The Additional Hetero Ring Is 1,3-diazine (including Hydrogenated) Patents (Class 540/601)
  • Patent number: 5696053
    Abstract: Salts of the formula (I) ##STR1## in which n is 0, 1, 2 or 3,R is halogen, alkyl or alkoxy, mainly in each case independently of other substituents R in the event that n is greater than 1,R.sup.1 is a substituted or unsubstituted hydrocarbon radical or a substituted or unsubstituted heterocyclic radical,R.sup.2 is an acyl radical,R.sup.3 is hydrogen or C.sub.1 -C.sub.5 -alkyl,M.sym. is a metal or ammonium ion,X and Y independently of one another are halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy or C.sub.1 -C.sub.6 -alkylthio, each of the three last-mentioned radicals being unsubstituted or substituted by one or more radicals selected from the group consisting of halogen, C.sub.1 -C.sub.4 -alkoxy and C.sub.1 -C.sub.4 -alkylthio, or are C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.3 -C.sub.6 -alkenyloxy, C.sub.2 -C.sub.6 -alkynyloxy, mono- or di(C.sub.1 -C.sub.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: December 9, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5656625
    Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 17, 1995
    Date of Patent: August 12, 1997
    Assignees: The United States of America as represented by the Department of Health and Human Services, Brown University Research Foundation
    Inventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 5654428
    Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-[4-(3-pyridyl)-3,5-difluorophenyl]-2-oxazolid inone.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 5, 1997
    Assignee: Pharmacia & Upjohn Company
    Inventors: Michael R. Barbachyn, Steven J. Brickner
  • Patent number: 5627136
    Abstract: Pyridine-N-oxide-substituted salicylaldehyde and salicylic acid derivatives of the general formula I ##STR1## where R is a formyl group, a CO.sub.2 H group or a radical which can be hydrolyzed to CO.sub.2 H and the other substituents have the following meanings:R.sup.2 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio;X is nitrogen or CR.sup.13, R.sup.13 being hydrogen or halogen or together with R.sup.3 forming a 3- to 4-membered alkylene or alkenylene chain in which at least one methylene group is replaced by oxygen;R.sup.3 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio, or R.sup.3 is linked with R.sup.13 as indicated above to give a 5- or 6-membered ring;Y is oxygen or sulfur;R.sup.14 -R.sup.
    Type: Grant
    Filed: November 1, 1994
    Date of Patent: May 6, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Joachim Rheinheimer, Uwe J. Vogelbacher, Ernst Baumann, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 5620971
    Abstract: The present invention relates to novel compounds which possess a broad range of useful biological activities. These compounds can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. They can also suppress, modify, or significantly reduce an immune response, including an autoimmune response in a mammal. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, for use in multi-drug resistant cancer therapy, and for prevention or treatment of graft rejection and various autoimmune diseases.
    Type: Grant
    Filed: March 25, 1994
    Date of Patent: April 15, 1997
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David M. Armistead, Jeffrey O. Saunders, Joshua S. Boger
  • Patent number: 5597824
    Abstract: A compound of the formula: ##STR1## wherein B is a purin-9-yl group or a heterocyclic isostere of a purin-9-yl group; or a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; A is --CH-- or A--G taken together is --C(.dbd.O)--, --C(.dbd.CH.sub.2)--, --C(OH)(CH.sub.2 OH)-- or ##STR2## and G and D are functional groups; or a pharmaceutically acceptable salt or ester thereof.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: January 28, 1997
    Assignee: Abbott Laboratories
    Inventors: Daniel W. Norbeck, Jacob J. Plattner, Terry J. Rosen
  • Patent number: 5595992
    Abstract: Substituted pyridines and pyrimidines, processes for their preparation and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## in which A is N or CH, R is H, halogen, alkyl or cycloalkyl, R.sup.2 and R.sup.3 are H, halogen or an aliphatic radical or together form a ring, X is O, NH Or S(O).sub.q where q=0, 1 or 2, R.sup.4.sub.q is 0-4 radicals selected from the series consisting of halogen, optionally substituted alkyl or alkoxy, cycloalkyl and optionally substituted phenyl, n=0-2, m=1-3 and Y is optionally substituted methylene or imino.The invention furthermore relates to a process for their preparation and for their use as pesticides, in particular as insecticides, acaricides and fungicides. The compounds are furthermore suitable for controlling nematodes, helminths and molluscs, and for controlling endoparasites and ectoparasites in the field of veterinary medicine.
