Triazine Ring Patents (Class 544/112)
  • Patent number: 6458950
    Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):
    Type: Grant
    Filed: August 3, 2000
    Date of Patent: October 1, 2002
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yasuhiro Nishitani, Koji Ishikura
  • Patent number: 6458952
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl uracil compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Grant
    Filed: May 18, 2000
    Date of Patent: October 1, 2002
    Assignee: Pharmacia Corporation
    Inventors: Michael South, Darin E. Jones, Melvin L. Rueppel
  • Publication number: 20020137930
    Abstract: The present invention relates to a process for the preparation of sulphonamide-substituted imidazotriazinones of the general formula (I) 1
    Type: Application
    Filed: December 17, 2001
    Publication date: September 26, 2002
    Inventors: Marc Nowakowski, Reinhold Gehring, Werner Heilmann, Karl-Heinz Wahl
  • Patent number: 6417187
    Abstract: 3-(Substituted aryl)-5-{substituted aryl-(alkynyl-aryl)}-[1,2,4]- triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.
    Type: Grant
    Filed: April 13, 2001
    Date of Patent: July 9, 2002
    Assignee: Dow AgroSciences LLC
    Inventors: Vidyadhar Babu Hegde, Scott Jerome Bis, Emilie Chassat Heo, Christopher Thomas Hamilton, Peter Lee Johnson, Laura Lee Karr, Timothy Patrick Martin, Paul Allen Neese, Nailah Orr, Francis Eugene Tisdell, Maurice Chee Hoong Yap, Yuanming Zhu
  • Publication number: 20020040019
    Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.
    Type: Application
    Filed: August 10, 2001
    Publication date: April 4, 2002
    Inventors: Hui Cai, James P. Edwards, Steven P. Meduna, Barbara A. Pio, Jianmei Wei
  • Patent number: 6362178
    Abstract: The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: March 26, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Niewöhner, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jörg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Serno, Marc Nowakowski
  • Patent number: 6350748
    Abstract: A sulfamoyl compound of the general formulae (1): wherein R1 and R2 are each independently C1-4 alkyl, or R1 and R2 together are C4-6 alkylene or C4-6 alkyleneoxy, Y is H, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylthio, C1-8 haloalkyl, C1-8 haloalkoxy or C1-8 haloalkylthio, A is a predetermined heterocyclic group, B is a predetermined heterocyclic group which is identical with or different from A, W is a chemical bond or O, V is O or S, D, E, F and G are each independently N, CR7, CR8, CR9 or CR10, and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are each independently predetermined group such as H, or an unsubstituted or substituted aliphatic, aromatic or heterocyclic group. The sulfamoyl compound is useful as an agricultural and horticultural fungicide.
    Type: Grant
    Filed: June 2, 2000
    Date of Patent: February 26, 2002
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Toshiaki Takeyama, Toshimasa Hamada, Hiroaki Takahashi, Junichi Watanabe, Kazuhiro Yamagishi, Masanori Nishioka, Hiroyuki Suzuki
  • Publication number: 20020019397
    Abstract: The present invention provides a compound of formula I 1
    Type: Application
    Filed: June 22, 2001
    Publication date: February 14, 2002
    Applicant: Pharmacia & Upjohn Company
    Inventors: Mark E. Schnute, Valerie A. Vaillancourt, Scott D. Larsen
  • Publication number: 20010049379
    Abstract: The present invention relates to 2-aminopyridine derivatives of the formula 1
    Type: Application
    Filed: December 20, 2000
    Publication date: December 6, 2001
    Inventor: John Adams Lowe
  • Publication number: 20010039341
    Abstract: Biphenyl-substituted triazines of the formulae 1
    Type: Application
    Filed: May 3, 2001
    Publication date: November 8, 2001
    Inventors: Ian John Fletcher, Jurgen Kaschig, Georges Metzger, Dieter Reinehr, Pascal Hayoz
  • Patent number: 6288082
    Abstract: This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
    Type: Grant
    Filed: September 24, 1999
    Date of Patent: September 11, 2001
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Hwei-Ru Tsou, Dan M. Berger, Middleton B. Floyd, Jr., Philip R. Hamann, Nan Zhang, Mark E. Salvati, Philip Frost
  • Patent number: 6235738
    Abstract: The invention relates to novel diphenyl-substituted heterocycles with 6-membered ring of general formula (I) in which A, X and the residues R1, R2, R3, R4 and R5 are as defined in the claims, processes for the preparation thereof and the use thereof as medicaments.
