Plural Hetero Atoms In The Hetero Ring Patents (Class 514/439)
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Patent number: 5037825Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.6 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.Type: GrantFiled: July 10, 1989Date of Patent: August 6, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
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Patent number: 5017618Abstract: Compounds having the formula ##STR1## and their pharmaceutically acceptable acid addition salts, wherein --X-- is --O--, --CH.sub.2 -- or --; .dbd.Y is .dbd.O or a derivatized keto group which is hydrolyzable or enzymatically convertible to a keto group; R is alkyl having from 1 to 12 carbon atoms or aralkyl having from 7 to 20 carbon atoms; and Ar is the 3-aromatic or heterocyclic residue of a 1-alkylamino-2-propanol having an aromatic or heterocyclic substituent at the 3-position and having .beta.-adrenergic blocking properties; are useful as .beta.-adrenergic blocking agents and are of particular interest in the treatment of glaucoma or for lowering intraocular pressure.Type: GrantFiled: September 18, 1989Date of Patent: May 21, 1991Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 4987130Abstract: Substituted amino derivatives represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each stand for an acyclic hydrocarbon residue or an alicyclic hydrocarbon residue; R.sup.3 and R.sup.4 each stand for hydrogen or a hydrocarbon residue optionally containing hetero-atom(s); A stands for a carbon chain having two or more carbon atoms optionally containing ether linkage or sulfide linkage, which may be substituted and which may per se form a ring; X.sup.1 and X.sup.2 each stand for oxygen atom or sulfur atom; and Y stands for amino group or an organic residue bonded through nitrogen atom, which may form a ring by combining with a carbon atom constituting A; and their salts have anti-arrhythmic activity and are useful for prevention and treatment of a variety of arrhythmias.Type: GrantFiled: December 22, 1989Date of Patent: January 22, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Susumu Tsushima, Muneo Takatani, Minoru Hirata
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Patent number: 4987132Abstract: A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.Type: GrantFiled: August 16, 1988Date of Patent: January 22, 1991Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Toshiyasu Mase, Hiromu Hara, Hitoshi Nagaoka, Takumi Takahashi, Takeshi Suzuki, Kenichi Tomioka, Toshimitsu Yamada
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Patent number: 4963537Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: April 26, 1989Date of Patent: October 16, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
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Patent number: 4957941Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## where Y is H or OH;j is an integer from 0 to 4;k is an integer from 0 to 4, and whereinm is an integer from 1 to 4;n is an integer from 1 to 4;p is an integer from 1 to 4; andX may be nonexistent or may be O, S, NH or CH.sub.2 or salts thereof, but when X is nonexistent the terminal group in which both the n-chain and the p-chain is a methyl group. ##STR2## The reaction was performed under reflux condensation. Following the reaction, which was usually complete within a few hours, the acid chlorides were vacuum distilled and reacted with a thiol compound as described above.The compounds of this invention are anti-muscarinic agents (cholinergic-muscarinic receptor antagonists) which inhibit the actions of acetylcholine on autonomic effectors innervated by postganglionic cholinergic nerves as well as on smooth muscle that lacks cholinergic innervation.Type: GrantFiled: January 9, 1990Date of Patent: September 18, 1990Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
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Patent number: 4927845Abstract: Anthralin analogues containing a thio-substituent, especially in one or more of the positions 2-, 7- and 10- of the anthralin ring. They may be made by reacting an anthralin derivative (e.g. 10-bromoanthralin) with a thiol or a compound containing a group convertible to a thio-group. Alternatively, a 1,8-dihydroxy anthraquinone containing a thio-substituent may be reduced. Reactive intermediates may be made by introducing one or more nuclear allylic groups into a 1,8-dihydroxy anthraquinone and then converting them into a reactive form, e.g. by epoxidation or halide addition. The intermediate can then reduced to the oxidation state corresponding to anthralin.Additional products having the 10-carbon atom of the anthralin ring as part of a heterocyclic ring, may be made by anthralins containing various substitutes thioalkyl groups as the 10-substituent.The compounds are useful for treatment of psoriasis, and may be formulated in the conventional vehicles for topical application, for example petrolatum.Type: GrantFiled: August 15, 1989Date of Patent: May 22, 1990Assignee: The Victoria University of ManchesterInventor: John M. Bruce
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Patent number: 4876270Abstract: Novel substituted .alpha.,.alpha.-diphenylethylene derivatives of formula I ##STR1## in which R.sub.1 and R.sub.4 independently of one another each represents hydrogen, hydroxy, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.1 -C.sub.3 -alkoxy substituted by from 1 to 7 halogen atoms, alkoxyalkoxy having a total of from 2 to 6 carbon atoms, C.sub.3 -C.sub.5 -alkenyloxy or C.sub.3 -C.sub.5 -alkynyloxy;R.sub.2 and R.sub.3 independently of one another each represents hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.5 -alkoxy or nitro; orR.sub.1 and R.sub.2 together represent a radical --O--CH.sub.2 --O-- or --O--CH.sub.2 --CH.sub.2 --O--;R.sub.5 and R.sub.6 independently of one another each represents hydrogen, halogen or methyl;R.sub.7 and R.sub.Type: GrantFiled: February 10, 1988Date of Patent: October 24, 1989Assignee: Ciba-Geigy CorporationInventor: Hans-Rudolf Waespe