    Type: Grant
    Filed: September 12, 1994
    Date of Patent: January 21, 1997
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Rainer Preuss, Wolfgang Schaper, Martin M arkl, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter L ummen, Werner Bonin
  • Patent number: 5559128
    Abstract: The present invention is directed to certain novel compounds identified as 3-substituted piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.1a, R.sup.2a, R.sup.4, R.sup.5, A, X, and Y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing these compounds as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: April 18, 1995
    Date of Patent: September 24, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, Ravi Nargund, Robert W. Marquis, Arthur A. Patchett, Lihu Yang
  • Patent number: 5550240
    Abstract: An intermediate compound is disclosed that is useful in the preparation of a lipid-peroxidation inhibiting substance and that is selected from the group consisting of:2,4-bis[1-adamantylamino]-6-(1-piperazinyl)pyrimidine; and4,6-bis(1-adamantylamino)-2-(1-piperazinyl)pyrimidine;or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: December 8, 1994
    Date of Patent: August 27, 1996
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: S andor Mah o, Zolt an Tuba, Csaba S anta, G abor Balogh, Eva Czajlikn e Csiz er, M aria Lovasn e Marsai, Gy orgy G alik
  • Patent number: 5541186
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 to R, R.sup.a, R.sup.b X, Y, Z, m and n have the significance given in the description, can be used as medicaments, especially for the treatment and prophylaxix of conditions which are associated with endothelin activities.
    Type: Grant
    Filed: June 27, 1994
    Date of Patent: July 30, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael L offler, Marcel M uller, Werner Neidhart, Henri Ramuz
  • Patent number: 5536837
    Abstract: The present invention provides an N-sulfonyl carboxylic amide derivative including an N-containing 6-membered aromatic ring represented by formula [I]: ##STR1## wherein R.sup.1 represents an alkyl group, an alkenyl group, or the like, R.sup.2 represents a hydrogen atom, an alkyl group, or the like, R.sup.3 and R.sup.4 represent independently an alkyl group, alkoxy group, or the like, and X and Y represent independently a methyne group or a nitrogen atom; or the salt of the same, a method for producing the same, and a biocide containing the same as an active ingredient. The N-sulfonyl carboxylic amide derivative including an N-containing 6-membered aromatic ring according to the present invention exhibits superior effects against blight caused by plant pathogenic fungi belonging to Oomycetes such as downy mildew, late blight, or the like in a low concentration as well as controls weeds occurring in paddy fields and plowed fields.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: July 16, 1996
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Ikumi Urushibata, Takumi Yoshimura, Takeshi Deguchi, Norihisa Yonekura, Junetsu Sakai, Shigeru Hayashi
  • Patent number: 5532203
    Abstract: Mixtures of a herbicidally effective amount of a pyridylsulfonylurea of formula I, ##STR1## wherein R, R.sub.1, R.sub.2 and A are as defined in claim 1, and of a herbicide-antagonistically effective amount of a sulfamoylphenylurea of formula II, ##STR2## wherein R.sub.7 to R.sub.11 and A.sub.2 are as defined in claim 1, are very suitable for controlling weeds in crops of useful plants, especially maize and sugar cane.
