Six-membered Hetero Ring Consists Of Oxygen, Sulfur, Nitrogen And Carbon (e.g., Oxathiazines, Etc.) Patents (Class 544/2)
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Patent number: 5874382Abstract: Compounds of Formula I and II, and their agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein X is a direct bond; O; S; NH; N(C.sub.1 -C.sub.3 alkyl); N(C.sub.1 -C.sub.3 haloalkyl); or N(allyl);R.sup.1 is H; F; Cl; or Br;R.sup.2 is H; F; Cl; Br; CF.sub.3 ; nitro; or cyano;R.sup.4 is H; C.sub.1 -C.sub.3 alkyl; or halogen;R.sup.5 is H; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl; halogen; S(O).sub.2 (C.sub.1 -C.sub.6 alkyl); or C(.dbd.O)R.sup.8 ; orR.sup.4 and R.sup.5 are taken together along with the carbon to which they are attached to form a spiro-cyclopropane ring;and R.sup.3, R.sup.8, and J are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formulae I and II and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I or II.Type: GrantFiled: January 23, 1998Date of Patent: February 23, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Balreddy Kamireddy, William Mark Murray
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Patent number: 5824677Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5780465Abstract: 4-Substituted 5-polycyclylpyrimidine compounds in which the 5-substituent is polycyclic and is attached to the pyrimidine moiety through an aliphatic carbon atom, such as 5-(2,2-dimethylindan-1-yl)-4-methylthiopyrimidine, were prepared and found to possess excellent herbicidal activity. The compounds are especially useful for the control of undesirable vegetation in paddy rice.Type: GrantFiled: April 3, 1997Date of Patent: July 14, 1998Assignee: Dow AgroSciences LLCInventors: Lowell D. Markley, Kim E. Arndt, Patricia G. Ray, Terry W. Balko, Erik N. K. Cressman, David G. Ouse, Johnny L. Jackson, Jacob Secor
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Patent number: 5777110Abstract: The present invention provides certain 3-aryl-5,6-dihydro-1,4,2-ocathiazines and their oxides, useful for the long-term preservation of wood and composite wood materials against wood damaging and wood destroying materials. The present invention also provides compositions containing these 3-aryl-5,6-dihydro-1,4,2-oxathiazines and their oxides, and a suitable vehicle therefor. A method of preserving wood is also disclosed in which a fungicidally or bactericidally effective amount of the present 3-aryl-5,6-dihydro-1,4,2-oxathiazines and their oxides, are applied to the wood substrate to be protected.Type: GrantFiled: August 24, 1994Date of Patent: July 7, 1998Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd./LteeInventors: Robert Allan Davis, Alex R. A. Valcke, Walter Gerhard Brouwer
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Patent number: 5744010Abstract: The invention relates to a process for the preparation of acesulfam salts by reaction of salts of amidosulfonic acid with diketene to give a salt of acetoacetamidosulfonic acid (I), ring closure by the action of at least about an equivalent amount of SO.sub.3, at least this ring closure reaction being carried out in the presence of a halogenated, aliphatic hydrocarbon as an inert solvent, treatment of the cyclization product with water and conversion of the resulting acesulfam-H (II) into the form of a non-toxic salt, which comprises, in the work-up by distillation of the resulting crude solvent, after removal of water and low-boilers and recovery of solvent sufficiently pure for reuse in the preparation of compounds (I) and/or (II), directly returning :he remaining, solvent-containing distillation residue, without further purification, into the system downstream of the reaction vessel for carrying out the ring closure reaction.Type: GrantFiled: June 19, 1995Date of Patent: April 28, 1998Assignee: Hoechst AktiengesellschaftInventors: Gunter Roscher, Heinz Litterer, Axel Engelmann, Wolf-Dietmar Kaufmann, Bernd Laugwitz, Hans-Dietmar Schnabel
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Patent number: 5696154Abstract: Provided are brefeldin A derivatives of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is H and the other of R.sub.1 and R.sub.2 is a substituent group having 1 to 12 carbon atoms containing a basic nitrogen atom or a quaternary ammonium group, or a salt thereof. These derivatives exhibit good antitumor activity, and are administrable to human patients without the problems associated with brefeldin A.Type: GrantFiled: June 29, 1994Date of Patent: December 9, 1997Assignees: The United States of America as represented by the Department of Health and Human Services, Starks Associates, Inc.Inventors: Louis Malspeis, B. Rao Vishnuvajjala, Jeffrey G. Supko, Charles Theodore Kane, Jr.
