Three-membered Ring In R Patents (Class 514/624)
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Patent number: 6313163Abstract: 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 indepType: GrantFiled: August 17, 2000Date of Patent: November 6, 2001Assignee: Allergen Sales, Inc.Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 6262104Abstract: 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: GrantFiled: June 5, 1998Date of Patent: July 17, 2001Assignee: SmithKline Beecham p.l.c.Inventors: Giulio Dondio, Silvano Ronzoni
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Patent number: 6262091Abstract: 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: GrantFiled: October 21, 1998Date of Patent: July 17, 2001Assignee: BASF AktiengesellschaftInventors: Oliver Wagner, Karl Eicken, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Harald Köhle, Günter Retzlaff
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Patent number: 6251947Abstract: 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: GrantFiled: August 4, 1999Date of Patent: June 26, 2001Assignee: Board of Trustees of the University of ArkansasInventors: Gregory Steven Basarab, Douglas Brian Jordan, Thomas Arend Lessen, Stephen L. Hansen
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Patent number: 6235789Abstract: 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: GrantFiled: May 28, 1997Date of Patent: May 22, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Osamu Uchikawa, Masaomi Miyamoto
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Patent number: 6214869Abstract: 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: GrantFiled: May 25, 1999Date of Patent: April 10, 2001Assignee: Bristol-Myers SquibbInventors: Jie Chen, Pierre Dextraze, Marco Dodier, Katherine S. Takaki
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Patent number: 6143789Abstract: 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: GrantFiled: November 25, 1998Date of Patent: November 7, 2000Assignee: Adir et CompagnieInventors: Fran.cedilla.ois Lefoulon, Luc Demuynck, Daniel Lesieur, Patrick Depreux, Caroline Bennejean, Pierre Renard, Philippe Delagrange
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Patent number: 6090854Abstract: 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: GrantFiled: January 22, 1999Date of Patent: July 18, 2000Assignee: Bristol-Meyers CompanyInventor: James R. Epperson
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Patent number: 6028112Abstract: 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: GrantFiled: July 31, 1998Date of Patent: February 22, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Karen L. Leboulluec, Katherine S. Takaki
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Patent number: 5965621Abstract: 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: GrantFiled: April 30, 1998Date of Patent: October 12, 1999Assignee: AllerganInventor: Lidija Balodis
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Patent number: 5962413Abstract: 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: GrantFiled: September 22, 1997Date of Patent: October 5, 1999Assignees: Schering Aktiengesellschaft, The University of Texas SystemInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
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Patent number: 5929119Abstract: 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: GrantFiled: August 11, 1997Date of Patent: July 27, 1999Assignee: BASF AktiengesellschaftInventors: Oliver Wagner, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5925674Abstract: This invention relates to cycloalkylcarboxanilides of the formula ##STR1## which are used to combat pests.Type: GrantFiled: October 26, 1995Date of Patent: July 20, 1999Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Krueger, Klaus Sasse, Thomas Schenke, Michael Negele, Heinz-Wilhelm Dehne
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Patent number: 5922771Abstract: 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: GrantFiled: August 19, 1996Date of Patent: July 13, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
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Patent number: 5885621Abstract: 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: GrantFiled: April 4, 1997Date of Patent: March 23, 1999Assignee: The General Hospital CorporationInventors: C. Alvin Head, Warren M. Zapol
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Patent number: 5880157Abstract: 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: GrantFiled: November 25, 1996Date of Patent: March 9, 1999Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Jeff Sterling, Yaacov Herzig, Meir Bialer, Abdullah Haj-Yehia, Boris Yagen
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Patent number: 5780512Abstract: 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: GrantFiled: March 26, 1997Date of Patent: July 14, 1998Assignee: Adir et CompagnieInventors: Daniel Lesieur, Eric Fourmaintraux, Patrick Depreux, Philippe Delagrange, Pierre Renard, Beatrice Guardiola-Lemaitre