    Type: Grant
    Filed: May 1, 1995
    Date of Patent: July 2, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Werner Fory, Elmar Kerber, Manfred Hudetz
  • Patent number: 5525604
    Abstract: A 4-aminopyrimidine of the formula (I): ##STR1## wherein A is a bond, C1-4 alkylene or C1-4 oxyalkylene;Y is a bond, C1-4 alkylene, C1-4 alkyleneoxy, C1-4 alkoxyphenylene or phenyl(C1-4)alkylene;Z is a bond or vinylene;R1 is 4-15 membered heterocyclic ring containing one or two nitrogen atom;R2 is (i) 4-15 membered heterocyclic ring containing one or two nitrogen, one or two of oxygen or one sulfur atom,(ii) C4-15 carbocyclic ring,(iii) C1-4 alkoxy,(iv) hydroxy(C1-4 alkoxy) or(v) hydroxy;R3 is (i) 4-15 membered heterocyclic ring containing one or two nitrogen, one oxygen, one sulfur, or one nitrogen and one sulfur atom,(ii) C4-15 carbocyclic ring,(iii) formula:CH2.dbd.CH(X)--whereinX is halogen.(iv) hydrogen.l is 1 or 2.and some compounds are excluded.and acid addition salts thereof, salts thereof; have inhibitory effect on cGMP-PDE, or additionally on TXA2 synthetase.
    Type: Grant
    Filed: August 24, 1994
    Date of Patent: June 11, 1996
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Sung J. Lee, Yoshitaka Konishi, Orest T. Macina, Kigen Kondo, Dingwei T. Yu, Tamara A. Miskowski
  • Patent number: 5512567
    Abstract: Analgesic compounds of the formula (I); ##STR1## in which, R.sup.1 and R.sup.2 each represents hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocycle; E represents oxygen or an imino group optionally substituted with C.sub.1 -C.sub.6 alkyl or aralkyl; ring A is an aryl or heteroaryl ring, optionally substituted; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen or R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(.dbd.Y)-- (IV)wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen, up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygen; provided that when E represents a methylene group, then R.sup.3 is a C.sub.1 -C.sub.6 alkyl group or R.sup.3 and R.sup.4 together represent a group of the formula (IV).
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: April 30, 1996
    Assignee: Sankyo Company, Limited
    Inventors: Atsusuke Terada, Yoshio Iizuka, Kazuyuki Wachi, Kenji Fujibayashi
  • Patent number: 5500406
    Abstract: The present invention provides novel iminosulfonylurea derivatives which are useful as herbicides with excellent activity and selectivity. These derivatives can be used to protect rice, wheat, corn, soybean, cotton and sugar beet from weeds.
    Type: Grant
    Filed: April 15, 1994
    Date of Patent: March 19, 1996
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Kenzi Makino, Shigeaki Akiyama, Hideaki Suzuki, Takeshi Nagaoka, Toshio Niki, Koichi Suzuki, Tsutomu Nawamaki, Shigeomi Watanabe, Kimihiro Ishikawa
  • Patent number: 5492916
    Abstract: The present invention is directed to certain novel compounds identified as di- and tri-substituted piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R.sub.1, R.sub.4, R.sub.5, A,X,Y, and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such di and tri substituted piperidines, pyrrolidines, and hexahydro-1H-azepines as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: October 17, 1994
    Date of Patent: February 20, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Gregori J. Morriello, Arthur A. Patchett, Lihu Yang
  • Patent number: 5478934
    Abstract: 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: Grant
    Filed: November 23, 1994
    Date of Patent: December 26, 1995
    Inventors: Jun Yuan, Jan W. F. Wasley
  • Patent number: 5470975
    Abstract: Novel A-II receptor antagonists have the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.
    Type: Grant
    Filed: January 11, 1994
    Date of Patent: November 28, 1995
    Assignee: E.R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 5466687
    Abstract: The invention relates to arylidene-1-azacycloalkanes and arylalkyl-1-azacycloalkanes of the general formula ##STR1## (wherein n, m, p, A, W.sup.1, W.sup.2, X, Y, and R.sup.1 to R.sup.11 are as defined in claim 1) and the isomers, isomer mixtures and salts thereof, which have useful properties, in particular an inhibitory effect on cholesterol biosynthesis.
    Type: Grant
    Filed: March 25, 1994
    Date of Patent: November 14, 1995
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
  • Patent number: 5462940
    Abstract: The 4-oxocyclic ureas and the pharmaceutically acceptable salts and esters thereof, of the present invention are useful as antiarrhythmic and antifibrillatory agents and have the following general structure: ##STR1## wherein X, Y, A, L, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are defined as in the specification.