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Patent number: 5688809Abstract: The present invention relates to compounds of the formula ##STR1## The present invention also relates to intermediates for the preparation of compounds of the formula I, pharmaceutical compositions and method of use.Type: GrantFiled: October 7, 1996Date of Patent: November 18, 1997Assignee: Pfizer Inc.Inventor: John E. Macor
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Patent number: 5641783Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: September 8, 1994Date of Patent: June 24, 1997Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5624981Abstract: Polyalkylpiperidine-containing acetic acid and 3-aminoacrylic acid derivatives I ##STR1## where R.sup.1 is hydrogen, C.sub.1 - to C.sub.6 -alkyl, formyl, C.sub.2 - to C.sub.6 -alkanoyl, C.sub.1 - to C.sub.12 -alkoxy, C.sub.5 - to C.sub.6 -cycloalkoxy, cyanomethyl, hydroxymethyl, 2-hydroxyethyl or a radical of the formula --CR.sup.3 =CH--CO--OR.sup.4, whereR.sup.3 is hydrogen, C.sub.1 -to C.sub.6 -alkyl or a radical of the formula --CO--OR.sup.4 andR.sup.4 is C.sub.1 - to C.sub.20 -alkyl, C.sub.5 - to C.sub.8 -cycloalkyl, C.sub.7 - to C.sub.18 -aralkyl, phenyl, tolyl or a radical of the formula --(CH.sub.2 CH.sub.2 O).sub.n H or --[CH(CH.sub.3)CH.sub.2 O].sub.n H, where n is a number from 1 to 30,X is O, NH or NR.sup.6, whereR.sup.6 is C.sub.1 - to C.sub.12 -alkyl, andY is hydrogen or a group of the formula =CH--NHR.sup.7 or =CH--NR.sup.6 R.sup.7, whereR.sup.7 is phenyl which can be substituted by one to three C.sub.1 - to C.sub.12 -alkyl, C.sub.1 - to C.sub.Type: GrantFiled: October 7, 1994Date of Patent: April 29, 1997Assignee: BASF AktiengesellschaftInventors: Martin Holderbaum, Alexander Aumueller, Hubert Trauth
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Patent number: 5614626Abstract: The invention relates to compounds of the formula (I) ##STR1## which R is hydrogen or (C.sub.1 -C.sub.4)-alkyl, to a process for their preparation and to their use as electrophilic fluorinating agents.Type: GrantFiled: July 11, 1995Date of Patent: March 25, 1997Assignee: Hoechst AGInventors: Ivan Cabrera, Wolfgang Appel
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Patent number: 5571773Abstract: There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.Type: GrantFiled: June 2, 1995Date of Patent: November 5, 1996Assignee: American Cyanamid CompanyInventors: Barrington Cross, Marinus Los, Robert F. Doehner, Jr., David W. Ladner, Jerry L. Johnson
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Patent number: 5532228Abstract: The invention discloses side-chain homologous vitamin D derivatives of formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, B, and D have the meanings defined in the specification and either (1) A is a direct bond between carbon atoms 20 and 22 and X is an oxy alkylene radical, --(CH.sub.2).sub.n O-- where n is 1 to 3; (2) A is a methylene bridge, --CH.sub.2 --, between carbon atoms 20 and 22 and X is either an alkylene radical, --(CH.sub.2).sub.n -- or an oxy alkylene radical, --(CH.sub.2).sub.n O--, where n is 1 to 3; or (3) if A is a direct bond and B and D together form a second bond, then X(R.sup.5) (R.sup.6) is ##STR2## The compounds possess proliferation-inhibiting and cell-differentiating activity.Type: GrantFiled: June 1, 1993Date of Patent: July 2, 1996Assignee: Schering AktiengesellschaftInventors: Gunter Neef, Gerald Kirsch, Andreas Stein-Eyer, Katica Schwarz, Matthias Brautigam, Ruth Thieroff-Ekerdt, Petra Rach
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Patent number: 5525729Abstract: The invention relates to compounds of the formula (I) ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, independently of one another, hydrogen, CF.sub.3, NO.sub.2, CN, halogen, --S(NSO.sub.2 CF.sub.3)CF.sub.3, (C.sub.1 -C.sub.4)-alkyl, phenyl, SO.sub.2 R.sup.5, COOR.sup.5, NR.sub.2.sup.5, where R.sup.5 is (C.sub.1 -C.sub.4)-alkyl, which can also be fluorinated, or phenyl, or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3 or R.sup.3 and R.sup.4 together form an aliphatic or aromatic ring which can also contain an oxygen, sulfur or nitrogen atom.The invention further provides a process for preparing the compounds of the formula (I), which comprises reacting compounds of the formula (II) ##STR2## where R.sup.1 to R.sup.4 are as defined above and X is hydrogen or an alkali metal, with elemental fluorine in the presence of an inert solvent and, if desired, an alkali metal fluoride at low temperatures.Type: GrantFiled: March 13, 1995Date of Patent: June 11, 1996Assignee: Hoechst AktiengesellschaftInventors: Ivan Cabrera, Wolfgang Appel
