin Muller, Gerhard Stern, Erich Schulz, Markus Rossler
  • Patent number: 5231216
    Abstract: There are described novel trans-2-acylaminocyclohexyloxyacyldipeptides of formula I ##STR1## wherein R.sub.1 represents --CO--R.sub.6, --SO.sub.2 --R.sub.7 or ##STR2## R.sub.6 is C.sub.1 -C.sub.18 alkyl or C.sub.1 -C.sub.18 alkoxy, R.sub.7 is C.sub.1 -C.sub.18 alkyl or an optionally substituted phenyl group,Y is .dbd.O, .dbd.S or .dbd.NH;R.sub.2 =R.sub.3 and represent --H or C.sub.1 -C.sub.12 alkyl,R.sub.4 represents --OR.sub.8 or --NHR.sub.9,R.sub.8 is --H, C.sub.1 -C.sub.8 alkyl or benzyl,R.sub.9 is --H, a straight or branched chain C.sub.1 -C.sub.18 alkyl group or benzyl group;R.sub.5 represents --OR.sub.9 or --NHR.sub.9,and novel (1R,2R)- and (1S,2S)-trans-2-acylaminocyclohexyloxyacetyldipeptides of the formulas Ia and Ib ##STR3## wherein R.sub.1 is --CO--R.sub.6, R.sub.6 is C.sub.1 -C.sub.18 alkyl,R.sub.2 is --H,R.sub.3 is --H or C.sub.1 -C.sub.12 alkyl,R.sub.4 is --OR.sub.8 or --NHR.sub.9,R.sub.8 is --H, C.sub.1 -C.sub.8 alkyl or benzyl,R.sub.9 is --H, C.sub.1 -C.sub.18 alkyl or benzyl,R.sub.5 is --OR.
    Type: Grant
    Filed: August 19, 1991
    Date of Patent: July 27, 1993
    Assignee: Univerza Edvarda Kardelja v Ljubljana
    Inventors: Slavko Pecar, Danijel Kikelj, Uros Urleb, Marija Sollner, Gasper Marc, Ales Krbavcic, Vlado Kotnik, Branka Wraber-Herzog, Sasa Simcie, Alojz Than, Lidija Klamfer, Lucka Povsic, Zdravko Kopitar, Anton Stalc
  • Patent number: 5227401
    Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.
    Type: Grant
    Filed: October 29, 1991
    Date of Patent: July 13, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • 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: 5223535
    Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R.sub.5 and R.sub.8 is independently propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.
    Type: Grant
    Filed: October 29, 1991
    Date of Patent: June 29, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5169954
    Abstract: Process for the N-alkylation of ureas by reacting a urea with an alkylating agent in the presence of a solid base and a phase transfer catalyst in a diluent.
    Type: Grant
    Filed: December 16, 1991
    Date of Patent: December 8, 1992
    Assignee: Chemie Linz Gesellschaft m.b.H.
    Inventors: Kurt A. Hackl, Heinz Falk
  • 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: 5124451
    Abstract: Process for the N-alkylation of ureas by reacting a urea with an alkylating agent in the presence of a solid base and a phase transfer catalyst in a diluent.
    Type: Grant
    Filed: July 10, 1991
    Date of Patent: June 23, 1992
    Assignee: Chemie Linz Gesellschaft m.b.H.
    Inventors: Kurt A. Hackl, Heinz Falk
  • Patent number: 5091419
    Abstract: Diurea derivatives are provided which are represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A cholesterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester on the smooth muscle of arterial wall in the blood vessels.
    Type: Grant
    Filed: October 2, 1990
    Date of Patent: February 25, 1992
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
  • Patent number: 5081294
    Abstract: There are disclosed quaternary ammonium salts which are obtainable by reacting basic carbamides containing a quaternisable nitrogen atom with epihalohydrins.These quaternary ammonium salts are particularly suitable for enhancing the color yield and the wet fastness properties of dyeings or printings produced on cellulosic fibre materials with anionic dye, e.g. reactive or direct dyes.
    Type: Grant
    Filed: March 21, 1989
    Date of Patent: January 14, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Rosemarie Topfl, Jorg Binz
  • Patent number: 5055582
    Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.
    Type: Grant
    Filed: December 13, 1988
    Date of Patent: October 8, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert B. Garland, Masateru Miyano
  • Patent number: 5043444
    Abstract: Process for the preparation of asymmetrically substituted ureas by reaction of a gaseous mixture of isocyanic acid and ammonia having a temperature of 260.degree. to 600.degree. C. with a primary or secondary amine.
    Type: Grant
    Filed: July 12, 1990
    Date of Patent: August 27, 1991
    Assignee: Chemie Linz Gesellschaft m.b.H.
    Inventors: Martin Mullner, Gerhard Stern, Markus Rossler
  • Patent number: 4988688
    Abstract: 4-(N-Substituted amino)-2-butynyl-1-ureas and thioureas and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.
    Type: Grant
    Filed: August 2, 1989
    Date of Patent: January 29, 1991
    Assignee: Warner-Lambert Company
    Inventors: Jeffrey A. Kester, Walter H. Moos, Anthony J. Thomas
  • Patent number: 4983630
    Abstract: There are provided new 2,2-difluorocyclopropylethane derivatives of general formula I ##STR1## in which A, B and R.sup.1-5 have the meanings given in the description and processes for their preparation. The compounds of the invention can be used as pesticides, especially against insects and mites.