    Type: Grant
    Filed: June 3, 1994
    Date of Patent: October 31, 1995
    Assignee: Norwich Eaton Pharmaceuticals, Inc.
    Inventors: Chia-Nien Yu, Stanford S. Pelosi, Jr., Mark A. Calcagno
  • Patent number: 5444060
    Abstract: The present invention provides an N-sulfonyl carboxylic amide derivative including an N-containing 6-membered aromatic ring represented by formula [I]: ##STR1## wherein R.sup.1 represents an alkyl group, an alkenyl group, or the like, R.sup.2 represents a hydrogen atom, an alkyl group, or the like, R.sup.3 and R.sup.4 represent independently an alkyl group, alkoxy group, or the like, and X and Y represent independently a methyne group or a nitrogen atom; or the salt of the same, a method for producing the same, and a biocide containing the same as an active ingredient. The N-sulfonyl carboxylic amide derivative including an N-containing 6-membered aromatic ring according to the present invention exhibits superior effects against blight caused by plant pathogenic fungi belonging to Oomycetes such as downy mildew, late blight, or the like in a low concentration as well as controls weeds occurring in paddy fields and plowed fields.
    Type: Grant
    Filed: November 2, 1993
    Date of Patent: August 22, 1995
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Ikumi Urushibata, Takumi Yoshimura, Takeshi Deguchi, Norihasa Yonekura, Junetsu Sakai, Shigeru Hayashi
  • Patent number: 5403816
    Abstract: 3-Pyrimidinyloxy-substituted picolinic acid derivatives of the formula ##STR1## and their salts are useful as herbicides against annual and perennial gramineous and broadleaf weeds while exhibiting low phytotoxicity to desired crop plants.
    Type: Grant
    Filed: April 20, 1993
    Date of Patent: April 4, 1995
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Fumiaki Takabe, Yoshihiro Saito, Masatoshi Tamaru, Shigehiko Tachikawa, Ryo Hanai
  • Patent number: 5360804
    Abstract: Multicomponent agent or kit for preparing the sulpho-conjugated form of pyridino, pyrimidino or triazino N-oxide compounds and method of use.The present invention relates to a multicomponent agent or kit for preparing the sulpho-conjugated form of pyridino, pyrimidino or triazino N-oxide compounds,comprising at least one compound of the pyridino, pyrimidino or triazino N-oxide type, on the one hand,and a sulphating agent, on the other hand.
    Type: Grant
    Filed: December 12, 1991
    Date of Patent: November 1, 1994
    Assignee: L'Oreal
    Inventors: Quintino Gaetani, Andre Rougier, Albert Duranton, Michel Hocquaux
  • Patent number: 5300640
    Abstract: A novel herbicidal pyrimidine derivative represented by the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y.sup.1, Y.sup.2, Y.sup.3, X and Z are as defined herein.
    Type: Grant
    Filed: December 19, 1991
    Date of Patent: April 5, 1994
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Mitsumori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
  • Patent number: 5276007
    Abstract: Substituted sulfonylureas of the general formula I ##STR1## where n and m are each 0 or 1, andR.sup.1 is hydrogen, alkyl, alkenyl or alkynyl;R.sup.2 is halogen or trifluoromethyl when m is 0, or, when m is 1, alkyl, alkenyl or alkynyl and, when X is 0 or S and m is 1, is trifluoromethyl or chlorodifluoromethyl;X is 0, S or N--R.sup.4, where R.sup.4 is hydrogen or alkyl;R.sup.3 is hydrogen, halogen, alkyl, haloalkyl or alkoxy;A is haloalkyl, halogen or ##STR2## where Z is oxygen or alkylimino N--R.sup.6 ;R.sup.5 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, alkenyl or alkynyl;R.sup.6 is hydrogen, alkyl, or together with R.sup.5 is a C.sub.4 -C.sub.6 -alkylene chain, where one methylene may be replaced by an oxygen atom or a C.sub.1 -C.sub.4 -alkylimino group, andR.sup.7 is hydrogen or halogen,and environmentally tolerated salts thereof, processes and intermediates for the manufacture of compounds I, and their use as herbicides and bioregulators.
