Three-membered Ring In R Patents (Class 514/624)
  • Patent number: 6313163
    Abstract: Compounds of formula 1 wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, Y is cyclopropyl optionally substituted with one or two R4 groups, the divalent Y radical being substituted by the Z and —CR1═CR1—CR1═CR1 groups on adjacent carbons; X is S, O, or NR5; n is 1 or 2; R1 and R2 independently are H, lower alkyl or fluoroalkyl; R3 is hydrogen, lower alkyl, Cl or Br; R4 is lower alkyl, fluoroalkyl or halogen; R5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR8, CONR9R10, —CH2OH, CH2OR11, CH2OCOR11, CHO, CH(OR12)2, CHOR13O, 13 COR7, CR7(OR12)2, CR7OR13O, or tri-lower alkylsilyl, where R7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R8 is phenyl or lower alkylphenyl, R9 and R10 indep
    Type: Grant
    Filed: August 17, 2000
    Date of Patent: November 6, 2001
    Assignee: Allergen Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 6262104
    Abstract: Compounds, or solvates or salts thereof, of formula (I): selective delta opioid agonists and antagonists and may be of therapeutic utility as analgesics, immunosuppressants to prevent rejection in organ transplant and skin graft, anti-allergic and anti-inflammatory agents, brain cell protectants, agents for treating drug and alcohol abuse, gastritis, diarrhoea, cardiovascular and respiratory diseases, cough, mental illness, epilepsy and, in general, agents for the treatment of those pathological conditions which, customarily, can be treated with agonists and antagonists of the delta opioid receptor.
    Type: Grant
    Filed: June 5, 1998
    Date of Patent: July 17, 2001
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Giulio Dondio, Silvano Ronzoni
  • Patent number: 6262091
    Abstract: Compositions for controlling harmful fungi, containing in a solid or liquid carrier a) at least one p-hydroxyaniline derivative of the formula I b) at least one amide compound of the formula II A—CO—NR8—R9  (II) where the substituents have the meanings indicated in the description; and methods of controlling harmful fungi using compositions of this type are described.
    Type: Grant
    Filed: October 21, 1998
    Date of Patent: July 17, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Oliver Wagner, Karl Eicken, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Harald Köhle, Günter Retzlaff
  • Patent number: 6251947
    Abstract: Compounds of Formula (I) are disclosed which are useful as fungicides, wherein Q is: (Q−1) or (Q−2), Z is (Z−1); (Z−2); (Z−3) or (Z−4); X is —O—, —CH(R11)— or ═C(R11)—; R1 is H or C1-C2 alkyl; R2 is H; C1-C6 alkyl; C3-C6 cycloalkyl; or phenyl optionally substituted with halogen, cyano, C1-C2 alkyl or C1-C2 alkoxy; and R3-R11 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula (I).
    Type: Grant
    Filed: August 4, 1999
    Date of Patent: June 26, 2001
    Assignee: Board of Trustees of the University of Arkansas
    Inventors: Gregory Steven Basarab, Douglas Brian Jordan, Thomas Arend Lessen, Stephen L. Hansen
  • Patent number: 6235789
    Abstract: A compound of the formula wherein R1 and R2 are H, a hydrocarbon group or a heterocyclic group, or R1 and R2 are combinedly a spiro ring; R3 is a hydrocarbon group, a substituted amino group, a substituted hydroxyl group or a heterocyclic group; R4 is H or alkyl; ring A is a substituted benzene ring; m and n denote 1 to 4; {overscore (.........)} means a single or double bond or a salt, a process of producing thereof and a composition having a binding affinity for melatonin receptor.
    Type: Grant
    Filed: May 28, 1997
    Date of Patent: May 22, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigenori Ohkawa, Osamu Uchikawa, Masaomi Miyamoto
  • Patent number: 6214869
    Abstract: There is provided a novel series of cis cyclopropane compounds of Formula I wherein R1, R2, R3, R4, X, Y, Z and m are as defined herein which bind to the human melatonin receptor and therefore are useful as melatonergic agents.