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Patent number: 5763466Abstract: 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: GrantFiled: July 8, 1997Date of Patent: June 9, 1998Assignee: Bayer AktiengesellschaftInventors: Gerd Hanssler, Stefan Dutzmann, Matthias Wunsch
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Patent number: 5753709Abstract: Certain N-acyl 2-aryl cyclopropylmethylamine derivatives are useful as melatonergic agents.Type: GrantFiled: May 9, 1996Date of Patent: May 19, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Daniel J. Keavy, Michael F. Parker, Ronald J. Mattson, Graham Johnson
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Patent number: 5736578Abstract: 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: GrantFiled: May 10, 1996Date of Patent: April 7, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Brett T. Watson, Katherine S. Takaki, Joseph P. Yevich, James R. Epperson, George N. Karageorge, Karen L. Leboulluec
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Patent number: 5696150Abstract: 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: GrantFiled: September 13, 1996Date of Patent: December 9, 1997Assignee: Bayer AktiengesellschaftInventors: Gerd Hanssler, Stefan Dutzmann, Matthias Wunsch
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Patent number: 5693630Abstract: 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: GrantFiled: October 26, 1994Date of Patent: December 2, 1997Assignee: Astra AktiebolagInventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
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Patent number: 5661186Abstract: Certain tetralinyl- and indanyl-ethylamides are useful central nervous system agents.Type: GrantFiled: December 21, 1995Date of Patent: August 26, 1997Assignee: Bristol-Myers Squibb Co.Inventors: Katherine S. Takaki, Brett T. Watson, Graham S. Poindexter, James R. Epperson
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Patent number: 5612368Abstract: 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: GrantFiled: October 25, 1995Date of Patent: March 18, 1997Assignee: Adir et CompagnieInventors: Jean Andrieux, Michel Langlois, Pierre Renard, Philippe Delagrange
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Patent number: 5578595Abstract: 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: GrantFiled: March 21, 1995Date of Patent: November 26, 1996Assignee: Ciba-Geigy CorporationInventor: Manfred B oger
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Patent number: 5567735Abstract: 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: GrantFiled: June 7, 1995Date of Patent: October 22, 1996Assignee: Imperial Chemical Industries PLCInventors: Keith Russell, Cyrus J. Ohnmacht, Keith H. Gibson
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Patent number: 5554642Abstract: 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: GrantFiled: May 22, 1995Date of Patent: September 10, 1996Assignee: Adir et CompagnieInventors: Michel Langlois, Pierre Renard, G erard Adam
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Patent number: 5547984Abstract: 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: GrantFiled: June 6, 1995Date of Patent: August 20, 1996Assignee: Rohm and Haas CompanyInventor: Ashok K. Sharma
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Patent number: 5541228Abstract: 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: GrantFiled: March 8, 1995Date of Patent: July 30, 1996Assignee: Bristol-Myers Squibb Co.Inventors: Katherine S, Takaki, George N. Karageorge, Daniel J. Keavy, Michael F. Parker, Brett T. Watson
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Patent number: 5532264Abstract: 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: GrantFiled: May 17, 1995Date of Patent: July 2, 1996Assignee: Eli Lilly and CompanyInventors: David T. Wong, Juan I. Oguiza
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Patent number: 5532250Abstract: 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: GrantFiled: May 17, 1995Date of Patent: July 2, 1996Assignee: Eli Lilly and CompanyInventors: David T. Wong, Juan I. Oguiza
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Patent number: 5492931Abstract: 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: GrantFiled: January 21, 1994Date of Patent: February 20, 1996Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Krueger, Klaus Sasse, Thomas Schenke, Michael Negele, Heinz-Wilhelm Dehne
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Patent number: 5464872Abstract: 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: GrantFiled: January 18, 1995Date of Patent: November 7, 1995Assignee: Adir et CompagnieInventors: Michel Langlois, Pierre Renard, Gerard Adam
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Patent number: 5455273Abstract: 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: GrantFiled: November 19, 1993Date of Patent: October 3, 1995Assignee: Karl Thomae GmbHInventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