    Type: Grant
    Filed: February 19, 1991
    Date of Patent: January 4, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerhard Hamprecht, Horst Mayer, Karl-Otto Westphalen, Bruno Wuerzer, Matthias Gerber, Klaus Grossmann, Wilhelm Rademacher
  • Patent number: 5262386
    Abstract: Pyrimidinyl- and triazinyl-salicylamides of the formula I ##STR1## in which the meanings of the radicals are described in claim 1, and the salts of compounds of the formula I which have a free hydroxycarbonyl group have a herbicidal and plant-growth regulating action. They are suitable as active substances in weed killers and in compositions for positively influencing the growth of crop plants.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: November 16, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Christoph Luthy, Raymond Fisher
  • Patent number: 5260293
    Abstract: The present invention provides pyrazines, pyridazines or pyrimidines, or salts or prodrugs thereof, substituted on one of the ring carbon atoms thereof with a non-aromatic azacyclic or azabicyclic ring system; and independently substituted on each of the other ring carbon atoms with a substituent of low lipophilicity or a hydrocarbon substituent; which compounds stimulate central muscarinic acetylcholine receptors and therefore are useful in the treatment of neurological and mental illnesses.
    Type: Grant
    Filed: October 10, 1991
    Date of Patent: November 9, 1993
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Leslie J. Street, John Saunders
  • Patent number: 5252567
    Abstract: This invention concerns compounds of the formula I: ##STR1## wherein R.sup.1 is (1-10C)alkyl, (3-8C)cycloalkyl, (3-8C)cycloalkyl-(1-4C)-alkyl, phenyl or phenyl(1-4C)alkyl, the phenyl moiety of the latter two optionally bearing one or more substituents; R.sup.2 is hydrogen, (1-4C)alkyl, amino or (1-4C)alkylamino; R.sup.6 is (1-4C)alkyl, amino or (1-4C)alkylamino; Q is a group of formula II, in which case R.sup.3 and R.sup.4 are independently hydrogen, (1-4C)alkyl, phenyl or benzyl the phenyl moiety of the latter two optionally bearing one or two substituents; R.sup.5 is hydrogen, (1-4C)alkyl or (2-4C)alkenyl; A and B are independently ethylene or trimethylene; Z is a direct bond between A and B, or an oxy, thio, carbonyl, methylene, ethylenedioxymethylene, ethylidene, or isopropylidene link, or Z is a group of the formula .dbd.N.
    Type: Grant
    Filed: December 18, 1990
    Date of Patent: October 12, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Stuart D. Mills, Rodney B. Hargreaves, Bernard J. McLoughlin
  • Patent number: 5250530
    Abstract: Aminopyrimidine derivatives, their preparation, and agents containing them, and their use as fungicides comprising ##STR1## in which R.sup.1 is alkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, alkenyl, alkynyl, cycloalkylalkyl, substituted aminoalkyl, phenyl, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl or phenoxyphenoxyalkyl, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl, or phenyl, R.sup.5 is H, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, alkoxy, alkylthio, alkoxyalkyl, R.sup.7 R.sup.8 N-,alkylthioalkyl, R.sup.7 R.sup.8 N-alkyl, halogen, alkenyl, alkynyl, phenyl, phenoxy, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl, phenylmercapto, phenylalkoxy or phenylalkylthio, R5 is H, alkyl, alkyloxy, alkenyloxy, alkynyloxy, alkylthio, halogen, or phenyl or R.sup.5 and R.sup.6 together form a chain, and R.sup.7 and R.sup.8 are H, alkyl, alkoxyalkyl, hydroxyalkyl, alkylthioalkyl, alkenyl, substituted formyl, phenyl or phenylalkyl, or R.sup.7 or R.sup.
    Type: Grant
    Filed: July 9, 1990
    Date of Patent: October 5, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Giencke, Burkhard Sachse, Heinrich Wicke
  • Patent number: 5151424
    Abstract: [(Bicyclic heterocyclyl)methyl and -hetero] substituted hexahydro-1H-azepines and pyrrolidines and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.
