A Ring Or Polycyclo Ring System In A Substituent E Is Attached Indirectly To The Carboxamide Nitrogen Or To An Amino Nitrogen In Substituent E By Acyclic Nonionic Bonding Patents (Class 514/630)
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Patent number: 4988730Abstract: The invention relates to novel diphenylpropylamine derivatives of the general formula (I). ##STR1## R.sup.1 stands for hydrogen or a methyl group; R.sup.2 stands for hydrogen, a methyl or n-decyl group;Z means a phenyl group substituted by R.sup.3, R.sup.4 and R.sup.5, whereinR.sup.3 means hydrogen, fluorine, chlorine or bromine, or a nitro, C.sub.1-12 alkyl, C.sub.1-4 alkoxy, phenoxy or benzyloxy group;R.sup.4 and R.sup.5 represent hydrogen, chlorine or a hydroxy, alkoxy, benzyloxy, acetamino or carboxy group; orR.sup.4 and R.sup.5 together form a methylendioxy group;orZ may stand for a 4-methoxynaphtyl or 4-ethoxy-naphthyl group; andR.sup.6 stands for hydrogen or fluorine, with the proviso that each of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 cannot simultaneously stand for hydrogen, as well as their physiologically acceptable acid addition salts.The invention also relates to a process for the preparation of these compounds and to the pharmaceutical compositions containing these compounds.Type: GrantFiled: July 21, 1989Date of Patent: January 29, 1991Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyar RTInventors: Dezso Korbonits, Pal Kiss, Laszlo Szekeres, Gyula Papp, Gabor Kovacs, Andrea Santane Csutor, Sandor Virag, Eva Udvari, Imre Bata, Katalin Marmarosi nee Kellner, Laszlo Tardos, Peter Kormoczy, Vera Gergely, Zoltan Vargai
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Patent number: 4988679Abstract: There is provided an orally ingestible liquid composition for suspending therein an orally administrable pharmaceutically active composition releasable over an extended period of time comprises triglyceride of a medium chain length alkanoic acid or distilled acetylated monoglycerides, a liquid, high HLB polyglyceryl ester, and colloidal silicon dioxide together with a material soluble or dispersible therein and capable of being insolubilized by a pharmaceutically acceptable polyvalent cation and a solid pharmaceutically acceptable salt containing the cation required therefore. Sustained release compositions based thereon containing pharmaceutically active agents are also disclosed.Type: GrantFiled: June 19, 1989Date of Patent: January 29, 1991Inventors: Leonard Chavkin, Leonard Mackles
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Patent number: 4980366Abstract: Novel 4'-hydroxybenzylamine derivatives of the formula ##STR1## pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, succh as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.Type: GrantFiled: March 16, 1989Date of Patent: December 25, 1990Assignee: Warner-Lambert Co.Inventors: Graham Johnson, Michael F. Rafferty
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Patent number: 4975466Abstract: Pharmaceutical preparations for topical, i.e. dermal, application that contain as active ingredient a compound of the formula I ##STR1## especially 2-hydroxy-5-[(RS)-1-hydroxy-2-[[(RS)-1-(p-methoxyphenyl)-prop-2-yl]-amino] -ethyl]-formanilide (formoterol), or one of its pharmaceutically acceptable salts, especially its semifumarate, are proposed for the treatment of inflammatory skin diseases.Type: GrantFiled: December 7, 1988Date of Patent: December 4, 1990Assignee: Ciba-Geigy CorporationInventors: Irmgard Bottcher, Werner Pignat