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Patent number: 5478934Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.Type: GrantFiled: November 23, 1994Date of Patent: December 26, 1995Inventors: Jun Yuan, Jan W. F. Wasley
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Patent number: 5463052Abstract: A selective and high-yield method is described for producing stereoisomeric benzylidene derivatives of the formula III: ##STR1## wherein R.sup.1 and R.sup.2 each independently is lower alkyl, lower alkoxy or halogen; Y is SO.sub.2, SO or CO; --A-- is optionally substituted lower alkylene; --B-- is --CH.sub.2 -- or --O--; or --A-- and --B-- taken together may form optionally substituted phenylene or optionally substituted lower alkenylene; and R is hydrogen, optionally substituted lower alkyl, cycloalkyl, lower alkoxy, hydroxy, optionally substituted aryl, optionally substituted arylalkyl; optionally substituted arylalkyloxy, heterocyclic ring or N-protecting groups, which comprises reacting a compound of the formula I: ##STR2## wherein R.sup.1 and R.sup.2 are as defined above and X is lower alkoxy or halogen with a compound of the formula II: ##STR3## wherein Y, --A--, --B-- and R are as defined above in the presence of a base.Type: GrantFiled: May 20, 1994Date of Patent: October 31, 1995Assignee: Shionogi & Co., Ltd.Inventors: Nobuhiro Haga, Masanao Inagaki, Saichi Matsumoto, Susumu Kamata
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Patent number: 5418230Abstract: Benzylidene derivatives having anti-inflammatory activities, are shown by the following formula I: ##STR1## wherein A is -CH.sub.2 - or -CH.sub.2 CH.sub.2 -; B is a bond or -CH.sub.2 -, -CHOH-, -CO-, -O-, or A and B may taken together form -CH=CH-; D is >N- or >CH-; R.sup.1 and R.sup.2 each independently is hydrogen, lower alkyl or lower alkoxy; R.sup.3 is hydrogen, lower alkyl, cycloalkyl, lower alkoxy, arylalkyloxy, heteroarylalkyloxy, lower alkylcarbonyl, arylcarbonyl, substituted or unsubstituted carbamoyl, or a group of the formula:-(CH.sub.2).sub.n -R.sup.4wherein R.sup.4 is hydrogen, hydroxy, substituted or unsubstituted amino, aryl, heteroaryl, hydroxycarbonyl or lower alkyloxycarbonyl; n is an integer of 0-3.Type: GrantFiled: October 28, 1993Date of Patent: May 23, 1995Assignee: Shionogi & Co., Ltd.Inventors: Saichi Matsumoto, Tatsuo Tsuri, Masanao Inagaki, Hirokuni Jyoyama
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Patent number: 5356862Abstract: The invention relates to herbicidal sulfonylurea compounds, agriculturally suitable compositions thereof and a method for their use as general or selective preemergent or postemergent herbicides or plant growth regulants.Type: GrantFiled: July 22, 1992Date of Patent: October 18, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventor: William T. Zimmerman
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Patent number: 5330987Abstract: Novel substituted pyridopyrimidinones of formula (I), which are useful as angiotensin II antagonists, are disclosed.Type: GrantFiled: June 4, 1992Date of Patent: July 19, 1994Assignee: Merck & Co., Inc.Inventors: Eric E. Allen, Prasun K. Chakravarty, Stephen E. de Laszlo, William J. Greenlee, Arthur A. Patchett, Thomas F. Walsh
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Patent number: 5283355Abstract: Compounds of the Formula (5) and processes for their preparation and use, particularly in the manufacture of unsymmetrical triphenodioxazine dyes: ##STR1## wherein: Y is H, alkyl, substituted alkyl, alkoxy, Cl or Br;R is a group of Formula (3) ##STR2## R.sup.1 and R.sup.2 are each independently alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form an optionally substituted 4, 5 or 6 membered alicyclic or heterocyclic ring;R.sup.3 is H;Z is Cl, Br or A--NH; andA is H or the residue of a primary amine.Type: GrantFiled: October 22, 1991Date of Patent: February 1, 1994Assignee: Imperial Chemical Industries PLCInventor: William J. E. Norris