    Type: Grant
    Filed: September 9, 1991
    Date of Patent: September 29, 1992
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Gaston S. M. Diels, Geert M. E. Pille
  • Patent number: 5147876
    Abstract: 2,6-di-, 2,4,6-, 2,5,6-tri- or 2,4,5,6-tetra-substituted pyrimidines, and 2,6-di-substituted pyridines. These compounds are useful for treatment of neurological diseases.
    Type: Grant
    Filed: December 29, 1989
    Date of Patent: September 15, 1992
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Akira Mizuchi, Kazutoshi Horikomi, Tadayuki Sasaki, Akira Awaya, Ikuo Tomino, Mitsuyuki Takesue, Noriaki Kihara
  • Patent number: 5135563
    Abstract: The present invention relates to a pyrimidine derivative having the formula ##STR1## (wherein the variables are defined in the full text of the patent), a method for producing the same, and its use as a herbicide.
    Type: Grant
    Filed: July 5, 1991
    Date of Patent: August 4, 1992
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saitoh, Hideyuki Shibata
  • Patent number: 5130317
    Abstract: Pyrimidine-4,6-dicarboxylic acid diamides, processes for the use thereof, and pharmaceuticals based on these compoundsThe invention relates to pyrimidine-4,6-dicarboxylic acid diamides of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The compounds according to the invention inhibit proline hydroxylase and lysine hydroxylase and can be employed as fibrosuppressants and immunosuppressants.
    Type: Grant
    Filed: September 19, 1990
    Date of Patent: July 14, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ekkehard Baader, Martin Bickel, Volkmar Gunzler-Pukall, Stephan Henke
  • Patent number: 5125957
    Abstract: A pyrimidine derivative represented by the formula ##STR1## wherein the variables are defined below in the specification, and their production and herbicidal activities are described.
    Type: Grant
    Filed: October 24, 1990
    Date of Patent: June 30, 1992
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
  • Patent number: 5116835
    Abstract: Enzyme-inhibiting urea derivatives of dipeptides, a process for the preparation thereof, agents containing these, and the use thereof.The present invention relates to compounds of the formula I ##STR1## in which A and B denote, indpendently of one another, an amino acid,X as desired can be absent or represents --O--, --S--, --CF.sub.2 --, --CO-- or --CHR.sup.8,p and q denote, independently of one another, 0, 1, 2, 3 or 4, andR.sup.1 to R.sup.4 are defined in the description, as well as the salts thereof.The invention furthermore relates to a process for the preparation of the compounds of the formula I and to the use thereof as medicines.
    Type: Grant
    Filed: December 7, 1989
    Date of Patent: May 26, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Ruger, Hansjorg Urbach, Dieter Ruppert, Bernward Scholkens
  • Patent number: 5104872
    Abstract: Compound of the general formula (I), which is useful as an agricultural and horticultural fungicide, an agricultural and horticultural fungicidal composition containing said compound, use of said composition for controlling plant disease, and process for the production of said compound: ##STR1## wherein ##STR2## shows a case in which R.sup.3 and R.sup.4 together form a cyclic substituent, and R.sup.1 and R.sup.4 are substituents disclosed in the specification.
    Type: Grant
    Filed: August 15, 1990
    Date of Patent: April 14, 1992
    Assignee: Nihon Hohyaku Co., Ltd.
    Inventors: Kenji Tsubata, Nobuyuki Niino, Katsutoshi Endo, Yoshinobu Yamamoto, Hideo Kanno
  • Patent number: 5093336
    Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: March 3, 1992
    Assignee: Hoechat-Roussel Pharmaceuticals, Inc.