    Type: Grant
    Filed: April 12, 1999
    Date of Patent: May 22, 2001
    Assignees: Boehringer Ingelheim Pharma KG, Boehringer Ingelheim Italia S.p.A.
    Inventors: Michael Brenner, Rainer Palluk, Marion Wienrich, Thomas Weiser, Enzo Cereda, Maura Bignotti, Carlo Maria Pellegrini, Giovanni Battista Schiavi, Raffaele Cesana
  • Patent number: 6218391
    Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I) and their use in treating psychiatric disorders and neurological diseases including major depression, anxiety-related disorders, post-traumatic stress disorders, supranuclear palsy and eating disorders.
    Type: Grant
    Filed: August 16, 1999
    Date of Patent: April 17, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Argyrios Georgios Arvanitis, Richard E. Olson, Charles R. Arnold, III, William E. Frietze
  • Patent number: 6197750
    Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.
    Type: Grant
    Filed: October 22, 1998
    Date of Patent: March 6, 2001
    Assignee: Idun Pharmaceuticals, Inc.
    Inventors: Donald S. Karanewsky, Robert J. Ternansky
  • Patent number: 6194413
    Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.
    Type: Grant
    Filed: May 12, 1998
    Date of Patent: February 27, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding
  • Patent number: 6096886
    Abstract: Novel morpholino end-capped polyamino-1,3,5-triazines, methods for their use as light stabilizers for materials which are subject to degradation (for example, by actinic radiation), stabilizer compositions based on these morpholino end-capped polyamino-1,3,5-triazines and methods for their synthesis are herein described.
    Type: Grant
    Filed: November 3, 1998
    Date of Patent: August 1, 2000
    Assignee: Cytec Technology Corp.
    Inventor: Martin L. Cohen
  • Patent number: 5837869
    Abstract: An asymmetric dioxazine compound represented, when shown in free acid form, by the general formula (I): ##STR1## wherein T.sub.1 and T.sub.2 represent a hydrogen atom, a chlorine atom, a bromine atom, a lower alkyl group, a phenoxy group or others, A.sub.1 represents an alkyl group, a chlorine atom, a carboxyl group or others, A.sub.2 represents a hydrogen atom, an alkyl group, a chlorine atom, a carboxyl group or others, R represents a hydrogen atom or a lower alkyl group, X and Y represent a halogen atom, a fiber-reactive group or others, respectively, with the proviso that at least one of X and Y is a fiber-reactive group is provided.The compound is suitable for dyeing or printing of a fiber material or the like which has a hydroxy group and/or an amide group, and provides a blue-dyed product with various fastness, including particularly chlorine fastness.
    Type: Grant
    Filed: January 23, 1997
    Date of Patent: November 17, 1998
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masato Inoue, Junya Hada, Toshiyuki Araki
  • Patent number: 5756732
    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 an 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: May 26, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventors: Michael R. Barbachyn, Steven J. Brickner
  • Patent number: 5633248
    Abstract: A compound of the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; P and Q independently represent a divalent aliphatic hydrocarbon group having at least 2 carbon atoms and optionally having either oxygen or sulfur in the carbon chain; R.sup.1 and R.sup.3 independently represent --CO--R, --CONH--R (R represents a hydrocarbon group or a heterocyclic group) or a hydrocarbon group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4, taken together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic group; and j represents 0 or 1, or a salt thereof, has excellent GnRH-receptor antagonizing activity and is useful as a prophylactic and therapeutic agent for hormone-dependent and other diseases.