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Patent number: 5281614Abstract: Novel substituted triazolinone, triazolinethione, and triazolinimine compounds of the formula I are useful as angiotensin II antagonists.Type: GrantFiled: November 2, 1992Date of Patent: January 25, 1994Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Prasun K. Chakravarty, Linda L. Chang, William J. Greenlee, Dooseop Kim, Nathan B. Mantlo, Arthur A. Patchett
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Patent number: 5260285Abstract: Novel substituted imidazopyridazines of formula (I) which are useful as angiotensin II antagonists, are disclosed.Type: GrantFiled: November 25, 1991Date of Patent: November 9, 1993Assignee: Merck & Co., Inc.Inventors: Eric E. Allen, William J. Greenlee, Prasun K. Chakravarty, Malcolm MacCoss, Arthur A. Patchett, Thomas F. Walsh
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Patent number: 5250521Abstract: Novel substituted pyrazolopyrimidines of formula (I) which are useful as angiotensin II antagonists, are disclosed.Type: GrantFiled: November 25, 1991Date of Patent: October 5, 1993Assignee: Merck & Co., Inc.Inventors: Eric E. Allen, William J. Greenlee, Prasun K. Chakravarty, Malcolm MacCoss, Arthur A. Patchett, Thomas F. Walsh
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Patent number: 5223501Abstract: Novel substituted fused pyrimidinones of formula (I) are useful as angiotensin II antagonists.Type: GrantFiled: May 10, 1991Date of Patent: June 29, 1993Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Nathan B. Mantlo, William J. Greenlee, Arthur A. Patchett, Dooseop Kim
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Patent number: 5212301Abstract: Introduction of a fluoro substituent into an aromatic ring adjacent an electron donating group is difficult producing mixed isomers and low yields of desired products.A process for the introduction of a fluoro substituent into a substantially adjacent position to an electron-donating group into an aromatic compound in high yield is disclosed.The fluoroaromatic compounds are useful as synthetic intermediates for example in the manufacture of agrochemicals, pharmaceuticals and dyestuffs.Type: GrantFiled: May 8, 1992Date of Patent: May 18, 1993Assignee: Imperial Chemical Industries PLCInventors: John S. Moilliet, Richard D. Chambers, Michael H. Rock
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Patent number: 5162340Abstract: Substituted 1-(2H)-isoquinolinones of the structural formula: ##STR1## are angiotensin II antagonists which are useful in the treatment of hypertension and congestive heart failure.Type: GrantFiled: May 10, 1991Date of Patent: November 10, 1992Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Dooseop Kim
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Patent number: 5158959Abstract: What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.Type: GrantFiled: December 27, 1983Date of Patent: October 27, 1992Assignee: Hoechst AktiengesellschaftInventors: Rolf Geiger, Volker Teetz, Hansjorg Urbach, Bernward Scholkens, Rainer Henning
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Patent number: 5106840Abstract: The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## wherein R.sub.1 is lower alkyl or alkoxy, halogen, trifluoromethyl, lower alkylthio, hydroxy, amino, lower mono- or dialkyl- or acylamino.n has the value 0, 1 or 2,R.sub.2 is hydrogen, lower alkyl or acyl,R.sub.3 is hydrogen, lower alkyl or alkoxycarbonyl, or a phenyl group optionally substituted with a group R.sub.Type: GrantFiled: June 5, 1990Date of Patent: April 21, 1992Assignee: Duphar International Research B.V.Inventors: Peter H. H. Hermkens, Jan H. Van Maarseveen, Johan W. Scheeren, Cornelis G. Kruse
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Patent number: 5097027Abstract: Heterocyclic compounds of the formula ##STR1## are used as pigments for surface coatings and for coloring and pigmenting high molecular weight organic material.Type: GrantFiled: October 5, 1990Date of Patent: March 17, 1992Assignee: Bayer AktiengesellschaftInventor: Hans Hochstetter