    Inventors: Raymond W. Kosley, Jr., Bettina Spahl
  • Patent number: 5071847
    Abstract: The invention relates to compounds of formula I: ##STR1## in which m=2-4,n and p, which may be identical or different, are an integer equal to 1, 2 or 3, with the proviso that the sum of n and p is 5,q=0 or 1,R is a 1,2,3,4-tetrahydro-3-quinazolinyl radical, optionally substituted, a 1,3,4,6,11,11a-hexahydro-1,3-dioxo-2H-pyrazino[1,2-b]isoquinol-2-yl radical, a 1,2-dihydro-1-oxo-2-phthalazinyl radical, optionally substituted, a 2,6-dioxo-1-piperazinyl radical of formula W: ##STR2## (R.sub.3 is a 2-pyridyl radical or an optionally substituted phenyl radical),a radical of formula Z: ##STR3## (R.sub.4 is a carbamoyl radical, a cyano radical, a hydroxycarbonyl radical or an alkoxycarbonyl radical having 1 to 6 carbon atoms),or a radical of formula Y: ##STR4## (R.sub.5 is a 2-pyrimidinyl radical, a 1-isoquinolyl radical, a 2-quinolyl radical, a 2-pyridyl radical, a benzyl radical, optionally substituted, a 2-thiazolyl radical, optionally substituted, or a 2-benzothiazolyl radical) andeither R.sub.1 and R.sub.
    Type: Grant
    Filed: August 24, 1990
    Date of Patent: December 10, 1991
    Assignee: Adir et Compagnie
    Inventors: Gilbert Lavielle, Francis Colpaert, Michel Laubie
  • Patent number: 5047406
    Abstract: Substituted cyclohexanols and cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
    Type: Grant
    Filed: May 2, 1990
    Date of Patent: September 10, 1991
    Assignee: Warner-Lambert Co.
    Inventors: Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
  • Patent number: 5026702
    Abstract: The invention relates to new morpholines and morpholine-N-oxides of formula ##STR1## wherein the substituents are defined hereunder, which compounds have valuable pharmacological properties, namely an effect on the metabolism, preferably the effect of lowering blood sugar and reducing body fat, and the effect of lowering the atherogenic .beta.-lipoproteins VLDL and LDL, and a performance enhancing effect in animals.
    Type: Grant
    Filed: March 23, 1989
    Date of Patent: June 25, 1991
    Assignee: Dr. Karl Thomae, GmbH
    Inventors: Manfred Reiffen, Michael Mark, Robert Sauter, Wolfgang Grell
  • Patent number: 5017211
    Abstract: The invention is concerned with novel compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the significances given in the description, as well as enol ethers and salts thereof and their manufacture, weed control compositions which contain such compounds as the active substance and the use of the active substances or compositions for the control of weeds. The invention is also concerned with certain novel starting materials and their production.
    Type: Grant
    Filed: May 19, 1989
    Date of Patent: May 21, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Jean Wenger, Paul Winternitz, Martin Zeller
  • Patent number: 5015284
    Abstract: Compounds of the formula I, their stereoisomers or their salts ##STR1## wherein A denotes >C(R.sup.4).sub.2 or >C.dbd.C(R.sup.5).sub.2 ; R.sup.1 denotes H, an optionally substituted aliphatic or cycloaliphatic radical, forfuryl, tetrahydrofurfuryl or (substituted) phenyl; R.sup.2 denotes H, alkyl, alkenyl, alkynyl or alkoxy; R.sup.3 denotes a radical of the formulae ##STR2## X denotes O, S or NR.sup.12 and Y denotes O or S, possess excellent herbicidal and plant-growth regulating properties.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: May 14, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
  • Patent number: 5008268
    Abstract: 2-Amino-pyrimidininone derivatives possessing antihistaminic and serotonin-antagonistic properties. Compositions containing these compounds as the active ingredient and a method of treating subjects from allergic diseases.
    Type: Grant
    Filed: December 26, 1989
    Date of Patent: April 16, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Ludo E. J. Kennis, Francois M. Sommen, Ann C. J. Dierckx
  • Patent number: 4996318
    Abstract: The amino-9,10-secosteroids ##STR1## of the present invention contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain and are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc.
    Type: Grant
    Filed: September 19, 1989
    Date of Patent: February 26, 1991
    Assignee: The Upjohn Company
    Inventors: Martin Gall, Robert I. Higuchi
  • Patent number: 4968341
    Abstract: Novel substituted aryloxyureas, processes for their production, and herbicides comprising them as active ingredients are provided.The substituted aryloxyureas exhibit an excellent herbicidal efficacy against weeds when applied, for example, to the weeds in a wide range of period from a preemergence stage to a growth stage.The substituted aryloxyureas of the invention have the excellent advantage of maintaining high safety on crops or crop plants in spite of their herbicidal efficacy.