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Patent number: 4960798Abstract: Acetylene compounds of the formula (I): ##STR1## wherein Y, R.sub.1, R.sub.2 R.sub.3, and R.sub.4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The compounds possess anti-hypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.Type: GrantFiled: January 26, 1990Date of Patent: October 2, 1990Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4943591Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein X represents a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain andY represents a bond, or a C.sub.1-4 alkylene, C.sub.2-4 alkenylene or C.sub.2-4 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 8;Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-3 alkyl, nitro, --(CH.sub.2).sub.q R [where R is hydroxy, C.sub.1-3 alkoxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represent a hydrogen atom, or a C.sub.1-4 alkyl group, or --NR.sup.3 R.sup.4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O-- or --S-- or a group --NH-- or --N(CH.sub.3)--), --NR.sup.5 COR.sup.6 (where R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.6 represents a hydrogen atom or a C.sub.Type: GrantFiled: October 14, 1986Date of Patent: July 24, 1990Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell
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Patent number: 4937267Abstract: A method of treatment of obesity or diabetes mellitus in a warm-blooded animal requiring such treatment which comprises administering to said animal an effective amount of the compound N-(2-[2-hydroxy-3-phenoxypropyl]aminoethyl)-isobutyramide in racemic (R,S) or levorotatory optically active (S) form, or of a pharmaceutically acceptable acid-addition salt thereof.Type: GrantFiled: March 10, 1987Date of Patent: June 26, 1990Assignee: Imperial Chemical Industries PLCInventors: Brian R. Holloway, Ralph Howe, Balbir S. Rao, Donald Stribling
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Patent number: 4933370Abstract: The present invention relates, by way of novel industrial products, to 1-(4-aminophenyl)-2-dimethylaminopropanone derivatives which are selected from:(a) the compounds having the general formula ##STR1## in which R is H or CH.sub.3 CO, and (b) addition salts thereof.These products are useful as antidepressants. Furthermore, 1-(4-acetylamino-3,5-dichlorophenyl)-2-dimethylaminopropanone and non-toxic addition salts thereof are useful as immunostimulants.Type: GrantFiled: January 31, 1989Date of Patent: June 12, 1990Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4925877Abstract: The present invention provides new physiological active substance erbstatin analogue compounds of a general formula (I), which have excellent tyrosine-specific protein-kinase inhibitory activity, antitumor activity and antimicrobial activity. ##STR1## (in which R.sup.1 represents a hydrogen atom, a lower alkanoyl group or a lower alkyl group; n represents a positive integer of 1 to 3;X represents a hydrogen atom or a halogen atom;Y represents a group of formula --CH.dbd.CH--NC, --CH.dbd.CH--NHR.sup.2 or --CH.sub.2 --CH.sub.2 --NHR.sup.2(where R.sup.2 represents a formyl group or a lower alkanoyl group; with the exception of the cases where X is hydrogen atom, (R.sup.1 O).sub.n group is 2,5-dihydroxy group and Y is --CH.dbd.CH--NHCHO or --CH.sub.2 --CH.sub.2 --NHCHO).The present invention further provides a tyrosine-specific protein-kinase inhibitor, tumoricide or bactericide containing at least one compound of the said formula (I).Type: GrantFiled: February 20, 1987Date of Patent: May 15, 1990Assignee: Zaidanhojin Biseibutsu Kagaku KenkyukaiInventors: Hamao Umezawa, deceased, Tomio Takeuchi, Kuniaki Tatsuta, Kunio Isshika, Masaya Imoto
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Patent number: 4904697Abstract: Certain chalcone derivatives are reported to inhibit the polymerization of tubulin to form microtubules and are therefore antimitotic agents which can be used to control the growth of tumor tissue and can be used as antigout agents.Type: GrantFiled: April 9, 1987Date of Patent: February 27, 1990Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Sai P. Sunkara, Michael L. Edwards, David M. Stemerick
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Patent number: 4904662Abstract: The fat content of sows' milk is increased, thereby increasing the energy supplied to the sow's piglets, by administering one of a small group of phenethanolamines.Type: GrantFiled: March 23, 1987Date of Patent: February 27, 1990Assignee: Eli Lilly and CompanyInventors: David B. Anderson, Edward L. Veenhuizen