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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Patent number: 5001115Abstract: Prodrugs of bio-active hydroxyaromatic drugs having the structural formula:A pharmaceutically acceptable prodrug of a biologically active, therapeutically effective hydroxyaromatic drug, said prodrug being selected from the group consisting of, (A) compounds having the structural formula:DRUG--O--CR'R"--Z].sub.nwherein:DRUG --O-- is the hydroxyaromatic O-dehydro residue of said drug;R' and R' may be the same or different and may be H, alkyl, aryl or electron withdrawing groups;Z is a displaceable leaving group; andn is an integer in the range of from 1 to 3, and (B) pharmaceutically acceptable salts thereof.Type: GrantFiled: May 17, 1989Date of Patent: March 19, 1991Assignee: University of FloridaInventor: Kenneth B. Sloan
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Patent number: 4996316Abstract: A process for the preparation of tertiary N,N-dimethylamines by the reaction of primary amines, formaldehyde, and hydrogen under pressure and at elevated temperature in the presence of a nickel-containing hydrogenation catalyst in the liquid phase. The hydrogenation catalyst is suspended in a solvent, the nickel concentration is 0.1 to 10% by weight, based on the primary amine. The starting materials are separate from each other, brought to 80.degree. to 150.degree. C. and 1 to 15 MPa and fed into the catalyst suspension simultaneously with stirring and reacted in one step to form the tertiary N,N-dimethylamines.Type: GrantFiled: December 24, 1988Date of Patent: February 26, 1991Assignee: Hoechst AktiengesellschaftInventors: Jurgen Weber, Detlef Kampmann, Claus Kniep
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Patent number: 4968676Abstract: Cyclohexylamines of the formula ##STR1## where X is a single bond or an alkylene chain, Y is hydrogen or an aryl, cyclohexyl, 4-cyclohexylcyclohexyl, perhydro-1- or 2-naphthyl or piperidyl radical, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, cycloalkyl, cycloalkenyl or arylalkyl, or R.sup.1 and R.sup.2 together form an alkylene group and, together with the N atom, form a ring, and acid addition salts thereof, with the exception of compounds in which X is a single bond, Y is cyclohexyl, R.sup.1 and R.sup.2 are hydrogen or methyl, and the compounds in which X is C.sub.6 -, C.sub.7 - and C.sub.8 -alkyl, Y is hydrogen and R.sup.1 and R.sup.2 together with the N atom whose substituents they are form a 2,6-dimethylmorpholine radical, and fungicides containing such cyclohexylamines.Type: GrantFiled: September 20, 1989Date of Patent: November 6, 1990Assignee: BASF AktiengesellschaftInventors: Bernhard Zipperer, Ernst Buschmannm, Norbert Goetz, Ulrich Schirmer, Eberhard Ammermann, Ernst-Heinrich Pommer
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Patent number: 4954509Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4 -12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group; R.sub.4 and R.sub.5, which may be the same or different and may be attached to the same or different carbon atoms of the isoquinoline nucleus, are each hydrogen, halogen, hydroxy, C.sub.1-6 alkyl, aryl, or R.sub.4 together with R.sub.5 form a --(CH.sub.2).sub.p -- group, where p is an integer of from 1 to 5 and one or more of the --(CH.sub.2)-- moieties is optionally substituted by a C.Type: GrantFiled: February 17, 1989Date of Patent: September 4, 1990Assignee: Dr. Lo. Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Giuseppe Giardina
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Patent number: 4939251Abstract: Novel 1-azaspiro[4.4] lactams are produced by reaction of at least one hydroxy-containing primary amino compound with a 4-ketodiacid compound or a 1,6-dioxaspiro[4.4]lactone. Molar excesses of amion compound result in production of spirodilactams, while limited molar quantities of amino compound results in production of a spirolactam-lactone which reacts further with hydroxy-containing primary amino compound or with hydroxy-free primary amino compound to produce a spirodilactam. Certain of the spirolactams are useful as precursors for glycidyloxy derivatives which react with epoxy curing agents to form insoluble thermoset resins while others are useful as curing agents and yet others are converted to glycidyloxy derivatives useful as reactive diluents in epoxy resin applications.Type: GrantFiled: September 16, 1988Date of Patent: July 3, 1990Assignee: Shell Oil CompanyInventor: Pen C. Wang