    Type: Grant
    Filed: November 21, 1995
    Date of Patent: May 27, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato
  • Patent number: 5563139
    Abstract: Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein A is selected from ##STR2## wherein m is one; wherein R.sup.1 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, benzyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R.sup.
    Type: Grant
    Filed: June 14, 1993
    Date of Patent: October 8, 1996
    Assignee: G. D. Searle & Co.
    Inventor: David B. Reitz
  • Patent number: 5489603
    Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.
    Type: Grant
    Filed: July 15, 1993
    Date of Patent: February 6, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideki Uneme, Koichi Iwanaga, Noriko Higuchi, Isao Minamida, Tetsuo Okauchi
  • Patent number: 5470984
    Abstract: This invention relates to 1-dimethylcarbamoyl-3-substituted-5-substituted-1H-1,2,4-triazoles as defined herein, compositions containing those compounds and methods of use.
    Type: Grant
    Filed: May 10, 1994
    Date of Patent: November 28, 1995
    Assignee: Shell Research Limited
    Inventors: Richard M. Jacobson, J. Roger Ramsay, Harold E. Aller, Muthuvelu Thirugnanam
  • Patent number: 5420099
    Abstract: A compound having the formula ##STR1## wherein A is CR.sub.7 ; and R.sup.1 through R.sup.7 are substituents such as hydrogen, halogen, branched and straight chain hydrocarbons, cyclic hydrocarbons, aromatics, and sulfur and nitrogen containing functional groups. Further, R.sup.5 and R.sup.6 may be taken together with the atom to which they are attached to form a group ##STR2## in which R.sup.9 and R.sup.10 are further functional groups. The compounds are useful in herbicidal compositions, particularly in combination with carriers and surfactants. A process for making this compound is also presented.
    Type: Grant
    Filed: December 21, 1992
    Date of Patent: May 30, 1995
    Assignee: Shell Research Limited
    Inventor: Trevor W. Newton
  • Patent number: 5319092
    Abstract: This invention relates to 1-dimethylcarbamoyl-3-substituted-5-substituted-1H-1,2,4-triazoles as defined herein, compositions containing those compounds and methods of use.
    Type: Grant
    Filed: October 22, 1990
    Date of Patent: June 7, 1994
    Assignee: Shell Research Limited
    Inventors: Richard M. Jacobson, J. Roger Ramsay, Harold E. Aller, Muthuvelu Thirugnanam
  • Patent number: 5290931
    Abstract: Water-insoluble naphthalic acid imide dyestuffs of the following formula: ##STR1## wherein D is ##STR2## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl which may be substituted, R.sup.2 is hydrogen, halogen, lower alkyl, lower alkoxy or cyano, X is oxygen or sulfur, and m is 0 or 1; A is phenylene, alkylene, aralkylene or --C.sub.2 H.sub.4 OC.sub.2 H.sub.4 --; B is oxygen, sulfur or ##STR3## wherein R.sup.3 is hydrogen or lower alkyl; Y is a 6-membered nitrogen-containing heterocyclic ring having at least one active halogen atom; and n is 0 or 1.
    Type: Grant
    Filed: September 4, 1992
    Date of Patent: March 1, 1994
    Assignee: Hoechst Mitsubishi Kasei Co., Ltd.
    Inventors: Kiyoshi Himeno, Toshio Hihara
  • Patent number: 5256667
    Abstract: Substituted quinazolinones and pyridopyrimidines of structural formula I ##STR1## are angiotensin II antagonists useful in the treatment of disorders related to the renin-angiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.
    Type: Grant
    Filed: July 31, 1992
    Date of Patent: October 26, 1993
    Assignees: Merck & Co., Inc., E. I. Du Pont De Nemours & Co.
