The Aryl Ring Or Aryl Ring System And Amino Nitrogen Are Bonded Directly To The Same Acylic Carbon, Which Carbon Additionally Has Only Hydrogen Or Acyclic Hydrocarbyl Substituents Bonded Directly Thereto Patents (Class 514/655)
  • Patent number: 5280046
    Abstract: Provided is a method for treating Type I diabetes in mammals utilizing certain phenol and benzamide compounds.
    Type: Grant
    Filed: February 22, 1991
    Date of Patent: January 18, 1994
    Assignee: The University of Colorado Foundation, Inc.
    Inventors: Kevin Lafferty, Jill A. Panetta
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5274002
    Abstract: Novel trisubstituted phenyl analogs are now found to have activity as for the treatment of congestive heart failure.
    Type: Grant
    Filed: September 6, 1990
    Date of Patent: December 28, 1993
    Assignee: Warner-Lambert Company
    Inventor: Lynn D. Hawkins
  • Patent number: 5234946
    Abstract: The substituted alkylamine derivatives represented by formula (I) ##STR1## wherein R.sup.1 represents (a) substituted or unsubstituted C.sub.2-6 alkenyl group, (b) substituted or unsubstituted C.sub.3-6 cycloalkenyl group, (c) substituted or unsubstituted C.sub.2-6 alkynyl group, (d) substituted or unsubstituted aryl group, (e) substituted or unsubstituted heterocyclic group, (f) fused heterocyclic group which may be substituted, or (g) group represented by the formula Ru.sup.11 -Ar wherein R.sup.11 is a heterocyclic group and Ar is a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and which may be substituted; ##STR2## represents a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and may be substituted by R.sup.7,X and Y are linking groups,R.sup.2 is H or lower alkyl,R.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower cycloalkyl,R.sup.4 and R.sup.5 are independently hydrogen or halogen atoms,R.sup.
    Type: Grant
    Filed: August 30, 1991
    Date of Patent: August 10, 1993
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Takezawa, Masahiro Hayashi, Yoshikazu Iwasawa, Masaaki Hosoi, Yoshiaki Iida, Yoshimi Tsuchiya, Masahiro Horie, Toshio Kamei
  • Patent number: 5217964
    Abstract: The present invention relates to certain polyamine thiols which are useful as radioprotective agents.
    Type: Grant
    Filed: January 23, 1991
    Date of Patent: June 8, 1993
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Michael L. Edwards, Ronald D. Snyder
  • Patent number: 5189065
    Abstract: The use of products of formula (I) is described, wherein X and Y represent hydrogen, hydroxy or alkoxy; and R.sub.1 and R.sub.2 represent H, alkyl, alkenyl or alkynyl, arylalkyl, acyl or R.sub.1 and R.sub.2 together with nitrogen form a heterocycle for preparing an antitumoral drug.
    Type: Grant
    Filed: October 17, 1991
    Date of Patent: February 23, 1993
    Assignee: Roussel Uclaf
    Inventors: Jorg Czech, Hans H. Sedlacek, Lucien Nedelec, Jacques Guillaume, Christian Marchandeau
  • Patent number: 5182267
    Abstract: A pharmaceutical oil-in-water type microemulsion having an action of potentiating the activities of anti-cancer agents, said micro-emulsion comprisesfine particles of a vegetable oil or a triglyceride of a medium-chain fatty acid having 8 to 12 carbon atoms containing 0.1 to 10% (w/v) of N-solanesyl-N,N'-bis(3,4-dimethoxybenzyl)ethylenediamine malate of formula (I) below, ##STR1## an aqueous medium, and 0.05 to 25% (w/v) of a physiologically acceptable phospholipid for dispersing said fine particles in said aqueous medium.
    Type: Grant
    Filed: December 12, 1990
    Date of Patent: January 26, 1993
    Assignees: Lederle (Japan), Ltd., Nisshin Flour Milling Co., Ltd.