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Patent number: 4895942Abstract: Novel epoxyalkoxy-containing [4.4] spirodilactams having ring nitrogen atoms in the 1- and the 6- ring positions and having a substituent on each ring nitrogen atom, at least one of which substituents contains an epoxyalkyl moiety. Such epoxy compounds are produced by reaction of a 1-halo-2,3-epoxyalkane and the corresponding hydroxy-containing spirodilactam followed by treatment with strong base.Type: GrantFiled: September 16, 1988Date of Patent: January 23, 1990Assignee: Shell Oil CompanyInventor: Pen C. Wang
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Patent number: 4877789Abstract: Compound, corresponding to the formulaC.sub.8 H.sub.17 --(C.tbd.C--CH.sub.2).sub.3 --CH.sub.2 CH.sub.2 CH.sub.2 R O (I)in which R is a C.sub.1 -C.sub.8 lower alkoxy or C.sub.4 -C.sub.6 cycloalkoxy group, substituted with one or more hydroxyl groups and/or interrupted by one or more hetero atoms chosen from oxygen and sulphur, an amino group of structure ##STR1## in which R.sub.1 or R.sub.2, which may be identical or different, denote a hydrogen atom or a linear or branched C.sub.1 -C.sub.8 lower alkyl radical, optionally interrupted by one or more hetero atoms chosen from oxygen, sulphur and nitrogen, this alkyl radical being able to be substituted with one or more hydroxyl groups, R.sub.1 and R.sub.2 not being able to denote hydrogen simultaneously, or alternatively R.sub.1 and R.sub.2 form, together with the nitrogen atom, a heterocyclic system optionally containing oxygen, sulphur or nitrogen as an additional hetero atom, one of the radicals R.sub.1 and R.sub.Type: GrantFiled: July 3, 1986Date of Patent: October 31, 1989Assignee: Centre International de Recherches Dermatologiques dite C.I.R.D.Inventors: Braham Shroot, Christopher Hensby, Jean Maignan, Gerard Lang, Serge Restle, Michel Colin
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Patent number: 4876341Abstract: Acetoacetamide-N-sulfonic acid and its salts are cyclized with at least approximately the equimolar amount of SO.sub.3 in short times, preferably in special apparatus, to give 6-methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide. In the case where more than the equimolar amount of SO.sub.3 is used, the latter compound is produced as an SO.sub.3 adduct which then needs to be hydrolyzed; the hydrolysis also takes place in short times and, particularly advantageously, in apparatus of the same type as for the cyclization.The non-toxic salts, especially the potassium salt - of 6-methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide are valuable synthetic sweeteners.Type: GrantFiled: August 2, 1988Date of Patent: October 24, 1989Assignee: Hoechst AktiengesellschaftInventors: Joachim Schutz, Otto E. Schweikert
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Patent number: 4861879Abstract: Substituted [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H -imidazoles and 1H-1,2,4-triazoles having antimicrobial properties and being particularly useful in the treatment of vaginal candidosis.Type: GrantFiled: February 9, 1988Date of Patent: August 29, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Heeres, Raymond A. Stokbroekx, Leo J. J. Backx
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Patent number: 4855423Abstract: Sulfatobetaines are prepared by reacting an addition compound of sulfur trioxide and a tertiary amine with an alkylene carbonate.Type: GrantFiled: October 13, 1987Date of Patent: August 8, 1989Assignee: BASF AktiengesellschaftInventors: Gerold Braun, Chung-Ji Tschang, Christos Vamvakaris, Klaus Glaser