    Inventors: Eric E. Allen, Richard E. Olson
  • Patent number: 5188832
    Abstract: A method of using certain triazine-dione compounds for the control of endo- and ectoparasites of fish and/or insects. The compounds may be combined with aids to form an agent for controlling the endo- or ectoparasites.
    Type: Grant
    Filed: February 14, 1990
    Date of Patent: February 23, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz Mehlhorn, Horst Taraschewski, Gunter Schmahl, Wolfgang Raether, Manfred Rosner
  • Patent number: 5102880
    Abstract: Substituted Imidazo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogren atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
    Type: Grant
    Filed: September 5, 1991
    Date of Patent: April 7, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Thomas F. Walsh
  • Patent number: 5047404
    Abstract: This invention relates to fused pyrimidine derivatives which have bronchodilator and anti-allergic activities. A compound of the invention is 2-(2-propoxyphenyl)pyrido[2,3-d]pyrimid-4(3H)-one.
    Type: Grant
    Filed: June 13, 1989
    Date of Patent: September 10, 1991
    Assignee: Smith Kline & French Laboratories, Ltd.
    Inventors: William J. Coates, Sean T. Flynn, Derek A. Rawlings
  • Patent number: 5043443
    Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.
    Type: Grant
    Filed: July 24, 1990
    Date of Patent: August 27, 1991
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventors: Randall K. Carlson, Chung-Ho Park, Walter A. Gregory
  • Patent number: 4994448
    Abstract: The new compounds of the general Formula I ##STR1## (wherein R.sub.1 stands for C.sub.1-4 alkyl or aralkyl; andR.sub.2 represents hydroxy; orR.sub.1 and R.sub.2 together form a valency bond;R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl, amino, alkylthio or a group of the Formula --NR.sub.7 R.sub.8 in which R.sub.7 and R.sub.8 may be the same or different and stand for hydrogen, C.sub.1-4 alkyl, phenyl-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl or di-(C.sub.1-4 alkyl)-amino-C.sub.1-4 alkyl or together with the nitrogen atom they are attached to form a 6-membered heterocyclic ring which may optionally contain a further nitrogen, oxygen or sulfur atom; orR.sub.2 and R.sub.3 together form an oxo (.dbd.O) or thixo (.dbd.S) group;R.sub.4 represents hydrogen, C.sub.1-4 alkyl or phenyl which may optionally bear one or two halogen or nitro substituent(s);Z is a group of the Formula (a) or (b) ##STR2## A.sup.
    Type: Grant
    Filed: September 30, 1988
    Date of Patent: February 19, 1991
    Assignee: Egis Gyogyszergyar
    Inventors: Andras Messmer, Gyorgy Hajos, Zsuzsa Juhasz nee Riedl, Pal Benko, Laszlo Pallos, Lujza Petocz, Eniko Szirt nee Kiszelly, Gabor Gigler, Istvan Gyertyan, Maria Hegedus
  • Patent number: 4921527
    Abstract: The invention relates to sulfonylurea compounds with a substituted or unsubstituted bicyclic nine-membered ring having one to five heteroatoms which are preemergent and/or postemergent herbicides or plant growth regulants.
    Type: Grant
    Filed: May 4, 1988
    Date of Patent: May 1, 1990
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 4916129
    Abstract: Imidazole compounds such as ##STR1## which have angiotensin II antagonizing properties as well as .beta.-adrenoceptor antagonizing properties are useful as antihypertensives and for treatment of congestive heart failure.
    Type: Grant
    Filed: January 19, 1989
    Date of Patent: April 10, 1990
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: David J. Carini, John J. V. Duncia
  • Patent number: 4912106
    Abstract: Novel 5,6-dihydro-2-(substituted phenyl)-1,2,4-triazine-3,5(2H, 4H)-diones which are effective in destroying or preventing the growth of Protozoa in subjects suffering from such Protozoa.