    Inventors: Osamu Ogawa, Ikuo Kishi, Yoshiyuki Tahara, Masanori Sugita
  • Patent number: 5180736
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 19, 1993
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5180746
    Abstract: An aralkylamine compound of the formula ##STR1## wherein R.sup.1 means a hydrogen atom or a lower alkyl group; R.sup.2 means an aromatic group which may be substituted; R.sup.3 means a hydrogen atom, a lower alkyl group or an aromatic group which may be substituted; n means an integer of 0 to 7; ring A means a five-through eight-membered cyclic group which may be substituted and may contain one or two hetero atom(s) of O and S atoms as the ring-constituents; and ring B means a benzene ring which may be substituted, or a salt thereof, which is useful as an cholinesterase inhibitor and a cerebral function ameliorating agent.
    Type: Grant
    Filed: February 15, 1990
    Date of Patent: January 19, 1993
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Akinobu Nagaoka, Yuji Ishihara
  • Patent number: 5166181
    Abstract: Halogenoalkylphenyl-alcohols, ketones and their hydrates of formula I, ##STR1## wherein R.sub.1 to R.sub.8 are as defined in the description, are useful as acetylcholinesterase inhibitors.
    Type: Grant
    Filed: August 15, 1990
    Date of Patent: November 24, 1992
    Assignee: Sandoz Ltd.
    Inventor: Sylvain Cottens
  • Patent number: 5149714
    Abstract: The present invention provides novel aryloxy indanamines of the formula ##STR1## wherein n, p and q are each independently 0, 1 or 2,Y and X are each independently lower alkyl, lower alkoxy, hydroxy, CF.sub.3, halogeno or when p or q are 2 and each of the Y or each of the X groups are on adjacent aryl carbon atoms, both of the X or both of the Y groups can be taken together to form a methylenedioxy moiety,R.sub.1 and R.sub.2 are each independently hydrogen, lower alkyl, aralkyl, or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached are pyrrolidino, morpholino, piperidino, piperazino, or 4-methylpiperazino,or an acid addition salt thereof, which are useful as antidepressants and as inhibitors of synaptic norepinephrine and serotonin uptake.
    Type: Grant
    Filed: August 15, 1990
    Date of Patent: September 22, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Jules Freedman
  • Patent number: 5143938
    Abstract: A compound which is a propanamine of general formula (I) ##STR1## in which: R1 is a phenyl radical optionally mono-, di- or trisubstituted,or is a 5- or 6-membered monocyclic heteroaryl radical in which the single heteroatom is nitrogen, oxygen or sulfur,R2 is a lower alkyl radical,R3 and R4 are a hydrogen atom or a lower alkyl, lower alkenyl or lower cycloalkylalkyl radical,or, together with the nitrogen atom to which they are attached, form a saturated 5- to 6-membered heterocycle comprising only one heteroatom,R5 is a 5- to 7-membered cycloalkyl radical, a phenyl radical or a 5- or 6-membered monocyclic heteroaryl radical,and W representsa group .dbd.CH--QH,or a heterocycle .dbd.C[Q--(CH2)n--Q],or a group .dbd.C.dbd.Q, in which groupsQ is an oxygen or sulfur atom,n has the value 2 or 3,W being .dbd.C.dbd.Q only when R3 and R4 are not both hydrogen, and their additions salts with pharmaceutically acceptable acids.
    Type: Grant
    Filed: February 26, 1991
    Date of Patent: September 1, 1992
    Assignee: Jouveinal S.A.
    Inventors: Alain Calvet, Agnes Grouhel, Henri Jacobelli, Jean-Louis Junien, Xavier Pascaud
  • Patent number: 5134168
    Abstract: Drug-resistant protozoal infection, particularly, drug-resistant malarial infection in humans, can be effectively treated with standard antiprotozoal agents if administered in conjunction with a phenoxyamino-substituted benzocycloalkane derivative.
    Type: Grant
    Filed: March 13, 1991
    Date of Patent: July 28, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Alan J. Bitonti, Jules Freedman
  • Patent number: 5128365
    Abstract: The present invention provides compounds having glutathione peroxidase activity and, therefore, are effective glutathione peroxidase replacements. These compounds are useful as drugs for the prevention of cataracts and as anti-oxidants for H.sub.2 O.sub.2 and other peroxides. The present invention also provides methods and pharmaceutical compositions of the compound.
