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)
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Patent number: 5280046Abstract: Provided is a method for treating Type I diabetes in mammals utilizing certain phenol and benzamide compounds.Type: GrantFiled: February 22, 1991Date of Patent: January 18, 1994Assignee: The University of Colorado Foundation, Inc.Inventors: Kevin Lafferty, Jill A. Panetta
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Patent number: 5276053Abstract: 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: GrantFiled: October 6, 1992Date of Patent: January 4, 1994Assignee: Warner-Lambert CompanyInventor: Graham Johnson
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Patent number: 5274002Abstract: Novel trisubstituted phenyl analogs are now found to have activity as for the treatment of congestive heart failure.Type: GrantFiled: September 6, 1990Date of Patent: December 28, 1993Assignee: Warner-Lambert CompanyInventor: Lynn D. Hawkins
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Patent number: 5234946Abstract: 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: GrantFiled: August 30, 1991Date of Patent: August 10, 1993Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hiroshi Takezawa, Masahiro Hayashi, Yoshikazu Iwasawa, Masaaki Hosoi, Yoshiaki Iida, Yoshimi Tsuchiya, Masahiro Horie, Toshio Kamei
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Patent number: 5217964Abstract: The present invention relates to certain polyamine thiols which are useful as radioprotective agents.Type: GrantFiled: January 23, 1991Date of Patent: June 8, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Michael L. Edwards, Ronald D. Snyder
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Patent number: 5189065Abstract: 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: GrantFiled: October 17, 1991Date of Patent: February 23, 1993Assignee: Roussel UclafInventors: Jorg Czech, Hans H. Sedlacek, Lucien Nedelec, Jacques Guillaume, Christian Marchandeau
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Patent number: 5182267Abstract: 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: GrantFiled: December 12, 1990Date of Patent: January 26, 1993Assignees: Lederle (Japan), Ltd., Nisshin Flour Milling Co., Ltd.Inventors: Osamu Ogawa, Ikuo Kishi, Yoshiyuki Tahara, Masanori Sugita
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Patent number: 5180736Abstract: 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: GrantFiled: May 17, 1991Date of Patent: January 19, 1993Assignee: Warner-Lambert CompanyInventor: Graham Johnson
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Patent number: 5180746Abstract: 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: GrantFiled: February 15, 1990Date of Patent: January 19, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Akinobu Nagaoka, Yuji Ishihara
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Patent number: 5166181Abstract: 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: GrantFiled: August 15, 1990Date of Patent: November 24, 1992Assignee: Sandoz Ltd.Inventor: Sylvain Cottens
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Patent number: 5149714Abstract: 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: GrantFiled: August 15, 1990Date of Patent: September 22, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Jules Freedman
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Patent number: 5143938Abstract: 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: GrantFiled: February 26, 1991Date of Patent: September 1, 1992Assignee: Jouveinal S.A.Inventors: Alain Calvet, Agnes Grouhel, Henri Jacobelli, Jean-Louis Junien, Xavier Pascaud
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Patent number: 5134168Abstract: 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: GrantFiled: March 13, 1991Date of Patent: July 28, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Alan J. Bitonti, Jules Freedman
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Patent number: 5128365Abstract: 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: GrantFiled: July 19, 1989Date of Patent: July 7, 1992Assignees: The Trustees of Columbia University in the City of New York, New York UniversityInventors: Abraham Spector, Stephen R. Wilson, Paul A. Zucker
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Patent number: 5126371Abstract: 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: GrantFiled: August 20, 1990Date of Patent: June 30, 1992Assignee: BASF AkteingesellschaftInventors: Hans-Heiner Wuest, Fritz-Frieder Frickel, Axel Nuerrenbach
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Patent number: 5095039Abstract: 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: GrantFiled: June 5, 1990Date of Patent: March 10, 1992Assignee: Burroughs Wellcome Co.Inventors: Nariman B. Mehta, Lawrence E. Brieaddy
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Patent number: 5086073Abstract: 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: GrantFiled: May 30, 1990Date of Patent: February 4, 1992Assignee: John Wyeth & Brother LimitedInventors: John F. White, Michael C. Warren, Christine Ennis
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Patent number: 5071853Abstract: 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: GrantFiled: February 27, 1990Date of Patent: December 10, 1991Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
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Patent number: 5053431Abstract: 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: GrantFiled: June 26, 1990Date of Patent: October 1, 1991Assignee: Sloan-Kettering Institute For Cancer ResearchInventors: Kyoichi A. Watanabe, Masao Koyama, Ting-Chao Chou
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Patent number: 5051409Abstract: 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: GrantFiled: November 1, 1989Date of Patent: September 24, 1991Assignee: BASF AktiengesellschaftInventors: Matthias Zipplies, Bernhard Zipperer, Hubert Sauter, Norbert Goetz, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5036081Abstract: 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: GrantFiled: August 22, 1989Date of Patent: July 30, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Takao Matsuo, Hiroyuki Odaka, Tsuyoshi Suzuki, Masao Tsuda
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Patent number: 5032616Abstract: 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: GrantFiled: August 28, 1987Date of Patent: July 16, 1991Inventors: Hubert Sauter, Matthias Zipplies, Norbert Goetz, Eberhard Ammermann, Ernst-Heinrich Pommer
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Patent number: 5030625Abstract: 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: GrantFiled: August 14, 1989Date of Patent: July 9, 1991Assignee: Sandoz Ltd.Inventor: Anton Stuetz