    Type: Grant
    Filed: May 25, 1999
    Date of Patent: April 10, 2001
    Assignee: Bristol-Myers Squibb
    Inventors: Jie Chen, Pierre Dextraze, Marco Dodier, Katherine S. Takaki
  • Patent number: 6143789
    Abstract: Compound of formula (I): ##STR1## wherein: T represents alkylene,A and B together form a naphthalene, dihydronaphthalene, or tetrahydronaphthalene group,R represents hydrogen, hydroxy, R' or OR', R' being as defined in the description,G.sub.1 represents halogen, a radical R.sub.1 or a group --O--CO--R.sub.1, R.sub.1 being as defined in the description,G.sub.2 represents a group selected from: ##STR2## X, R.sub.2 and R.sub.21 being as defined in the description, and medicinal products containing the same which are useful in the treatment of a condition related to the melatoninergic system.
    Type: Grant
    Filed: November 25, 1998
    Date of Patent: November 7, 2000
    Assignee: Adir et Compagnie
    Inventors: Fran.cedilla.ois Lefoulon, Luc Demuynck, Daniel Lesieur, Patrick Depreux, Caroline Bennejean, Pierre Renard, Philippe Delagrange
  • Patent number: 6090854
    Abstract: There is provided novel aryloxyanilides and related compounds of the formula ##STR1## wherein R.sup.1 is --OR, --CO.sub.2 R, or halogen with R being C.sub.1-4 alkyl;R.sup.2 is R, cyclopropyl, C.sub.2-4 alkenyl or --CH.sub.2 OR; andX is O, S, CH.sub.2, NR, SO, SO.sub.2 or COwhich are melatonergic agents and are useful in the treatment of circadian rhythm-related disorders and other conditions affected by melatonin activity.
    Type: Grant
    Filed: January 22, 1999
    Date of Patent: July 18, 2000
    Assignee: Bristol-Meyers Company
    Inventor: James R. Epperson
  • Patent number: 6028112
    Abstract: There is provided novel spirocyclopropyl fluorene derivatives having the general Formula I ##STR1## wherein R, R.sup.1 and X are as defined herein which are useful as melatonergic agents.
    Type: Grant
    Filed: July 31, 1998
    Date of Patent: February 22, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Karen L. Leboulluec, Katherine S. Takaki
  • Patent number: 5965621
    Abstract: A method for reducing or maintaining the level of adipose tissue formation in a mammal includes the step of administering a pantethine composition to the mammal in an amount and for a period of time sufficient to achieve a desired body weight. Compositions useful in carrying out the method include an adipose modulating amount of the pantethine component and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: April 30, 1998
    Date of Patent: October 12, 1999
    Assignee: Allergan
    Inventor: Lidija Balodis
  • Patent number: 5962413
    Abstract: Dysmenorrhea, disfunctional uterine bleeding, preterm labor and postpartum labor in female mammals are treated by inhibiting uterine contractility by administering thereto a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in combination with one or more of a prostaglandin inhibitor, a prostacyclin-mimetic, a progestin, an oxytocin antagonist or a .beta.-agonist in an amount effective to ameliorate the symptoms thereof; and inadequate menses treated and induction of abortion or stimulation of labor in a pregnant female is achieved by uterine contractility stimulation by administering thereto a nitric oxide inhibitor, either alone or optionally in a combination of progesterone antagonist, an oxytocin or oxytocin analogue antagonist or a prostaglandin.