    Type: Grant
    Filed: July 19, 1989
    Date of Patent: July 7, 1992
    Assignees: The Trustees of Columbia University in the City of New York, New York University
    Inventors: Abraham Spector, Stephen R. Wilson, Paul A. Zucker
  • Patent number: 5126371
    Abstract: Novel diarylacetylenes of the formula I ##STR1## where A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meanings stated in the description, are useful for the treatment of disorders.
    Type: Grant
    Filed: August 20, 1990
    Date of Patent: June 30, 1992
    Assignee: BASF Akteingesellschaft
    Inventors: Hans-Heiner Wuest, Fritz-Frieder Frickel, Axel Nuerrenbach
  • Patent number: 5095039
    Abstract: A halogen-substituted diphenylsulfide compound is disclosed which produce a large selective inhibition of serotonin uptake in brain. This compound is useful in the treatment of depression as well as anxiety, obsessive compulsive disorders and alcoholism.
    Type: Grant
    Filed: June 5, 1990
    Date of Patent: March 10, 1992
    Assignee: Burroughs Wellcome Co.
    Inventors: Nariman B. Mehta, Lawrence E. Brieaddy
  • Patent number: 5086073
    Abstract: The invention concerns compounds having formula: ##STR1## or a salt thereof, wherein E represents hydrogen, lower alkyl or a group Ar.sup.1 --A.sup.1 ; Ar and Ar.sup.1 are the same or different aryl groups (including heteroaryl) which are optionally substituted, e.g. by one or more substituents commonly used in pharmaceutical chemistry; A and A.sup.1 are the same or different alkylene groups having one or two carbon atoms linking Ar or Ar.sup.1 to N and optionally substituted by lower alkyl and/or optionally substituted aryl, B is an alkylene group of 3 or 4 carbon atoms, which may be substituted by lower alkyl; D.sup.1 represents halogen, CH.sub.3, CR.sup.1 R.sup.2 NH.sub.2, SO.sub.3 H or SO.sub.2 NR.sup.6 R.sup.7 where R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl and R.sup.6 and R.sup.7 are each hydrogen, lower alkyl or aralkyl of 7 to 12 carbon atoms or R.sup.6 and R.sup.
    Type: Grant
    Filed: May 30, 1990
    Date of Patent: February 4, 1992
    Assignee: John Wyeth & Brother Limited
    Inventors: John F. White, Michael C. Warren, Christine Ennis
  • Patent number: 5071853
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: December 10, 1991
    Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
  • Patent number: 5053431
    Abstract: The present invention concerns compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, a hydroxy group or a methoxy group;R.sup.2 is hydrogen or a methyl group;R.sup.3 is hydrogen or a methyl group;Y is a secondary amino group (NHalkyl) or a tertiary amino group (N(alkyl).sub.2); andZ is hydrogen or a halogen.The invention further provides a method of inhibiting topoisomerase II using a compound having the structure: ##STR2## wherein R.sup.1 is hydrogen, a hydroxy group or a methoxy group;R.sup.2 is hydrogen or a methyl group;R.sup.3 is hydrogen or a methyl group;Y is a halogen, secondary amino group (NHalkyl) or a tertiary amino group (N(alkyl).sub.2); andZ is hydrogen or a halogen.The invention further concerns pharmaceutical compositions which comprise the above-identified compound or the acid salts thereof, and the use of the compound or compositions for treating a malignancy in a subject.