    Type: Grant
    Filed: April 22, 1988
    Date of Patent: March 27, 1990
    Assignee: Janssen Pharmaceutica N. V. Frame-319
    Inventors: Gustaaf M. Boeckx, Alfons H. M. Raeymaekers, Victor Sipido
  • Patent number: 4908056
    Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.
    Type: Grant
    Filed: February 17, 1989
    Date of Patent: March 13, 1990
    Assignee: E. I. Du Pont De Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 4908364
    Abstract: Novel substituted 3-phenyl-7H-thiazolo[3,2-b][1,2,4]-triazin-7-ones of the formula I are disclosed ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the meaning recited in the specification. The compounds are suitable for prevention and treatment of inflammatory disorders.
    Type: Grant
    Filed: January 28, 1988
    Date of Patent: March 13, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Werner Thorwart, Ulrich Gebert, Rudolf Schleyerbach, Robert R. Bartlett
  • Patent number: 4898862
    Abstract: Compounds of formula (I): ##STR1## (in which: R.sup.1 is hydrogen or alkl; R.sup.2 is a variety of groups or atoms; R.sup.3 is optionally substituted hydroxy or --(NH).sub.n --NR.sup.5 R.sup.6, wherein R.sup.5 and R.sup.6 are a variety of groups or atoms, preferably alkyl substituted by heterocyclic, and n is 0 or 1; Q is oxygen or sulfur; and A is a C.sub.1 -C.sub.6 alkylene group) have valuable cardiotionic activity and may be used for the treatment of cardiac disorders. They may be prepared from corresponding compounds containing a benzene ring with a group --QH at the 1-position and a group --CO--CHR.sup.1 --NH--COOR.sup.7 at the 4-position by ring closure and introduction of the group of formula --A--CO--R.sup.3 in any order.
    Type: Grant
    Filed: March 16, 1987
    Date of Patent: February 6, 1990
    Assignee: Sankyo Company Limited
    Inventors: Yasuhiro Morisawa, Mitsuru Kataoka, Mitsuo Sugiyama, Fujio Saito, Hiroyuki Koike, Takeshi Oshima, Yasuo Simoji, Hitoshi Nagahori
  • Patent number: 4892946
    Abstract: N-(heterocyclicaminocarbonyl)arylsulfonamides in which the aryl radical is substituted in the 2-position by a carboxy radical, ester, thioester, or amide thereof; e.g. N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonylbenzenesulf onamide or N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-2-methoxycarbonylbenze nesulfonamide; are useful for the regulation of plant growth and as pre-emergence and post-emergence herbicides.
    Type: Grant
    Filed: November 24, 1980
    Date of Patent: January 9, 1990
    Assignee: E. I. Du Pont De Nemours and Company
    Inventor: George Levitt
  • Patent number: 4870174
    Abstract: The synthesis of 7-n-alkyl-imidazolium[4,5-d]-pyrimidines, 6-substituted-3n-alkyl-benzimidazolium- and 3n-alkyl-5,6-substituted-benzthiazolium salts are described. There N.sup.+ -surfactants having a substituted heterocycle as a head group have distinguished small critical micelle concentrations (CMC) in the range of 10.sup.-5 -10.sup.-7 Mol/Liter. The size and shape of these micelles in watery solutions are determined by the nature of the anion. The N-surfactants can be used as pharmaceuticals as well as reporter groups in fluorescence studies including immunological assays.
    Type: Grant
    Filed: August 6, 1987
    Date of Patent: September 26, 1989
    Assignee: Medice chem.-pharm. Fabrik
    Inventor: Henrich H. Paradies
  • Patent number: 4853394
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof:Ar--CO--X--Y--Z--OR.sub.1 (I)wherein: Ar is a group of formula (a): ##STR1## wherein either R.sub.2 is C.sub.1-6 alkoxy and one of R.sub.3, R.sub.4 and R.sub.5 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, CX.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-6 alkoxy, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O)n wherein n is 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.2 is hydrogen and R.sub.3, R.sub.4 and R.sub.5 are independently selected from hydrogen, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or halo; or any two on adjacent carbon atoms together are C.sub.