    Type: Grant
    Filed: September 22, 1997
    Date of Patent: October 5, 1999
    Assignees: Schering Aktiengesellschaft, The University of Texas System
    Inventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
  • Patent number: 5929119
    Abstract: A composition which is suitable for controlling fungal pests, comprising conventional additives and an effective amount of a p-hydroxyaniline derivative of the general formula I ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted bicycloalkyl, unsubstituted or substituted bicycloalkenyl;R.sup.2 and R.sup.3 independently of one another are halogen, alkyl, haloalkyl, alkoxy or haloalkoxy,and a liquid or solid carrier, its use, the use of the compounds I for controlling fungal pests, and the use of the compounds I for the preparation of the compositions.
    Type: Grant
    Filed: August 11, 1997
    Date of Patent: July 27, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Oliver Wagner, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5925674
    Abstract: This invention relates to cycloalkylcarboxanilides of the formula ##STR1## which are used to combat pests.
    Type: Grant
    Filed: October 26, 1995
    Date of Patent: July 20, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Krueger, Klaus Sasse, Thomas Schenke, Michael Negele, Heinz-Wilhelm Dehne
  • Patent number: 5922771
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.
    Type: Grant
    Filed: August 19, 1996
    Date of Patent: July 13, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
  • Patent number: 5885621
    Abstract: Disclosed are methods for treating a patient identified as having a hemoglobinopathy that is characterized by a reduced affinity of hemoglobin for oxygen. The methods involve providing gaseous nitric oxide and/or carbon monoxide for (i) inhalation by the patient or (ii) ex vivo treatment of the patient's erythrocytes. Alternatively, a nitric-oxide-releasing compound can be administered to the patient.
    Type: Grant
    Filed: April 4, 1997
    Date of Patent: March 23, 1999
    Assignee: The General Hospital Corporation
    Inventors: C. Alvin Head, Warren M. Zapol
  • Patent number: 5880157
    Abstract: The present invention relates to derivatives of 2,2,3,3-tetramethylcyclopropane carboxylic acid (TMCA) of general formula (I), ##STR1## wherein R is lower alkyl group (C.sub.1 -C.sub.6), an aryl group, an aralkyl group or an amide of general formula (II), ##STR2## where R.sub.1 and R.sub.2 are the same or different and may be hydrogen, a alkyl group (C.sub.1 -C.sub.6), an aryl group or an aralkyl group, and n=0-3, to their racemic mixtures and the D and L enantiomers. The invention also relates to processes for the preparation of said compounds and for pharmaceutical preparations comprising the same. The new compounds show improved activity against epilepsy.
    Type: Grant
    Filed: November 25, 1996
    Date of Patent: March 9, 1999
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Jeff Sterling, Yaacov Herzig, Meir Bialer, Abdullah Haj-Yehia, Boris Yagen
  • Patent number: 5780512
    Abstract: The invention relates to a compounds selected from these of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and A are as defined in the description, and a medicinal product containing the same useful for treating a melatoninergic disorder.
    Type: Grant
    Filed: March 26, 1997
    Date of Patent: July 14, 1998
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Eric Fourmaintraux, Patrick Depreux, Philippe Delagrange, Pierre Renard, Beatrice Guardiola-Lemaitre
  • Patent number: 5763466
    Abstract: A novel fungicidal composition comprising a fungicidally effective amount of a combination consisting of(i) N-?1-(4-chloro-phenyl)-ethyl!-2,2-dichloro-1-ethyl-3-methyl-cyclopropaneca rboxamide of the formula ##STR1## and (ii) (A) a triazole derivative of the formula ##STR2## in which X represents chlorine or phenyl,and/or(B) a pyrrole derivative of the formula ##STR3## in which R represents ##STR4## and/or (C) the imidazole derivative of the formula ##STR5## The novel composition shows a synergistic activity.
    Type: Grant
    Filed: July 8, 1997
    Date of Patent: June 9, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerd Hanssler, Stefan Dutzmann, Matthias Wunsch
  • Patent number: 5753709
    Abstract: Certain N-acyl 2-aryl cyclopropylmethylamine derivatives are useful as melatonergic agents.