    Type: Grant
    Filed: June 26, 1990
    Date of Patent: October 1, 1991
    Assignee: Sloan-Kettering Institute For Cancer Research
    Inventors: Kyoichi A. Watanabe, Masao Koyama, Ting-Chao Chou
  • Patent number: 5051409
    Abstract: 2-Aminodecalin derivatives of the formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are H or methyl,A is H, OH, O-alkylcarbonyl, O-benzoyl or O-CH.sub.3,R.sup.4 is H, cyclopropyl, alkyl, alkenyl, or alkynyl,R.sup.5 is alkyl, alkenyl or alkynyl which is substituted or unsubstituted,cycloalkyl or cycloalkenyl whic is substituted or unsubstituted, substituted phenylalkyl, substituted cycloalkyl-alkyl, substituted 5-membered heterocyclic ring, bicycloalkyl-alkyl orR.sup.4 and R.sup.5, together with the nitrogen atom, are a substituted or unsubstituted, saturated or unsaturated piperidine radical,their plant-tolerated salts and N-oxides, and fungicides containing these compounds.
    Type: Grant
    Filed: November 1, 1989
    Date of Patent: September 24, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Zipplies, Bernhard Zipperer, Hubert Sauter, Norbert Goetz, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5036081
    Abstract: Alpha-glucosidase inhibitor is provided as a promoter of calcium absorption in mammals. The examples of the inhibitor are shown by the formula; ##STR1## wherein A stands for a C.sub.1 -C.sub.10 acyclic hydrocarbon group which may be substituted by hydroxyl, phenoxy, thienyl, furyl, pyridyl, cyclohexyl or phenyl group which itself may be further substituted, a C.sub.5 -C.sub.6 cyclic hydrocarbon group which may be substituted by hydroxyl, hydroxymethyl, methyl or amino group, or a sugar residue.There is also provided a calcium preparation which contains an .alpha.-glucosidase inhibitor and a calcium source.
    Type: Grant
    Filed: August 22, 1989
    Date of Patent: July 30, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takao Matsuo, Hiroyuki Odaka, Tsuyoshi Suzuki, Masao Tsuda
  • Patent number: 5032616
    Abstract: 4-trans-substituted cyclohexylamine derivatives of the formula ##STR1## where R.sup.1 is the group CR.sup.5 R.sup.6 R.sup.7, in which R.sup.5, R.sup.6 and R.sup.7 are hydrogen, unsubstituted or substituted alkyl, alkoxy, alkylthio or cycloalkyl, with the proviso that not more than one of the substituents R.sup.5, R.sup.6 and R.sup.7 may by hydrogen, or in which R.sup.6 and R.sup.7 together with the included carbon atom form a three-membered to six-membered carbocyclic aliphatic ring,R.sup.2 and R.sup.3 are hydrogen, alkyl, alkenyl or alkynyl or cycloalkyl or cycloalkenyl, which in turn may be substituted, with the proviso that the sum of the carbon atoms and hetero atoms (O, S and halogen) of R.sup.2 and R.sup.3 together is not less than 8,R.sup.4 is hydrogen, alkyl, cycloalkyl or alkoxy, and m is 1 to 4, and the bond is a single or a double bond,salts thereof, and their use as fungicides.
    Type: Grant
    Filed: August 28, 1987
    Date of Patent: July 16, 1991
    Inventors: Hubert Sauter, Matthias Zipplies, Norbert Goetz, Eberhard Ammermann, Ernst-Heinrich Pommer
  • Patent number: 5030625
    Abstract: The invention relates to novel homopropargylamines of formula I ##STR1## wherein n is 2 or 3,R.sub.1 is a group of formula IIa, IIb or IIc ##STR2## in which R.sub.6 and R.sub.7 indpendently are H, halogen, CF.sub.3, lower alkyl or lower alkoxy,s is a number of 3 to 5,X is O, S, OCH.sub.2, SCH.sub.2 CH.sub.2 or NR.sub.8, andR.sub.8 is H or lower alkyl,R.sub.2 is H or lower alkyl, eitherR.sub.3 and R.sub.4, independently, are H or lower alkyl, orR.sub.3 and R.sub.4 together are (CH.sub.2).sub.u,in which u is a number of 3 to 5, andR.sub.5 is H, alkenyl or is a group selected from alkyl, trialkylsilyl, dialkylphenylsilyl, phenyl, phenylalkyl and cycloalkyl, in which alkyl, phenyl and cycloalkyl groups or moieties are unsubstituted or substituted by OH, lower alkyl, lower alkoxy, phenyl or halogen,in free base form or acid addition salt form thereof, their preparation, their chemotherapeutical and agricultural use and to compositions comprising such novel compounds and suitable for such use.