    Type: Grant
    Filed: November 3, 1986
    Date of Patent: August 1, 1989
    Assignee: Beecham Group p.l.c.
    Inventors: Francis D. King, Roger T. Martin, Eric A. Watts
  • Patent number: 4782056
    Abstract: Compounds of the formula I ##STR1## with n=1-3, R=H, Hal, CF.sub.3, alkyl, cycloalkyl, alkyloxy, alkylthio, alkylsulfinyl, alkylsulfonyl, benzylsulfinyl, benzylsulfonyl, nitro, cyano, amino, alkylamino, dialkylamino, piperidino, morpholino, pyrrolidinyl, 4-methyl-1-piperazinyl, acylamino or substituted phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl, benzoyl, benzoylamino or anilino, with R.sup.2 =H, alkyl, cycloalkyl, optionally substituted benzyl, alkanoyl or benzoyl and R.sup.3 =H, alkyl, cycloalkyl or optionally substituted benzyl, at least R.sup.2 or R.sup.3 not being H, are obtained by alkylation or acylation of a compound II ##STR2## in which R.sup.1 is as defined above, with compounds R.sup.3 X (X=leaving group) or R.sup.2 Y (Y=leaving group), R.sup.2 and R.sup.3 being defined as indicated.Compounds I are coccidiostatics.
    Type: Grant
    Filed: September 5, 1986
    Date of Patent: November 1, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Manfred Rosner, Wolfgang Raether
  • Patent number: 4698352
    Abstract: This invention relates to a novel 4-oxo-1,4-dihydronicotinic acid derivative ##STR1## or a salt thereof, wherein R.sup.1 is hydrogen or carboxyl-protecting group;R.sup.2 is substituted phenyl and naphthyl, or a substituted or unsubstituted heterocyclic group; andR.sup.3 is haloalkyl, aminoalkyl, or substituted or unsubstituted alkenyl, phenylalkenyl, naphthylalkenyl, phenylalkyl, naphthylalkyl, phenylalkynyl, naphthylalkynyl, heterocyclic alkyl, heterocyclic alkenyl, phenyl, naphthyl, cycloalkyl, cycloalkenyl, carboxylic acyl, iminoalkyl, heterocyclic or bridged hydrocarbon, which has a broad antibacterial spectrum and a low toxicity, and are useful for treatment of diseases of human beings and animals, to a process for producing the same and to an antibacterial agent containing the same.
    Type: Grant
    Filed: October 27, 1983
    Date of Patent: October 6, 1987
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Hirokazu Narita, Yoshinori Konishi, Jun Nitta, Shunjiro Misumi, Hideyoshi Nagaki, Isao Kitayama, Yoriko Nagai, Yasuo Watanabe, Nobuyuki Matsubara, Shinzaburo Minami, Isamu Saikawa
  • Patent number: 4689072
    Abstract: N-(heterocyclicaminocarbonyl)arylsulfonamides in which the aryl radical is substiuted in the 2-position by a carboxy radical, ester, thioester, or amide thereof; e.g. N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonylbenzenesulf onamide or N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-2-methoxycarbonylbenze nesulfonamide; are useful for the regulation of plant growth and as pre-emergence and post-emergence herbicides.
    Type: Grant
    Filed: July 30, 1986
    Date of Patent: August 25, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: George Levitt
  • Patent number: 4689414
    Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;R.sub.5 is hydrogen, alkyl, aryl, arylalkyl, cyano, nitro, ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl-(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## amino, or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.
    Type: Grant
    Filed: February 24, 1986
    Date of Patent: August 25, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4684656
    Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR2## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.