    Type: Grant
    Filed: May 9, 1996
    Date of Patent: May 19, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: Daniel J. Keavy, Michael F. Parker, Ronald J. Mattson, Graham Johnson
  • Patent number: 5736578
    Abstract: Novel substituted fluorene compunds of Formula I are active as melatonergic agents: ##STR1## wherein: X=H, halogen, OH or OZ;Z=C.sub.1-6 alkyl; --(CH.sub.2).sub.m --CF.sub.3 (m=0-2); CD.sub.3 ; or ##STR2## n=1 or 2; and R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, halogen substituted C.sub.1-6 alkyl, or C.sub.1-6 alkoxy substituted C.sub.1-6 alkyl.
    Type: Grant
    Filed: May 10, 1996
    Date of Patent: April 7, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: Brett T. Watson, Katherine S. Takaki, Joseph P. Yevich, James R. Epperson, George N. Karageorge, Karen L. Leboulluec
  • Patent number: 5696150
    Abstract: A novel fungicidal composition comprising a fungicidally effective amount of a combination consisting of(i) N-?1-(4-chloro-phenyl)-ethyl!-2,2-dichloro-1-ethyl-3-methyl-cyclopropaneca rboxamide of the formula ##STR1## and (ii) (A) a triazole derivative of the formula ##STR2## in which X represents chlorine or phenyl, and/or (B) a pyrrole derivative of the formula ##STR3## in which R represents ##STR4## and/or (C) the imidazole derivative of the formula ##STR5## The novel composition shows a synergistic activity.
    Type: Grant
    Filed: September 13, 1996
    Date of Patent: December 9, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerd Hanssler, Stefan Dutzmann, Matthias Wunsch
  • Patent number: 5693630
    Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.
    Type: Grant
    Filed: October 26, 1994
    Date of Patent: December 2, 1997
    Assignee: Astra Aktiebolag
    Inventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
  • Patent number: 5661186
    Abstract: Certain tetralinyl- and indanyl-ethylamides are useful central nervous system agents.
    Type: Grant
    Filed: December 21, 1995
    Date of Patent: August 26, 1997
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Katherine S. Takaki, Brett T. Watson, Graham S. Poindexter, James R. Epperson
  • Patent number: 5612368
    Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which Ar, X, R.sub.1 and R.sub.2 are as defined in the description and a medicinal product containing the same in order to treat a disorder of the melatoninergic system.
    Type: Grant
    Filed: October 25, 1995
    Date of Patent: March 18, 1997
    Assignee: Adir et Compagnie
    Inventors: Jean Andrieux, Michel Langlois, Pierre Renard, Philippe Delagrange
  • Patent number: 5578595
    Abstract: Novel 2-(2,2-difluorocyclopropyl)-acetic acid derivatives of formula I ##STR1## wherein A is oxygen or --NR.sub.1 --,B is C.sub.2 -C.sub.6 alkylene,D is oxygen, sulfur or --O--CH.sub.2 --,E is phenyl; phenyl substituted by from one to three substituents selected from the group halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 haloalkyl and C.sub.1 -C.sub.4 alkoxy; a five-membered aromatic heterocycle having from one to three hetero atoms selected from the group nitrogen, oxygen and sulfur; a five-membered aromatic heterocycle having from one to three hetero atoms selected from the group nitrogen, oxygen and sulfur that is substituted by one or two substituents selected from the group halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.3 haloalkyl; a six-membered aromatic heterocycle having from one to three nitrogen atoms; or a six-membered aromatic heterocycle having from one to three nitrogen atoms that is substituted by one or two substituents selected from the group halogen, C.sub.1 -C.sub.4 alkyl and C.