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Patent number: 5021458Abstract: 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: GrantFiled: December 7, 1988Date of Patent: June 4, 1991Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Tetsuya Maeda, Toshiyuki Yamamoto, Mituo Takase, Kazuya Sasaki, Tadashi Arika, Mamoru Yokoo, Rieko Hashimoto, Kouji Amemiya, Sakae Koshikawa
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Patent number: 5021429Abstract: 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: GrantFiled: December 22, 1986Date of Patent: June 4, 1991Assignee: Allen & Hansburys LimitedInventor: Michael Martin-Smith
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Patent number: 5019598Abstract: 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: GrantFiled: June 15, 1989Date of Patent: May 28, 1991Assignee: BASF AktiengesellschaftInventors: Costin Rentzea, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5006563Abstract: 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: GrantFiled: July 31, 1990Date of Patent: April 9, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: R. Richard L. Hamer, Brian Freed, Richard C. Allen
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Patent number: 5004756Abstract: 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: GrantFiled: August 8, 1989Date of Patent: April 2, 1991Assignees: Lederle (Japan) Ltd., Nisshin Flour Milling Co., Ltd.Inventors: Osamu Ogawa, Ikuo Kishi, Yoshiyuki Tahara, Masanori Sugita
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Patent number: 4946863Abstract: 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: GrantFiled: January 18, 1989Date of Patent: August 7, 1990Assignee: H. Lundbeck A/SInventors: Klaus P. Boegesoe, Jens K. Perregaard
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Patent number: 4939148Abstract: 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: GrantFiled: January 29, 1987Date of Patent: July 3, 1990Assignee: Sandoz, Ltd.Inventors: Anton Stutz, Peter Nussbaumer
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Patent number: 4925831Abstract: 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: GrantFiled: June 11, 1987Date of Patent: May 15, 1990Assignee: Merck & Co., Inc.Inventor: Philippe L. Durette
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Patent number: 4914133Abstract: 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: GrantFiled: April 14, 1988Date of Patent: April 3, 1990Assignee: BASF AktiengesellschaftInventors: Walter Himmele, Hubert Sauter, Hardo Siegel, Eberhard Ammermann, Ernst-Heinrich Pommer
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Patent number: 4910208Abstract: 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: GrantFiled: February 19, 1988Date of Patent: March 20, 1990Assignee: E. R. Squibb & Sons, Inc.Inventor: Raj N. Misra
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Patent number: 4897425Abstract: 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: GrantFiled: November 16, 1987Date of Patent: January 30, 1990Assignee: BASF AktiengesellschaftInventors: Bernhard Zipperer, Ernst Buschmann, Norbert Goetz, Ulrich Schirmer, Eberhard Ammermann, Ernst-Heinrich Pommer
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Patent number: 4894392Abstract: 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: GrantFiled: May 12, 1988Date of Patent: January 16, 1990Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, Timothy F. Gallagher
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Patent number: 4882358Abstract: 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: GrantFiled: May 12, 1987Date of Patent: November 21, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4876283Abstract: 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: GrantFiled: March 20, 1989Date of Patent: October 24, 1989Inventor: Dietrich Reichert
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Patent number: 4829090Abstract: 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: GrantFiled: August 28, 1987Date of Patent: May 9, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4822822Abstract: 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: GrantFiled: October 27, 1986Date of Patent: April 18, 1989Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Masanobu Arita, Kiyoshi Arai, Nobuo Komoto, Setsuko Hirose, Takeshi Sekine
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Patent number: 4820737Abstract: Ophthalmic compositions useful as tear stimulants when topically applied to the eye for effective treatment of dry eye syndrome.Type: GrantFiled: March 16, 1988Date of Patent: April 11, 1989Assignee: University of Iowa Research FoundationInventors: Ronald D. Schoenwald, Charles F. Barfknecht
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Patent number: 4810727Abstract: 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: GrantFiled: August 6, 1987Date of Patent: March 7, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4808753Abstract: 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: GrantFiled: January 20, 1988Date of Patent: February 28, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4803226Abstract: 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: GrantFiled: January 6, 1988Date of Patent: February 7, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4791232Abstract: 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: GrantFiled: January 19, 1988Date of Patent: December 13, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4791233Abstract: 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: GrantFiled: January 19, 1988Date of Patent: December 13, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4791231Abstract: 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: GrantFiled: January 19, 1988Date of Patent: December 13, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4791123Abstract: 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: GrantFiled: January 22, 1987Date of Patent: December 13, 1988Assignee: Schering Akt.Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
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Patent number: 4789687Abstract: A food product comprising a food substance in combination with vanillylamine or a vanillylamide.Type: GrantFiled: January 13, 1987Date of Patent: December 6, 1988Assignee: Ajinomoto Co., Inc.Inventor: Kazuo Iwai
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Patent number: 4758561Abstract: 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: GrantFiled: July 22, 1985Date of Patent: July 19, 1988Assignee: Societe Cortial, S.A.Inventors: Guillaume Le Baut, Louis Sparfel, Marie-Helene Creuzet, Claude Feniou, Henri Pontagnier, Gisele Prat
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Patent number: 4757067Abstract: 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: GrantFiled: January 21, 1987Date of Patent: July 12, 1988Assignee: Societe Cortial, S.A.Inventors: Guillaume Le Baut, Louis Sparfel, Marie-Helene Creuzet, Claude Feniou, Henri Pontagnier, Gisele Prat