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Patent number: 4853381Abstract: The invention provides compounds of the general formula (I) ##STR1## whereinAr represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms, or the groups C.sub.1-6 alkyl, C.sub.1-6 alkoxy, nitro, --(CH.sub.2).sub.q R [where R is hydroxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represent a hydrogen atom or a C.sub.1-4 alkyl group, or --NR.sup.3 R.sup.4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O--, or --S-- or a group --NH-- or --N(CH.sub.3)--), --NR.sup.5 COR.sup.6 (where R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.6 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or --NR.sup.3 R.sup.4 group), --NR.sup.5 SO.sub.2 R.sup.7 (where R.sup.7 represents a C.sub.1-4 alkyl, phenyl or --NR.sup.3 R.sup.4 group), --COR.sup.8 (where R.sup.8 represents hydroxy, C.sub.1-4 alkoxy or --NR.sup.3 R.sup.4), --SR.sup.Type: GrantFiled: October 15, 1986Date of Patent: August 1, 1989Assignee: Glaxo Group LimitedInventors: Harry Finch, Lawrence H. C. Lunts, Alan Naylor, Ian F. Skidmore, Ian B. Campbell
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Patent number: 4846874Abstract: Novel N-(heterocyclicaminocarbonyl) substituted thiophene- , furan- and pyrrolesulfonamides, such as N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno- [3,2-b]thiopyran-3-sulfonamide. 4,4-dioxide and N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno[3,2-b ]thiopyran-3-sulfonamide, 4,4-dioxide and their method-of-use as herbicides are described.Type: GrantFiled: December 16, 1987Date of Patent: July 11, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Robert J. Pasteris
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Patent number: 4840951Abstract: Naphthalene derivative of the formula: ##STR1## wherein Ring A is a substituted or unsubstituted benzene ring; each of R.sup.1 and R.sup.2 is a group of the formula: --OR.sup.5, --NHR.sup.5 or ##STR2## or either one of R.sup.1 and R.sup.2 is a lower alkoxy group and the other one is a group of the formula: --OR.sup.5, --NHR.sup.5 or ##STR3## each of R.sup.3 and R.sup.4 is a lower alkoxy group, or one of R.sup.3 and R.sup.4 is a lower alkoxy group and the other is a hydrogen atom; R.sup.5 is a substituted alkyl group, a heterocyclic group, a cycloalkyl group, an alkyl group of at least 5 carbon atoms or alkenyl group; and each of R.sup.6 and R.sup.7 is hydrogen atom or a lower alkyl group and salts thereof are disclosed. Said naphthalene derivative (I) and its salts have excellent hypolipidemic activity and are useful for treatment or prophylaxis of hyperlipidemia and/or arteriosclerosis.Type: GrantFiled: June 17, 1987Date of Patent: June 20, 1989Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tameo Iwasaki, Kohki Takashima
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Patent number: 4837330Abstract: Sulfatobetaines are prepared by reacting an adduct of a base having a tertiary N atom and sulfur trioxide with an alkylene oxide in the presence of an alkylene carbonate as a solvent.Type: GrantFiled: March 15, 1988Date of Patent: June 6, 1989Assignee: BASF AktiengesellschaftInventors: Gerold Braun, Chung-Ji Tschang, Christos Vamvakaris, Klaus Glaser
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Patent number: 4806639Abstract: 6-Methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide is prepared by cylcizing acetoacetamide-N-sulfonic acid or its salts with an at least approximately equimolar amount of SO.sub.3 in the presence of a water-immiscible, inert organic solvent and, if appropriate, also an inert, inorganic solvent. In the event that an equimolar amount of SO.sub.3 is employed, working up is effected by adding aqueous sulfuric acid when the cyclization reaction is complete; in the event that the amount of SO.sub.3 employed is more than equimolar, the 6-methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide obtained in the form of the SO.sub.3 -adduct is hydrolyzed by adding water or ice, whereby sulfuric acid is formed from the SO.sub.3 combined in the SO.sub.3 -adduct.The inert, organic solvent is then removed from the resulting multi-phase mixture by distillation, and the 6-methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide is obtained in a pure form from the remaining aqueous sulfuric acid phase by crystallization.Type: GrantFiled: August 29, 1986Date of Patent: February 21, 1989Assignee: Hoechst AktiengesellschaftInventors: Dieter Reuschling, Adolf Linkies, Walter Reimann, Otto E. Schweikert, Karl E. Mack