    Type: Grant
    Filed: August 14, 1989
    Date of Patent: July 9, 1991
    Assignee: Sandoz Ltd.
    Inventor: Anton Stuetz
  • Patent number: 5021458
    Abstract: Amine derivatives having the general formula (I): ##STR1## wherein X is selected from the group consisting of ##STR2## wherein Q is oxygen, sulfur or nitrogen atom, and ##STR3## wherein Q is as above; Y is selected from the group consisting of ##STR4## R.sup.1 is hydrogen atom or an alkyl group; R.sup.2 is hydrogen atom or an alkyl group; R.sup.3 is hydrogen atom, a halogen atom or an alkyl group; R.sup.4 is hydrogen atom, an alkyl group, a cycloalkyl group, a halogenated alkyl group or a halogen atom; R.sup.5 is hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, nitro group or hydroxy group; R.sup.5 is attached to an arbitrary position of X, and R.sup.3 or R.sup.4 is attached to an arbitrary position of Y.The amine derivatives (I) are useful as fungicides.
    Type: Grant
    Filed: December 7, 1988
    Date of Patent: June 4, 1991
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Tetsuya Maeda, Toshiyuki Yamamoto, Mituo Takase, Kazuya Sasaki, Tadashi Arika, Mamoru Yokoo, Rieko Hashimoto, Kouji Amemiya, Sakae Koshikawa
  • Patent number: 5021429
    Abstract: Compounds of the general formula: ##STR1## and physiologically acceptable salts, and hydrates, N-oxides and bioprecursors of such compounds and such salts in whichR.sub.1 and R.sub.2, which may be the same or different, represent hydrogen or lower alkyl, cycloalkyl, aralkyl or lower alkenyl groups, or lower alkyl groups interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl; or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached form a heterocyclic ring which may contain the hetero functions --O-- and ##STR3## R.sub.3 represents hydrogen, lower alkyl, alkenyl or alkoxyalkyl; X represents --O--, --S-- or --CH.sub.2 -- or ##STR4## where R.sub.5 is hydrogen or lower alkyl; Y represents .dbd.S, .dbd.O, .dbd.NR.sub.6 or .dbd.CHR.sub.7 ;in which R.sub.6 represents hydrogen, nitro, cyano, lower alkyl, aryl, arylsulphonyl or lower alkylsulphonyl; R.sub.
    Type: Grant
    Filed: December 22, 1986
    Date of Patent: June 4, 1991
    Assignee: Allen & Hansburys Limited
    Inventor: Michael Martin-Smith
  • Patent number: 5019598
    Abstract: o-Aminomethylphenols of the formula ##STR1## where R.sup.1, R.sup.3 and R.sup.4 are hydrogen, fluorine, chlorine, bromine, alkyl, alkoxy or dimethylamino, R.sup.2 is hydrogen, chlorine, bromine, alkyl, alkenyl, alkoxyalkyl, cyclohexyl or phenyl, or R.sup.1 and R.sub.2, R.sup.2 and R.sup.3 or R.sup.3 and R.sup.4 form a carbocyclic, saturated or unsaturated five-membered or six-membered ring, and R is alkyl, and salts thereof, and fungicides containing these compounds.
    Type: Grant
    Filed: June 15, 1989
    Date of Patent: May 28, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Costin Rentzea, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5006563
    Abstract: This invention relates to alkylamino and alkyl amino alkyl diarylketones of the formula ##STR1## where Ar is aryl of the formula ##STR2## where V is hydrogen, halogen, loweralkyl, loweralkoxy, CF.sub.3, No.sub.2 and u is an integer of 1 to 3; X and Y are independently CH.sub.2 --, --CH.sub.2 -- or --CHF--; Z and W are independently --CH.sub.2 --, --O--, --CHOH--, or --CHF--; m, n, p, q and t are integers which are independently 0 or 1; R.sub.1 is H or loweralkyl; R.sub.2 and R.sub.3 are loweralkyl; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as analgesic agents and as agents for alleviating various memory dysfunctions, characterized by a decreased cholinergic function, such as Alzheimer's disease.