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Patent number: 5434190Abstract: 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: GrantFiled: October 11, 1994Date of Patent: July 18, 1995Assignee: Colgate-Palmolive Co.Inventor: Robert J. Steltenkamp
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Patent number: 5382598Abstract: 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: GrantFiled: September 24, 1993Date of Patent: January 17, 1995Assignees: Imperial Chemical Industries PLC, Imperial Chemical HouseInventors: Russell Keith, Cyrus J. Ohnmacht, Keith H. Gibson
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Amide derivatives, their production processes and their compositions for the control of insect pests
Patent number: 5356930Abstract: An amide derivative of the formula: ##STR1## which is useful for control of insect pests.Type: GrantFiled: August 5, 1993Date of Patent: October 18, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Hiroshi Kisida, Akira Shuto, Noriyasu Sakamoto, Noritada Matsuo, Hiroaki Fujimoto, Kimitoshi Umeda -
Patent number: 5270343Abstract: 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: GrantFiled: June 15, 1992Date of Patent: December 14, 1993Assignee: Roussel UclafInventors: John E. Robinson, George S. Cockerill
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Patent number: 5229424Abstract: 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: GrantFiled: February 14, 1992Date of Patent: July 20, 1993Assignee: The Wellcome Foundation LimitedInventors: Robert J. Blade, George S. Cockerill, John E. Robinson
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Patent number: 5225442Abstract: 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: GrantFiled: January 3, 1992Date of Patent: July 6, 1993Assignee: Adir et CompagnieInventors: Jean Andrieux, Raymond Houssin, Said Yous, Beatrice Guardiola, Daniel Lesieur
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Patent number: 5202356Abstract: 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: GrantFiled: July 12, 1991Date of Patent: April 13, 1993Assignee: The Wellcome Foundation LimitedInventors: Robert J. Blade, George S. Cockerill, John E. Robinston
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Patent number: 5151446Abstract: 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: GrantFiled: March 28, 1991Date of Patent: September 29, 1992Assignee: Northwestern UniversityInventors: Alan S. Horn, deceased, Margarita L. Dubocovich
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Patent number: 5145873Abstract: 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: GrantFiled: November 14, 1989Date of Patent: September 8, 1992Assignee: BASF AktiengesellschaftInventors: Uwe Kardorff, Hans-Juergen Neubauer, Joachim Leyendecker, Christoph Kuenast, Peter Hofmeister, Wolfgang Krieg, Rainer Buerstinghaus
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Patent number: 5071875Abstract: 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: GrantFiled: September 25, 1989Date of Patent: December 10, 1991Assignee: Northwestern UniversityInventors: Alan S. Horn, Margarita L. Dubocovich
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Patent number: 5064827Abstract: 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: GrantFiled: August 23, 1990Date of Patent: November 12, 1991Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Ghanshyam Patil, William L. Matier, Khuong H. X. Mai
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Patent number: 5061731Abstract: 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: GrantFiled: June 25, 1990Date of Patent: October 29, 1991Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Yoshio Kurahashi, Kozo Shiokawa, Shinzo Kagabu, Shinji Sakawa, Koichi Moriya
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Patent number: 5059620Abstract: 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: GrantFiled: April 7, 1988Date of Patent: October 22, 1991Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: David M. Stout, William L. Matier, Lawrence A. Black
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Patent number: 5059623Abstract: 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: GrantFiled: April 5, 1989Date of Patent: October 22, 1991Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Klaus Sasse, Hermann Hagemann, Albrecht Marhold, Wilhelm Brandes
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Patent number: 4988734Abstract: 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: GrantFiled: April 13, 1989Date of Patent: January 29, 1991Assignee: Bayer AktiengesellschaftInventors: Udo Kraatz, Gerd Hanssler
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Patent number: 4983630Abstract: 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: GrantFiled: November 28, 1988Date of Patent: January 8, 1991Assignee: Schering AktiengesellschaftInventors: Peter Wegner, Hartmut Joppien, Gunter Homberger, Arnim Kohn