    Type: Grant
    Filed: August 16, 1988
    Date of Patent: November 6, 1990
    Assignees: Kumiai Chemical Industry Co., Mitsui Petrochemical Industries, Ltd.
    Inventors: Isao Hashimoto, Tatsuyodihi Ishida, Kazutaka Tsuru, Yuji Yamada, Takeshige Miyazawa, Yasuo Nakamura, Susumu Katou, Katsuya Takahashi
  • Patent number: 4957921
    Abstract: Substituted cyclohexanols are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
    Type: Grant
    Filed: December 6, 1989
    Date of Patent: September 18, 1990
    Assignee: Warner-Lambert Company
    Inventors: Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
  • Patent number: 4956463
    Abstract: A pyrimidone compound or a pharmaceutically acceptable salt thereof such as a 5,6-di-substituted-2-[4-<3-(1-piperidinomethyl)-phenoxyl>-cis-2-butenylami no]-4-(1H)-pyrimidone or a 5,6-di-substituted-2-[4-<4-(1-piperidinomethyl)-pyridyl-2-oxy>-cis-2-buten ylamino]-4-(1H)-pyrimidone or a pharmaceutically acceptable salt thereof is herein disclosed. Such a compound or a salt thereof simultaneously shows gastric acid secretion inhibiting effect and gastric mucous membrane protecting effect and is useful as medicine for treating gastric diseases such as medicine for inhibiting gastric acid secretion or that for treating digestive ulcers.
    Type: Grant
    Filed: December 7, 1988
    Date of Patent: September 11, 1990
    Assignee: Ikeda Mohando Company, Ltd.
    Inventor: Fujio Nohara
  • Patent number: 4940792
    Abstract: Novel substituted N-sulfonyl-N'-pyrimidinylureas or N-sulfonyl-N'-triazinylureas of the formula I ##STR1## have good pre- and postemergence selective herbicidal and growth regulating properties.In this formulaE is nitrogen or --CH.dbd.,the group ##STR2## is a phenyl, naphthyl, furyl, thiophenyl, pyrrole or pyridinyl radical which is substituted in accordance with the definitions ofR.sup.1 and R.sup.2,R.sup.3 and R.sup.4 are hydrogen, lower alkyl or lower alkoxy, or one of R.sup.3 and R.sup.4 may also be halogen, lower alkenyl, lower haloalkenyl, lower haloalkoxy, amino, lower alkylamino, --CH(OCH.sub.3).sub.2, a cyclized ketal group or a saturated 5- or 7-membered heterocycle which is bound through the nitrogen atom,R.sup.5 is hydrogen, lower alkyl, lower haloalkyl, or an unsubstituted or substituted phenyl, benzyl or naphthyl radical, andR.sup.
    Type: Grant
    Filed: December 4, 1987
    Date of Patent: July 10, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Werner Topfl, Willy Meyer, Hans-Dieter Schneider
  • Patent number: 4904783
    Abstract: N-Arylsulfonyl-N'-(4-mercaptomethyl-pyrimidinyl)-ureas of the formula ##STR1## (symbols in this formula defined herein) and the salts of these compounds with amines, alkali metal bases or alkaline-earth metal bases or with ammonium bases, have good pre- and post-emergence-selective, herbicidal and growth-regulating properties.
    Type: Grant
    Filed: September 19, 1988
    Date of Patent: February 27, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Werner Topfl
  • Patent number: 4902336
    Abstract: N-Arylsulfonyl-N'-(4-mercaptomethyl-pyrimidinyl-ureas of the formula ##STR1## (symbols in this formula defined herein) and the salts of these compounds with amines, alkali metal bases or alkaline-earth metal bases or with ammonium bases, have good pre- and post-emergence-selective, herbicidal and growth-regulating properties.
    Type: Grant
    Filed: September 19, 1988
    Date of Patent: February 20, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Werner Topfl