    Type: Grant
    Filed: March 14, 1986
    Date of Patent: August 4, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4683228
    Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: July 28, 1987
    Assignees: ICI Americas Inc., Imperial Chemical Industries PLC
    Inventors: Karin M. Kirkland, Derrick M. Mant
  • Patent number: 4640917
    Abstract: Substituted 2-phenyl-hexahydro-1,2,4-triazine-3,5-diones of the formula ##STR1## in which n is one, two or three and the individual substituents R are independently of one another (a) hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, alkyl having 1 to 6 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, alkoxy, alkylthio, alkylsulfinyl or alkylsulfonyl each having 1 to 6 carbon atoms in the alkyl moiety, nitro, cyano, amino, alkylamino or dialkylamino each having 1 to 12 carbon atoms in the alkyl moiety, piperidino, morpholino, thiomorpholino, 1-pyrrolidinyl, 4-methyl-1-piperazinyl or acylamino having 1 to 6 carbon atoms in the acyl moiety, or (b) a phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl, benzoyl, benzoylamino or aniline radical which is in each case R.sub.(a) -substituted, and the alkali metal salts, alkaline earth metal salts or ammonium salts thereof, a process for their preparation, their use, veterinary drugs and a process for controlling protozoal diseases.
    Type: Grant
    Filed: March 8, 1985
    Date of Patent: February 3, 1987
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Manfred Rosner, Wolfgang Raether
  • Patent number: 4622397
    Abstract: The invention relates to a process for the preparation of aminotriazinone derivatives of the formula I ##STR1## wherein R.sub.1 and R.sub.2 are each independently alkyl, cycloalkyl, aralkyl or aryl, andR.sub.3 and R.sub.4 are each independently hydrogen, alkyl or cycloalkyl, or together with the nitrogen atom to which they are attached are a piperidine or morpholine ring, which process comprises phosgenating a compound of formula II ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, and reacting the resultant compound of formula III ##STR3## wherein R.sub.1 and R.sub.2 are as defined above, without isolation or after isolation, with a compound of formula IV ##STR4## wherein R.sub.3 and R.sub.4 are as defined above. The invention also relates to the novel compounds of formula I and to the use thereof for controlling undesirable plant growth, as well as to compounds of the formula III.
    Type: Grant
    Filed: July 5, 1985
    Date of Patent: November 11, 1986
    Assignee: Ciba-Geigy Corporation
    Inventor: Beat Bohner
  • Patent number: 4616002
    Abstract: Compounds of the formula I ##STR1## in which n represents 1, 2 or 3, Ar represents a carbocyclic or heterocyclic aryl radical, Ac represents the acyl radical of an acid, Z represents a radical --OR.sub.7 or --NR.sub.8 R.sub.9, R.sub.1 represents hydrogen, unsubstituted or substituted lower alkyl, a carbocyclic or heterocyclic aryl radical or free, etherified or esterified hydroxy, R.sub.2 and R.sub.3, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl, formyl or functionally modified formyl, carboxy or functionally modified carboxy, a carbocyclic or heterocyclic aryl radical or unsubstituted or mono- or di-substituted amino, R.sub.4 represents hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl or a carbocyclic or heterocyclic aryl radical, R.sub.7, R.sub.8 and R.sub.
    Type: Grant
    Filed: January 6, 1986
    Date of Patent: October 7, 1986
    Assignee: Ciba-Geigy Corporation
    Inventors: Bruno Kamber, Thomas Leutert, Hans Kuhnis, Kurt Eichenberger
  • Patent number: 4585861
    Abstract: This invention relates to certain amino-5,6-diaryl-1,2,4-triazines and -pyrazines useful as activators of GABA and benzodiazepine binding.
    Type: Grant
    Filed: January 4, 1985
    Date of Patent: April 29, 1986
    Assignee: Eli Lilly and Company
    Inventors: David T. Wong, William B. Lacefield