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Patent number: 4902709Abstract: Novel antihypercholesterolemic compounds of structure (I) or (II), ##STR1## pharmaceutically acceptable salts, thereof and a novel process for preparing compounds of structure I, are disclosed.Type: GrantFiled: August 12, 1988Date of Patent: February 20, 1990Assignee: Merck & Co., Inc.Inventor: Gerald E. Stokker
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Patent number: 4898889Abstract: Acetylene compounds of the formula (I): ##STR1## wherein Y, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The compounds possess antihypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.Type: GrantFiled: March 27, 1989Date of Patent: February 6, 1990Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4885314Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) or (II): ##STR1## and pharmaceutically acceptable salts thereof the compounds of the formula (II) in which R.sup.1 is hydrogen are disclosed.Type: GrantFiled: September 1, 1988Date of Patent: December 5, 1989Assignee: Merck & Co., Inc.Inventors: Kamlesh P. Vyas, Hanumath P. Kari
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Patent number: 4882339Abstract: Disclosed are compounds of the formula ##STR1## wherein R.sub.1 represents unsubstituted or lower alkyl-substituted C.sub.3 -C.sub.7 -cycloalkyl, unsubstituted or lower alkyl substituted C.sub.7 -or C.sub.8 -bicycloalkyl, unsubstituted or lower alkyl-substituted adamantyl, 4-piperidinyl or N-lower alkyl or aryl-lower alkyl-substituted piperidinyl, 1- or 2-indanyl, 1- or 2-tetrahydronaphthyl, 1- or 2-perhydroindanyl, 1- or 2-perhydronaphthyl; R.sub.2 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, lower alkanoyl or aryl-lower alkanoyl; or R.sub.1 and R.sub.2 combined with the nitrogen to which they are attached represent pyrrolidino, piperidino, perhydroazepino, morpholino, thiomorpholino, tetrahydro- or perhydro-(isoquinolinyl or quinolinyl), dihydro- or perhydroindolyl, piperazino or N-lower alkyl-piperazino; R.sub.Type: GrantFiled: July 10, 1987Date of Patent: November 21, 1989Assignee: Ciba-Geigy CorporationInventor: Jan W. F. Wasley
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Patent number: 4880834Abstract: A method for treating livestock to decrease birth mortality rate and to increase post-natal survival rate by administering ethanolamine derivatives is disclosed.Type: GrantFiled: October 30, 1986Date of Patent: November 14, 1989Assignee: Beecham Group p.l.c.Inventor: Jonathan R. Arch
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Patent number: 4880840Type: GrantFiled: June 30, 1987Date of Patent: November 14, 1989Assignee: Bayer AktiengesellschaftInventors: Hans Lindel, Axel Ingendoh, Friedrich Berschauer, Anno de Jong, Martin Scheer
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Patent number: 4877812Abstract: The present invention relates, by way of new industrial products, to 1-(acetylaminophenyl)-2-amino-propanone derivatives selected from the group consisting of(a) the compounds of the formulaAr--CO--CH(CH.sub.3)--NR.sub.1 R.sub.2 (I)in whichR.sub.1 represents a C.sub.1 -C.sub.4 alkyl group or a C.sub.3 -C.sub.6 cycloalkyl group;R.sub.2 represents the hydrogen atom or a C.sub.1 -C.sub.4 alkyl group;R.sub.1 and R.sub.2, taken together, can form, with the nitrogen atom to which they are bonded, an N-heterocyclic group with 5 to 7 ring members, capable (i) of including a second heteroatom selected from N, O and S, and (ii) of being substituted, the said heterocyclic group NR.sub.1 R.sub.2 being selected from the group comprising pyrrolidino, morpholino, thiomorpholino, piperidino, hexamethyleneimino, piperazino, 4-methylpiperazino, 4-(.beta.