    Type: Grant
    Filed: July 31, 1990
    Date of Patent: April 9, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: R. Richard L. Hamer, Brian Freed, Richard C. Allen
  • Patent number: 5004756
    Abstract: A pharmaceutical oil-in-water type microemulsion having an action of potentiating the activities of anti-cancer agents, said micro-emulsion comprises fine particles of a vegetable oil or a triglyceride of a medium-chain fatty acid having 8 to 12 carbon atoms containing 0.1 to 10% (w/v) of N-solanesyl-N,N'-bis(3,4-dimethoxybenzyl)ethylenediamine malate of formula (I) below, ##STR1## an aqueous medium, and, 0.05 to 25% (w/v) of a physiologically acceptable phospholipid for dispersing said fine particles in said aqueous medium.
    Type: Grant
    Filed: August 8, 1989
    Date of Patent: April 2, 1991
    Assignees: Lederle (Japan) Ltd., Nisshin Flour Milling Co., Ltd.
    Inventors: Osamu Ogawa, Ikuo Kishi, Yoshiyuki Tahara, Masanori Sugita
  • Patent number: 4946863
    Abstract: The present invention relates to 3-aminomethyl derivatives of indane, dihydrobenzofurane, dihydrobenzothiophene, and indoline, acid addition salts thereof, isomers thereof, methods of preparation, pharmaceutical compositions and method of treating CNS-disorders such as schizophrenia, Parkinson's disease, depression, anxiety, migraine and senile dementia, or in the cure of cardiovascular diseases, by administering such a derivative.
    Type: Grant
    Filed: January 18, 1989
    Date of Patent: August 7, 1990
    Assignee: H. Lundbeck A/S
    Inventors: Klaus P. Boegesoe, Jens K. Perregaard
  • Patent number: 4939148
    Abstract: Compounds of formula I ##STR1## wherein R.sub.1 represents a group of formula ##STR2## and R.sub.2 represents hydrogen or lower alkyl, orR.sub.1 and R.sub.2 together with the carbon atom to which they are attached represent a group of formula IIg ##STR3## R.sub.4 and R.sub.5 represent independently hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl or halogenalkyl andR.sub.6 represents a group of formula ##STR4## R.sub.1 represents a group of formula IIa to IIf as defined above, R.sub.2 and R.sub.3 together form a --(CH.sub.2)--.sub.u group wherein u stands for a whole number from 1 to 8 and R.sub.4, R.sub.5 and R.sub.6 have the meanings given above.which compounds are indicated for use as pharmaceuticals and agrochemicals.
    Type: Grant
    Filed: January 29, 1987
    Date of Patent: July 3, 1990
    Assignee: Sandoz, Ltd.
    Inventors: Anton Stutz, Peter Nussbaumer
  • Patent number: 4925831
    Abstract: Disclosed are specific aminoalkyl naphthalenediol derivatives that enhance natural human host resistance to viral infectious organisms and particularly AIDS-related viruses. Such agents are also administered prophylactically to individuals whose resistance to infection has been specifically immunocompromised by an AIDs-related (HIV) virus.
    Type: Grant
    Filed: June 11, 1987
    Date of Patent: May 15, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette
  • Patent number: 4914133
    Abstract: Amino compounds of the formula ##STR1## where R.sup.1 is alkyl, A is alkylene or alkenylene, and Ar is aryl, and their acid addition salts, and fungicides containing these compounds.