    Type: Grant
    Filed: November 28, 1988
    Date of Patent: January 8, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Peter Wegner, Hartmut Joppien, Gunter Homberger, Arnim Kohn
  • Patent number: 4970306
    Abstract: The invention relates to trans-cyclohexane-1,4-diisocyanate which is completely or partially blocked with epsilon-caprolactam and a method of manufacturing the same wherein 1 mole trans-cyclohexane-1,4-diisocyanate is reacted with 1 to 2 moles epsilon-caprolactam, without or with the presence of solvents. These blocked diisocyanates are used for polyurethane powders.
    Type: Grant
    Filed: December 9, 1988
    Date of Patent: November 13, 1990
    Assignee: Huels Aktiengesellschaft
    Inventors: Rainer Gras, Elmar Wolf
  • Patent number: 4906774
    Abstract: Polyoxyalkylene diamine reaction products which contain as the principle reaction component, a diamine having the formula: ##STR1## wherein R' independently represents hydrogen or methyl and x is a number having an average value of at least 1 to about 60 and a diisocyanate of the formula: ##STR2## The products of the invention are obtained by reacting an excess of polyoxyalkylene diamine with a diisocyanate in the presence of a polar solvent and have the following general structures: ##STR3## where B is alkyl group from diisocyanates, and R' has the same meaning as above.These products are further used to prepare coatings with improved properties by reacting said amine products with isocyanates prepolymers and epoxy material.
    Type: Grant
    Filed: July 27, 1987
    Date of Patent: March 6, 1990
    Assignee: Texaco Inc.
    Inventors: George P. Speranza, Jiang-Jen Lin, Michael Cuscurida
  • Patent number: 4902825
    Abstract: The present invention relates to N,N'-bis-(4-isocyanatocyclohexyl)urea obtained from the reaction with water of cyclohexane-1,4-diisocyanate having a high trans isomer content. This invention further relates to the process for preparing the N,N'-bis(4-isocyanatocyclohexyl)urea and to its use in the synthesis of polyurethanes.
    Type: Grant
    Filed: October 11, 1988
    Date of Patent: February 20, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Andreas Ruckes, Werner Rasshofer, Richard Kopp, Gerhard Grogler
  • Patent number: 4872902
    Abstract: The invention relates to the novel cyclohexanediones of formula I ##STR1## in which R is hydrogen or C.sub.1 -C.sub.6 -alkyl,A is R.sub.2, OR.sub.3 or NR.sub.3 R.sub.4,R.sub.2 is C.sub.1 -C.sub.6 -alkyl that is unsubstituted or is mono-substituted by C.sub.1 -C.sub.4 -alkoxy or mono- or poly-substituted by halogen, or is C.sub.3 -C.sub.6 -cycloalkyl,R.sub.3 is C.sub.1 -C.sub.6 -alkyl or C.sub.3 -C.sub.6 -cycloalkyl, or is phenyl or benzyl each of which is unsubstituted or is mono-, di- or tri-substituted by R.sub.5,R.sub.4 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.3 -C.sub.6 -cycloalkyl,R.sub.3 and R.sub.4 are, in addition, together with the nitrogen atom to which they are bonded, a pyrrolidine, morpholine or piperidine radical,B is one of the radicals ##STR2## m is 0, 1, 2 or 3, R.sub.5 is halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkylsulphinyl or C.sub.1 -C.sub.
    Type: Grant
    Filed: February 8, 1988
    Date of Patent: October 10, 1989
    Assignee: Ciba-Geigy Corporation
    Inventor: Hans-Georg Brunner
  • Patent number: 4837234
    Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.
    Type: Grant
    Filed: July 22, 1986
    Date of Patent: June 6, 1989
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 4788287
    Abstract: A high performance water and oil repellant composed of a compound comprising at least two terminal segments and an intermediate segment connecting the terminal segments and having a molecular weight of from 800 to 20,000, each terminal segment containing at least one polyfluoroalkyl group connected by a --CONH-- linking group, said intermediate segment being a urethane oligomer containing at least two --CONH-- linking groups in one molecule, and said terminal segments and intermediate segment being connected by a --CONH-- linking group.
    Type: Grant
    Filed: September 3, 1986
    Date of Patent: November 29, 1988
    Assignee: Asahi Glass Company Ltd.
    Inventors: Masashi Matsuo, Masayuki Tamura, Katsuji Ito
  • Patent number: 4762949
    Abstract: Synthetically produced substantially pure biologically active compounds having the general formula ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.20 alkyl, alkenyl, aryl, aralkyl, cycloalkyl, alkylcycloalkyl, cycloalkylalkyl, cycloalkenyl, alkylcycloalkenyl, or cycloalkenylalkyl;R.sub.2 is hydrogen, C.sub.1 -C.sub.10 alkyl or an amide-substituted alkyl having up to 10 carbon atoms;R.sub.3 is a cyclic, straight or branched chain hydrocarbon group having 2-12 carbon atoms, particularly --(CH.sub.2).sub.n --, wherein n is 2-12; orR.sub.2 and R.sub.3 are linked together to form an alkylene chain; andR.sub.4 is selected from ##STR2## (substituted or unsubstituted carbamimidoyl), ##STR3## (dimethylpyrimidyl), or ##STR4## (carbamyl) wherein each of R.sub.5, R.sub.6, and R.sub.7 is hydrogen or the same or different C.sub.1 -C.sub.8 alkyl group. The compounds are useful as bactericides for a wide variety of bacteria, including S.pyogenes, B.subtilis, K.pneumoniae, M.avium, B.fragilis, C.perfringens and C.albicans.
    Type: Grant
    Filed: January 24, 1983
    Date of Patent: August 9, 1988
    Assignee: University of Illinois Foundation
    Inventors: Kenneth L. Rinehart, Jr., Guy T. Carter, Michael T. Cheng