-hydroxyethyl) piperazino, 4-phenylpiperazino and 4-(p-chlorophenyl)-piperazino groups; andAr represents an acetylaminophenyl group of the formula ##STR1## in which X is CH.Type: GrantFiled: April 16, 1987Date of Patent: October 31, 1989Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4863968Abstract: Certain chalcone derivatives are reported to inhibit the polymerization of tubulin to form microtubules and are therefore antimitotic agents which can be used as antigout agents. The chalcone derivatives are also reported to inhibit the destruction of the myelin sheath in the central nervous system of multiple sclerosis patients and are thus useful in controlling the progressive nature of the disease.Type: GrantFiled: December 14, 1988Date of Patent: September 5, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Michael L. Edwards, Sai P. Sunkara, David M. Stemerick
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Patent number: 4859706Abstract: Carboxamides of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.3 -C.sub.10 -cycloalkyenyl or C.sub.4 -C.sub.10 -cycloalkenylalkyl, and R.sup.2 and R.sup.3 are each hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.3 -haloalkyl. C.sub.1 -C.sub.3 -haloalkoxy or methylthio, and their use for combating pests.Type: GrantFiled: August 6, 1987Date of Patent: August 22, 1989Assignee: BASF AktiengesellschaftInventors: Rainer Buerstinghaus, Peter Hofmeister, Christoph Kuenast
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Patent number: 4829064Abstract: Pharmaceutical compositions and methods of using same comprising aspirin, sodium salicylate, salicylamide or acetaminophen, in combination with a non-sedating antihistamine and optionally one or more other active components selected from a decongestant, cough suppressant (antitussive) or expectorant are provided for the relief of cough, cold, cold-like and/or flu symptoms and the discomfort, pain, headache, fever and general malaise associated therewith.Type: GrantFiled: June 8, 1987Date of Patent: May 9, 1989Assignee: Analgesic AssociatesInventors: Abraham Sunshine, Eugene M. Laska, Carole E. Siegel
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Patent number: 4829089Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.Type: GrantFiled: July 22, 1988Date of Patent: May 9, 1989Assignee: American Cyanamid CompanyInventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
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Patent number: 4752621Abstract: Intraocular hypertensive diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is alkyl of two to four carbon atoms;R.sub.2 is --(CH.sub.2).sub.n --C.sub.6 H.sub.4 --R.sub.5 ; wheren is an integer from 1 to 4; andR.sub.5 is --H, --OH, halo, lower alkyl, lower alkoxy, ureido, lower alkyl-ureido, lower alkyl-amido, or formamido;R.sub.3 is hydro or hydroxy; andR.sub.4 is hydro, lower alkyl, amino, or lower alkylamino.Type: GrantFiled: August 25, 1986Date of Patent: June 21, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: Robin D. Clark, L. David Waterbury
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Patent number: 4710519Abstract: The subject invention relates to a process for preparing acetaminophen powders by spray drying the acetaminophen in the presence of various excipients. Preferably a lubricant is incorporated into the acetaminophen powder during the spray drying process or after the spray drying process by passing the spray dried acetaminophen powder through a fluidized bed dryer which contains a lubricant.Type: GrantFiled: September 30, 1985Date of Patent: December 1, 1987Assignee: BASF CorporationInventors: Jeffrey L. Finnan, Rudolph E. Lisa, Douglass N. Schmidt