    Type: Grant
    Filed: April 14, 1988
    Date of Patent: April 3, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Walter Himmele, Hubert Sauter, Hardo Siegel, Eberhard Ammermann, Ernst-Heinrich Pommer
  • Patent number: 4910208
    Abstract: A method is provided for inhibiting leukotriene biosynthesis and thus treating asthma, psoriasis or inflammation by oral administration of p-aminophenols having the structure ##STR1## wherein m is 0 to 5; X is CH or N; R.sup.1 and R.sup.2 may be the same or different and are H, lower alkyl, aryl, hydroxy, hydroxyalkyleneoxy, alkylthio, alkoxy, alkanoyloxy, aryloxy, halo, carboxy, alkoxycarbonyl or amido; R.sup.3 is H, lower alkyl, alkanoyl or aroyl; and R.sup.4 is H, lower alkyl, benzoyl or alkanoyl, and including acid-addition salts thereof, with the proviso that when R.sup.4 is benzoyl, R.sup.2 is other than H.
    Type: Grant
    Filed: February 19, 1988
    Date of Patent: March 20, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Raj N. Misra
  • Patent number: 4897425
    Abstract: Cyclohexylamines of the formula ##STR1## where X is a single bond or an alkylene chain, Y is hydrogen or an aryl, cyclohexyl, 4-cyclohexylcyclohexyl, perhydro-1- or 2-naphthyl or piperidyl radical, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, cycloalkyl, cycloalkenyl or arylalkyl, or R.sup.1 and R.sup.2 together form an alkylene group and, togehter with the N atom, form a ring, and acid addition salts thereof, with the exception of compounds in which X is a single bond, Y is cyclohexyl, R.sup.1 and R.sup.2 are hydrogen or methyl, and the compounds in which X is C.sub.6 -, C.sub.7 - and C.sub.8 -alkyl, Y is hydrogen and R.sup.1 and R.sup.2 together with the N atom whose substituents they are form a 2,6-dimethylmorpholine radical, and fungicides containing such cyclohexylamines.
    Type: Grant
    Filed: November 16, 1987
    Date of Patent: January 30, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernhard Zipperer, Ernst Buschmann, Norbert Goetz, Ulrich Schirmer, Eberhard Ammermann, Ernst-Heinrich Pommer
  • Patent number: 4894392
    Abstract: Disclosed are specific aminoalkyl naphthalenediol derivatives that enhance host resistance to infectious organisms. Such agents are administered prophylactically to individuals whose resistance to infection is comprised by chemotherapy, surgery, burns or other forms of severe stress.
    Type: Grant
    Filed: May 12, 1988
    Date of Patent: January 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Timothy F. Gallagher
  • Patent number: 4882358
    Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4 or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar being planar or deviating only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.
    Type: Grant
    Filed: May 12, 1987
    Date of Patent: November 21, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4876283
    Abstract: Antisnoring agent for oral or local application in the nasal/pharyngal cavities comprising an active content of a secretolytically and/or secretoproductively effective substance, as the active ingredient, together with carrier substances for diluents which are compatible with mucous membranes.
    Type: Grant
    Filed: March 20, 1989
    Date of Patent: October 24, 1989
    Inventor: Dietrich Reichert
  • Patent number: 4829090
    Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a chrysene or substituted chrysene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.
    Type: Grant
    Filed: August 28, 1987
    Date of Patent: May 9, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4822822
    Abstract: Benzylamine derivatives having the general formula ##STR1## wherein R.sub.1 is an iso-propyl or tert-butyl group, R.sub.2 is a group of the formula: ##STR2## and R.sub.3 is a lower alkyl or lower alkenyl group, or its acid addition salt. These derivatives are useful for the treatment of animal epidemics or infectious diseases induced by fungi as an antimycotic agent for humans and animals, for the control of plant diseases as an agricultural fungicide, and for the control of fungi and bacteria in industrial materials or products as an industrial fungicide.
    Type: Grant
    Filed: October 27, 1986
    Date of Patent: April 18, 1989
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Masanobu Arita, Kiyoshi Arai, Nobuo Komoto, Setsuko Hirose, Takeshi Sekine
  • Patent number: 4820737
    Abstract: Ophthalmic compositions useful as tear stimulants when topically applied to the eye for effective treatment of dry eye syndrome.
    Type: Grant
    Filed: March 16, 1988
    Date of Patent: April 11, 1989
    Assignee: University of Iowa Research Foundation
    Inventors: Ronald D. Schoenwald, Charles F. Barfknecht
  • Patent number: 4810727
    Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a chrysene or substituted chrysene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl;--C--C-- is a five- or six-membered saturated carbocyclic ring;R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.