    Type: Grant
    Filed: March 21, 1995
    Date of Patent: November 26, 1996
    Assignee: Ciba-Geigy Corporation
    Inventor: Manfred B oger
  • Patent number: 5567735
    Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 22, 1996
    Assignee: Imperial Chemical Industries PLC
    Inventors: Keith Russell, Cyrus J. Ohnmacht, Keith H. Gibson
  • Patent number: 5554642
    Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description,its optical isomers and its addition salts thereof with a pharmaceuticaliy-accepable acid or base,and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: September 10, 1996
    Assignee: Adir et Compagnie
    Inventors: Michel Langlois, Pierre Renard, G erard Adam
  • Patent number: 5547984
    Abstract: Certain N-acetonyl-substituted-amides of the formula: ##STR1## wherein A is a heterocycle, a phenylalkyl, a phenylalkoxy, naphthyl, cycloalkyl, alkoxyalkyl, alkyl, haloalkyl or alkenyl group; X, Y and Z are selected from the group consisting of hydrogen, halo, cyano, thiocyano, isothiocyano, methylsulfonyloxy, thio(C.sub.1 -C.sub.2)alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyl, dithiocarbamoyl, hydroxy, azide, trifluoromethylcarboxy, (C.sub.1 -C.sub.4)alkylcarbonyloxy, phenylcarbonyloxy, phenoxy, thiophenyl, imidazolyl or triazolyl group as described herein; R.sup.1 and R.sup.2 are each independently a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group; and compositions containing these amides are fungicidally active, particularly against phytopathogenic fungi.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 20, 1996
    Assignee: Rohm and Haas Company
    Inventor: Ashok K. Sharma
  • Patent number: 5541228
    Abstract: New melatonergic agents are phenyl alkanyl or phenyl alkyl substituted carboxamides and ureas of Formula I: ##STR1## wherein: R.sub.1 =C.sub.1-3 alkyl, allyl, C.sub.3-6 cycloalkyl substituted C.sub.1-4 alkyl;R.sub.2 =hydrogen, halogen or C.sub.1-4 alkoxy;R.sub.3 =hydrogen or C.sub.1-4 alkyl;R.sub.4 =C.sub.1-4 alkyl, C.sub.1-4 alkyl substituted amino, carboxylic acid substitutedC.sub.1-4 alkyl or C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl, or straight or branched chain C.sub.2-4 alkenyl;A=a linear C.sub.2-4 alkanediyl or alkenediyl chain, provided that A not be --CH.sub.2 CH.sub.2 -- when X is a bond; andX=a covalent bond or oxygen.
    Type: Grant
    Filed: March 8, 1995
    Date of Patent: July 30, 1996
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Katherine S, Takaki, George N. Karageorge, Daniel J. Keavy, Michael F. Parker, Brett T. Watson
  • Patent number: 5532264
    Abstract: The power of fluoxetine, venlafaxine, milnacipran and duloxetine to increase the availability of serotonin, norepinephrine and dopamine, particularly serotonin, is augmented by administration in combination with a drug which is a serotonin 1A receptor antagonist.
    Type: Grant
    Filed: May 17, 1995
    Date of Patent: July 2, 1996
    Assignee: Eli Lilly and Company
    Inventors: David T. Wong, Juan I. Oguiza
  • Patent number: 5532250
    Abstract: The power of fluoxetine, venlafaxine, milnacipran and duloxetine to increase the availability of serotonin, norepinephrine and dopamine, particularly serotonin, is augmented by administration in combination with a drug which is a serotonin 1A receptor antagonist.
    Type: Grant
    Filed: May 17, 1995
    Date of Patent: July 2, 1996
    Assignee: Eli Lilly and Company
    Inventors: David T. Wong, Juan I. Oguiza
  • Patent number: 5492931
    Abstract: This invention relates to cycloalkylcarboxanilides of the formula ##STR1## in which R represents halogen or halogenoalkyl,R.sup.1 represents halogen, alkyl or halogenoalkyl,n represents the numbers 0, 1, 2 or 3,X.sup.1, X.sup.2, X.sup.3 and X.sup.4 independently of one another represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio or halogenoalkylthio, andZ represents hydrogen,which have the utility as pesticides and fungicides.