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Patent number: 4699920Abstract: The invention relates to 9-halo-.DELTA..sup.2 -prostane derivatives of general Formula I ##STR1## wherein Hal is a fluorine or chlorine atom in the .alpha.- or .beta.-position,R.sub.1 is the residue OR.sub.2 with R.sub.2 meaning a hydrogen atom, alkyl, cycloalkyl, aryl or a heterocyclic residue; or the residue NHR.sub.3 wherein R.sub.3 means an acid residue or the residue R.sub.2 andA is a --CH.sub.2 --CH.sub.2 -- or cis-CH.dbd.CH--group,B is a --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH-- or --C.tbd.C--group,W is a free or functionally modified hydroxymethylene or ##STR2## wherein the respective OH-groups can be in the .alpha.- or .beta.-position,D and E jointly mean a direct bond orD is a straight- or branched-chain alkylene group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms,E is an oxygen or sulfur atom, a direct bond, a --C.tbd.C--bond or a --CR.sub.6 .dbd.CR.sub.7 --group wherein R.sub.6 is a hydrogen atom or an alkyl group and R.sub.Type: GrantFiled: September 17, 1985Date of Patent: October 13, 1987Assignee: Schering AktiengesellschaftInventors: Werner Skuballa, Bernd Raduchel, Helmut Vorbruggen, Walter Elger, Olaf Loge
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Patent number: 4657929Abstract: There are provided pharmaceutical compounds useful in treating hypertension, heart diseases and renal failure. These compounds are 4-hydroxy phenethylamines wherein the 3 position on the phenyl nucleus is occupied by either an amino, amide, carbamyl, urea sulfonamide, substituted alkyl or fluorine atom, and the amine group is further linked to another phenyl radical through an alkylene radical which may contain nitrogen, oxygen, sulfur or cyclic hydrocarbon radicals as intervening groups.Type: GrantFiled: October 18, 1984Date of Patent: April 14, 1987Assignee: Fisons plcInventors: Francis Ince, Alan C. Tinker
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Patent number: 4652584Abstract: Phenoxypropanol derivatives having a 2-acetylenic moiety on the phenyl group thereof of the following formula (I): ##STR1## and their use as anti-hypertensives, e.g. in man. Also part of the invention are pharmaceutical compositions and intermediates used in the synthesis.Type: GrantFiled: July 13, 1984Date of Patent: March 24, 1987Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4619944Abstract: Provided are antihypertensive compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different,m is an integer from 0 to 2 inclusive,n is an integer from 0 to 4 inclusive,M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl.Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl-alkyl, heterocyclic, --CO--SR, --CS--SR, ##STR2## CH.sub.2 CO.sub.2 R, --CHM--CO.sub.2 R, --CH.sub.2 --CO--SR, --CN, ##STR3## --CO--NH--CH.sub.2 CO.sub.2 R, ##STR4## or --CO--CO.sub.Type: GrantFiled: February 19, 1985Date of Patent: October 28, 1986Assignee: USV Pharmaceutical CorporationInventors: Raymond D. Youssefyeh, Howard Jones
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Patent number: 4588747Abstract: 2-dipropylamino-5 or -7-formylamino-6-hydroxy-1,2,3-4-tetrahydronaphthalene and their pharmaceutically acceptable salts are useful as antiglaucoma agents.Type: GrantFiled: August 29, 1985Date of Patent: May 13, 1986Assignee: SynthelaboInventors: Icilio Cavero, Salomon Z. Langer
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Patent number: 4540695Abstract: Aminonaphthacene derivatives of the formula: ##STR1## wherein A is either one of the following groups: ##STR2## wherein R.sup.1 is a hydrogen atom or a group of the formula: --COR.sup.7, R.sup.2 and R.sup.3 are each a lower alkoxy group or, when taken together, represent an ethylenedioxy group or an oxo group, R.sup.4 and R.sup.5 are both hydrogen atoms or either one of them is a hydrogen atom and the other is a group of the formula: --COR.sup.7, R.sup.6 is a hydrogen atom, a hydroxyl group or a group of the formula: --OCOR.sup.7 and R.sup.7 is a lower alkyl group, a halo(lower)alkyl group, a phenyl group or a halophenyl group, which are useful as anti-microbial and/or anti-tumor agents, or as intermediates in their production.Type: GrantFiled: August 11, 1982Date of Patent: September 10, 1985Assignee: Sumitomo Chemical Co., Ltd.Inventors: Kikuo Ishizumi, Naohito Ohashi, Michihisa Muramatsu