    Type: Grant
    Filed: August 6, 1987
    Date of Patent: March 7, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4808753
    Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.
    Type: Grant
    Filed: January 20, 1988
    Date of Patent: February 28, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4803226
    Abstract: The present invention relates to compounds of formula (I) ##STR1## wherein Ar is an anthracene or substituted anthracene ring system;R.sup.1 is a C.sub.1-3 alkylene moiety;R.sup.2 is hydrogen or a C.sub.1-6 alkyl group;R.sup.3 is a hydroxy C.sub.1-6 alkyl group;R.sup.4 and R.sup.5 are the same or different and are hydrogen, C.sub.1-6 alkyl or hydroxy C.sub.1-6 alkyl, esters thereof derived from condensation of carboxy acids and hydroxyl groups of R.sup.3, R.sup.4, and R.sup.5 ;Acid addition salts thereof, which have been found useful for the treatment of tumors in mammals.
    Type: Grant
    Filed: January 6, 1988
    Date of Patent: February 7, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4791232
    Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.
    Type: Grant
    Filed: January 19, 1988
    Date of Patent: December 13, 1988
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4791233
    Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.
    Type: Grant
    Filed: January 19, 1988
    Date of Patent: December 13, 1988
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4791231
    Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.
    Type: Grant
    Filed: January 19, 1988
    Date of Patent: December 13, 1988
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4791123
    Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.
    Type: Grant
    Filed: January 22, 1987
    Date of Patent: December 13, 1988
    Assignee: Schering Akt.
    Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
  • Patent number: 4789687
    Abstract: A food product comprising a food substance in combination with vanillylamine or a vanillylamide.
    Type: Grant
    Filed: January 13, 1987
    Date of Patent: December 6, 1988
    Assignee: Ajinomoto Co., Inc.
    Inventor: Kazuo Iwai
  • Patent number: 4758561
    Abstract: The present invention to pharmaceutical composition comprising an effective amount of products having the structural formula ##STR1## where R.sub.1 is a hydrogen atom or a lower alkyl group such as methyl or ethyl,R.sub.2 is a straight or branched cyclopropylmethyl, 2-furyl methyl, benzyl, phenyl or lower alkyl group from C.sub.1 to C.sub.4 such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tertiary butyl; the NR.sub.1 R.sub.2 group can also represent a nitrogenous heterocyclic compound N(CH.sub.2).sub.n in which n can be any value between 4 and 6.The products are useful in human and veterinary therapy because of their anti-inflammatory, diuretic, bronchodilating, anticholinergic, antispasmodic and antidepressant properties.
    Type: Grant
    Filed: July 22, 1985
    Date of Patent: July 19, 1988
    Assignee: Societe Cortial, S.A.
    Inventors: Guillaume Le Baut, Louis Sparfel, Marie-Helene Creuzet, Claude Feniou, Henri Pontagnier, Gisele Prat
  • Patent number: 4757067
    Abstract: The present invention to pharmaceutical composition comprising an effective amount of products having the structural formula ##STR1## where R.sub.1 is a hydrogen atom or a lower alkyl group such as methyl or ethyl,R.sub.2 is a straight or branched cyclopropylmethyl, 2-furyl methyl, benzyl, phenyl or lower alkyl group from C.sub.1 to C.sub.4 such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tertiary butyl; the NR.sub.1 R.sub.2 group can also represent a nitrogenous heterocyclic compound N(CH.sub.2).sub.n in which n can be any value between 4 and 6.The products are useful in human and veterinary therapy because of their anti-inflammatory, diuretic, bronchodilating, anticholinergic, antispasmodic and antidepressant properties.
    Type: Grant
    Filed: January 21, 1987
    Date of Patent: July 12, 1988
    Assignee: Societe Cortial, S.A.
    Inventors: Guillaume Le Baut, Louis Sparfel, Marie-Helene Creuzet, Claude Feniou, Henri Pontagnier, Gisele Prat