    Type: Grant
    Filed: January 21, 1994
    Date of Patent: February 20, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Krueger, Klaus Sasse, Thomas Schenke, Michael Negele, Heinz-Wilhelm Dehne
  • Patent number: 5464872
    Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: November 7, 1995
    Assignee: Adir et Compagnie
    Inventors: Michel Langlois, Pierre Renard, Gerard Adam
  • Patent number: 5455273
    Abstract: The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: October 3, 1995
    Assignee: Karl Thomae GmbH
    Inventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
  • Patent number: 5434190
    Abstract: N-monosubstituted neoalkanamides of 11 to 14 carbon atoms wherein the substituent on the amide nitrogen is cyclic (aromatic or cycloaliphatic, such as aryl or cycloalkyl) and of at least five carbon atoms, have been discovered to be insect repellent, providing that any aromatic substituent is unsubstituted at the ortho position and that when the neoalkanoyl moiety is pivaloyl the total number of carbon atoms in the N-cyclic neoalkanamide is at least 12. Such neoalkanamides are useful as repellents against cockroaches, including American, German and Oriental cockroaches, and are also effective against mosquitoes (both Anopheles and Aedes), black flies and carpenter ants, and to some extent against deer ticks. They may be applied to areas, locations and items which are desirably to be kept free of such insects, with applications being direct or of solutions or emulsions thereof, preferably by spraying, or in detergent compositions or other products to be applied to such areas, etc.
    Type: Grant
    Filed: October 11, 1994
    Date of Patent: July 18, 1995
    Assignee: Colgate-Palmolive Co.
    Inventor: Robert J. Steltenkamp
  • Patent number: 5382598
    Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolyzable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.
    Type: Grant
    Filed: September 24, 1993
    Date of Patent: January 17, 1995
    Assignees: Imperial Chemical Industries PLC, Imperial Chemical House
    Inventors: Russell Keith, Cyrus J. Ohnmacht, Keith H. Gibson
  • Patent number: 5356930
    Abstract: An amide derivative of the formula: ##STR1## which is useful for control of insect pests.
    Type: Grant
    Filed: August 5, 1993
    Date of Patent: October 18, 1994
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hiroshi Kisida, Akira Shuto, Noriyasu Sakamoto, Noritada Matsuo, Hiroaki Fujimoto, Kimitoshi Umeda
  • Patent number: 5270343
    Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 .dbd.CR.sup.2 .dbd.CR.sup.3 CR.sup.4 .dbd.CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C.tbd.C-- where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or is (CH.sub.2).sub.7 ;a=0 or 1; b= 0 or 1;R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl;X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from:a) C.sub.1-4 alkyl, C.
    Type: Grant
    Filed: June 15, 1992
    Date of Patent: December 14, 1993
    Assignee: Roussel Uclaf
    Inventors: John E. Robinson, George S. Cockerill
  • Patent number: 5229424
    Abstract: The present invention discloses pesticidally active compounds of formula (II) ##STR1## or a salt thereof, wherein Q is a monocylcic aromatic ring, or fused bicyclic ring system of which at least one ring is aromatic containing 9 or 10 atoms of which one may be nitrogen and the rest carbon each ring system being optionally substituted, or Q is a dihalovinyl group or a group R.sup.6 --C.tbd.C-- where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; and R.sup.1 is selected from hydrogen and C.sub.1-8 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy and X.sup.1 is hydrogen, fluoro or chloro.
    Type: Grant
    Filed: February 14, 1992
    Date of Patent: July 20, 1993
    Assignee: The Wellcome Foundation Limited
    Inventors: Robert J. Blade, George S. Cockerill, John E. Robinson
  • Patent number: 5225442
    Abstract: Compounds of general formula: ##STR1## in which A and R are defined in the description. Medicaments containing the same and useful for the treatment of melatoninergic disorders.