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Patent number: 4804755Abstract: The non-toxic salts of 6-methyl-3,4-dihydro-1,2,3-oxothiazin-4-one 2,2-dioxide are prepared by cyclizing acetoacetamide-N-sulfonic acid or its salts with an at least approximately equimolar amount of SO3 in the presence of a water-immiscible, inert organic solvent and, if appropriate, also an inert inorganic solvent, hydrolyzing the 6-methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide obtained in the form of the SO3-adduct after the cyclization reaction, in the event that the amount of SO3 employed is more than equimolar, purifying the organic phase (which has separated out) by extraction with a small volume of water or dilute aqueous sulfuric acid, preferably only with water, and isolating, by neutralization with bases, the non-toxic salts of the 6-methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide from the organic phase thus purified.The said salts are obtained in this process in an extremely pure form; they are valuable synthetic sweetening agents. The potassium salt is known as acesulfam (K).Type: GrantFiled: August 29, 1986Date of Patent: February 14, 1989Assignee: Hoechst AktiengesellschaftInventors: Dieter Reuschling, Adolf Linkies, Walter Reimann, Otto E. Schweikert, Karl E. Mack, Wolfgang Ebertz
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Patent number: 4775406Abstract: The salts of 1-phenylimidazole-5-carboxylic acids substituted in the phenyl ring, of the general formula (I) ##STR1## exhibit a good plant growth-regulating activity. In the general formula the symbols have the following meaning:Y is an ammonium ion substituted up to fourfold by (substituted) alkyl, (substituted) alkenyl, alkynyl, (substituted) cycloalkyl, cycloalkenyl, and (substituted) phenyl, wherein the charged N may be part of a heterocyclic radial (NH.sub.4.sup.+ is excepted); phosphonium ion substituted fourfold by alkyl, (substituted) phenyl or (substituted) benzyl; sulfonium- or sulfoxonium ion substituted threefold by alkyl, (substituted) phenyl or (substituted) benzyl; the guanidinium ion or an O-alkylisourea cation;R.sup.1, R.sup.2 independently of each other are alkyl;R.sup.3 is alkyl, alkoxy or halogen; andn is 0, 1, 2 or 3.Type: GrantFiled: November 21, 1985Date of Patent: October 4, 1988Assignee: Hoechst AktiengesellschaftInventors: Roland Schmierer, Ernst-Friedrich Schulze, Helmut Bustell, Erwin Hacker
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Patent number: 4772309Abstract: A 5-Acylamino-pyrazole derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,R.sup.3 represents hydrogen or alkyl,R.sup.4 represents hydrogen or alkyl,X represents oxygen or sulphur,n represents the integer 0, 1 or 2,Ar represents in each case optionally substituted phenyl or pyridyl andHet represents an optionally substituted 5- or 6- membered heterocyclic radical linked via a carbon atom,which exhibit herbicidal and plant growth regulating activity.Type: GrantFiled: March 19, 1987Date of Patent: September 20, 1988Assignee: Bayer AktiengesellschaftInventors: Jorg Stetter, Reinhold Gehring, Otto Schallner, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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Patent number: 4762550Abstract: This invention relates to novel pyrazolesulfonamides, agricultural compositions thereof and the methods of their use as general and/or selective herbicides and/or plant growth regulants.Type: GrantFiled: August 13, 1987Date of Patent: August 9, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Stephen L. Hartzell
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Patent number: 4759790Abstract: This invention relates to herbicidally active sulfonamide compounds having a heterocyclic carbonyl group ortho to the sulfonyl bridge.Type: GrantFiled: May 21, 1987Date of Patent: July 26, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Joel R. Christensen
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Patent number: 4742055Abstract: A class of 3- and 5-amino thiatriazine compounds exhibiting pharmacological activity, including anti-ulcerogenic and gastrointestinal cytoprotective activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: April 27, 1984Date of Patent: May 3, 1988Assignee: Rorer Pharmaceutical CorporationInventors: William L. Studt, Donald E. Kuhla, Henry F. Campbell, Stuart A. Dodson