    Type: Grant
    Filed: January 3, 1992
    Date of Patent: July 6, 1993
    Assignee: Adir et Compagnie
    Inventors: Jean Andrieux, Raymond Houssin, Said Yous, Beatrice Guardiola, Daniel Lesieur
  • Patent number: 5202356
    Abstract: The present Application discloses pesticidally active compounds of the formula (I):Q Q.sup.1 CR.sup.2 =CR.sup.3 CR.sup.4 =CR.sup.5 C (.dbd.X) NHR.sup.1or a salt thereof, wherein Q is an monocyclic aromatic ring. or fused bicyclic ring system of which at least one ring is aromatic containing 9 or 10 atoms of which one may be nitrogen and the rest carbon each optionally substituted, or Q is a dihalovinyl group or a group R.sup.6 --C.tbd.C-- where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl. halo, C.sub.1-3 haloalkyl, alkynyl, or cyano; R.sup.2,R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo. C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X is oxygen or sulphur; and R.sup.1 is selected from hydrogen and C.sub.
    Type: Grant
    Filed: July 12, 1991
    Date of Patent: April 13, 1993
    Assignee: The Wellcome Foundation Limited
    Inventors: Robert J. Blade, George S. Cockerill, John E. Robinston
  • Patent number: 5151446
    Abstract: The present invention relates generally to compounds having melatonin receptor activities and in particular to substituted 2-amidotetralin derivatives; to pharmaceutical preparations comprising such compounds; and to methods for using these compounds as therapeutic and diagnostic reagents.
    Type: Grant
    Filed: March 28, 1991
    Date of Patent: September 29, 1992
    Assignee: Northwestern University
    Inventors: Alan S. Horn, deceased, Margarita L. Dubocovich
  • Patent number: 5145873
    Abstract: Cyclopropanecarboxyamides of the general formula I ##STR1## Where R.sup.1 is C.sub.1 -C.sub.4 -alkyl, fluorine, chlorine, bromine, C.sub.1 -C.sub.3 -haloalkyl or C.sub.1 -C.sub.3 -haloalkoxy, R.sup.2 is hydrogen, fluorine, chlorine or bromine, with the proviso that R.sup.1 is not fluorine if R.sup.2 is H, and pesticides containing these compounds.
    Type: Grant
    Filed: November 14, 1989
    Date of Patent: September 8, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Uwe Kardorff, Hans-Juergen Neubauer, Joachim Leyendecker, Christoph Kuenast, Peter Hofmeister, Wolfgang Krieg, Rainer Buerstinghaus
  • Patent number: 5071875
    Abstract: The present invention relates generally to compounds having melatonin receptor activities and in particular to substituted 2-amidotetralin derivatives; to pharmaceutical preparations comprising such compounds; and to methods for using these compounds as therapeutic and diagnostic reagents.
    Type: Grant
    Filed: September 25, 1989
    Date of Patent: December 10, 1991
    Assignee: Northwestern University
    Inventors: Alan S. Horn, Margarita L. Dubocovich
  • Patent number: 5064827
    Abstract: Compounds of the present invention, are represented by the general formula ##STR1## wherein R.sub.1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R.sub.2, R.sub.3 and R.sub.4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NHCOR.sub.5, --NHCONR.sub.5 R.sub.6, or --NHCOOR.sub.5 wherein R.sub.5 and R.sub.
    Type: Grant
    Filed: August 23, 1990
    Date of Patent: November 12, 1991
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventors: Ghanshyam Patil, William L. Matier, Khuong H. X. Mai
  • Patent number: 5061731
    Abstract: Novel fungicidally active N-benzyl-cyclopropanecarboxamides of the formula ##STR1## wherein X represents halogen,n represents 1 or 2,R.sup.1 represents hydrogen, halogen or lower alkyl,R.sup.2 represents lower alkyl, halogen-substituted lower alkyl or hydrogen, andR.sup.3 represents hydrogen or lower alkyl.The acid components thereof, other than when R.sup.1 is hydrogen or alkyl and R.sup.2 is hydrogen or alkyl, are also new.
    Type: Grant
    Filed: June 25, 1990
    Date of Patent: October 29, 1991
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Yoshio Kurahashi, Kozo Shiokawa, Shinzo Kagabu, Shinji Sakawa, Koichi Moriya
  • Patent number: 5059620
    Abstract: The present invention relates to new compounds of the formula ##STR1## wherein X is ##STR2## wherein R.sub.1 is hydrogen, lower alkyl, phenyl, benzyl, cinnamoyl, thiophene, furan, pyrrole, imidazole, pyrazole oxazole or thiazole; W is hydrogen or hydroxy; (Y).sub.A is positioned ortho to W and is an aminoloweralkyl having the formula --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 are the same or different and may be lower alkyl or R.sub.2 and R.sub.3 may together with N form a pyrrolidine, piperidine or azepine ring, and A is 2; n and m are independently from 0 to 5; and R is straight or branched C.sub.1 -C.sub.10 alkyl, straight or branched C.sub.3 -C.sub.10 cycloalkyl, straight or branched C.sub.2 -C.sub.4 alkenyl or straight or branched C.sub.2 -C.sub.4 alkynyl, or a pharmaceutically acceptable salt thereof.These compounds are useful in the treatment of various cardiac arrhythmias.
    Type: Grant
    Filed: April 7, 1988
    Date of Patent: October 22, 1991
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: David M. Stout, William L. Matier, Lawrence A. Black
  • Patent number: 5059623
    Abstract: A substituted cycloalkyl- or heterocyclyl-carboxanilide of the formula (I) ##STR1## in which X stands for an unsubstituted or an alkyl-substituted cycloalkyl or an unsubstituted or an alkyl-substituted heterocyclic,Hal stands for halogen andY.sup.1, Y.sup.2 and Y.sup.3 independently of one another stand for hydrogen, halogen, an unsubstituted or a halogen-substituted alkyl, an unsubstituted or a halogen-substituted alkoxy or an unsubstituted or a halogen-substituted alkylthio. Such substituted cycloalkyl- or heterocyclyl-carboxanilides are useful as fungicides.
    Type: Grant
    Filed: April 5, 1989
    Date of Patent: October 22, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Kruger, Klaus Sasse, Hermann Hagemann, Albrecht Marhold, Wilhelm Brandes
  • Patent number: 4988734
    Abstract: Highly fungicidal stereoisomers of N-(R)-(1-aryl-ethyl)-1-alkyl-2,2-dichloro-cyclopropanecarboxamides of the formula ##STR1## or a mixture thereof, substantially free of other stereoisomers, in which R.sup.1 stands for optionally branched alkyl having 2 to 4 carbon atoms,R.sup.2 stands for hydrogen, methyl or ethyl and X stands for hydrogen or halogen.Also new are intermediates of the formula ##STR2## or mixtures thereof, substantially free of other stereoisomers, in which R.sup.1 stands for optionally branched alkyl having 2 to 4 carbon atoms.R.sup.2 stands for hydrogen, methyl or ethyl, and Q stands for Cl, OH, or methoxy or ethoxy.
    Type: Grant
    Filed: April 13, 1989
    Date of Patent: January 29, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Udo Kraatz, Gerd Hanssler
  • Patent number: 4983630
    Abstract: There are provided new 2,2-difluorocyclopropylethane derivatives of general formula I ##STR1## in which A, B and R.sup.1-5 have the meanings given in the description and processes for their preparation. The compounds of the invention can be used as pesticides, especially against insects and mites.
    Type: Grant
    Filed: November 28, 1988
    Date of Patent: January 8, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Peter Wegner, Hartmut Joppien, Gunter Homberger, Arnim Kohn