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Patent number: 4871762Abstract: Compounds formula (I): ##STR1## in which: R.sup.1 represents a hydrogen atom, an alkyl group, a substituted alkyl group, a C.sub.2 -C.sub.6 alkenyl group, an aryl group, a substituted aryl group or an alkoxycarbonyl group wherein the alkoxy part has from 1 to 6 carbon atoms; R.sup.2 represenets a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.3 or C.sub.4 alkenyl group; R.sup.3 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.4 represents a hydroxy group, a C.sub.1 -C.sub.21 aliphatic acyloxy group or a carbocyclic aryl carboxylic aryloxy group; R.sup.5 represents a C.sub.1 -C.sub.12 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a hydroxy group, a C.sub.1 -C.sub.7 aliphatic acyloxy group or a carbocyclic aryl carboxylic acyloxy group; R.sup.6 represents a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.1 -C.sub.6 alkoxy group; and n is 0, 1, or 2;and pharmaceutically acceptable salts thereof are valuable in the treatment of circulatory disorders and allergies.Type: GrantFiled: December 24, 1987Date of Patent: October 3, 1989Assignee: Sankyo Company, LimitedInventors: Takao Yoshioka, Eiichi Kitazawa, Mitsuo Yamazaki, Yoshio Iizuka
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Patent number: 4870098Abstract: This invention encompasses compounds of Formula I ##STR1## and the pharmaceutically acceptable salts and geometrical and optical isomers thereof wherein:Alk is alkylene or hydroxyalkylene containing 1-6 carbon atoms;Ar is 5,6,7,8-tetrahydro-1-naphthalenyl or phenyl optionally substituted with one or more substituents selected from lower alkyl containing 1 to 6 carbon atoms, hydroxy, lower alkoxy containing 1 to 6 carbon atoms, or lower alkanoyl containing 1 to 6 carbon atoms;R is hydrogen and lower alkyl containing 1 to 6 carbon atoms;X, Y, and Z are each independently O or S with S optionally oxidized to S.dbd.O;m is an integer from 0 to 3;n is an integer from 0 to 5.The compounds are useful as anti-allergy agents and anti-inflammatory agents.Type: GrantFiled: January 17, 1989Date of Patent: September 26, 1989Assignee: G. D. Searle & Co.Inventors: Michael A. Stealey, Richard M. Weier
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Patent number: 4863940Abstract: Certain N-acetonyl-substituted-amides of the formula: ##STR1## wherein A is a heterocycle, a phenylalkyl, a phenylalkoxy, naphthyl, cycloalkyl, alkoxyalkyl, alkyl, haloalkyl or alkenyl group; X, Y and Z are selected from the group consisting of hydrogen, halo, cyano, thiocyano, isothiocyano, methylsulfonyloxy, thio(C.sub.1 -C.sub.2) alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyloxy, thiocarbamoylthio, hydroxy, azide, trifluoromethylcarboxy, (C.sub.1 -C.sub.4)alkylcarbonyloxy, phenylcarbonyloxy, phenoxy, thiophenyl, imidazolyl or triazolyl group as described herein; R.sup.1 and R.sup.2 are each independently a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group; and compositions containing these amides are fungicidally active, particularly against phytopathogenic fungi.Type: GrantFiled: July 26, 1984Date of Patent: September 5, 1989Assignee: Rohm and HaasInventor: Ashok K. Sharma
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Patent number: 4855138Abstract: According to the present invention, a skin therapeutic mixture is useful for the alleviation of certain skin disorders such as acne, psoriasis, burns, pimples, blackheads, and open sores, and such mixture comprises: the therapeutic agent being the extract from the dried leaves of the Matico plant; a preservative chosen from the group consisting of a sulfaderivative such as sulfathiazole and an alcohol amine; a skin softener such as an oil; and an oil soluble base. An inert pigment such as zinc oxide and a fragrance such as a perfume may be added. According to a specific illustrative embodiment of the present invention, the skin therapeutic mixture comprises about 2% to 35% by weight of the extract from the dried leaves of the Matico plant as the therapeutic agent; about 2% to 15% by weight of sulfathiazole as the preservative; about 5% to 10% by weight of zinc oxide as the inert white pigment; and about 40% to 91% by weight of petrolatum.Type: GrantFiled: June 24, 1986Date of Patent: August 8, 1989Assignee: Tecma Laboratories, Inc.Inventor: Theodore Trenzeluk
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Patent number: 4803286Abstract: Certain amino-2-hydroxypropyloximinoheterocycles are .beta.-adrenoceptor antagonists useful in the treatment of elevated intraocular pressure, hypertension, angina and arrhythmia.Type: GrantFiled: August 19, 1987Date of Patent: February 7, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, David C. Remy, David A. Claremon, Stella W. King
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Patent number: 4785002Abstract: A method of combating fungi or regulating the growth of plants which comprises applying to such fungi, such plants or to a fungus or plant growth situs an amount effective therefor of an imidazo-pyrrolo-pyridine of the formula ##STR1## in which R.sup.1 represents cyano, alkoxycarbonyl or aminocarbonyl,R.sup.2 represents hydrogen, alkyl, trimethylsilyl or one equivalent of a metal cation andR.sup.3 and R.sup.4 independently of one another each represent alkyl, cycloalkyl or cycloalkylalkyl orR.sup.3 and R.sup.4 together represent a divalent alkanediyl radical.Many of the compounds are new.Type: GrantFiled: October 1, 1986Date of Patent: November 15, 1988Assignee: Bayer AktiengesellschaftInventors: Wilfried Draber, Gerd Hanssler, Klaus Lurssen
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Patent number: 4780317Abstract: A sustained release antimicrobial agent comprises a clathrate compound composed of a water-soluble microbicide and at least one of the compounds shown at (I) to (V) below:(I) 1,1'-bi-2-naphthol;(II) 1,1,4,4-tetraphenyl-2-butyn-1,4-diol;(III) 9,10-di(4-methylphenyl)-9,10-dihydroznthracene-9,10-diol;(IV) 1,1-bis(4-hydroxyphenyl)-cyclohexane; and(V) 1,1,6,6-tetra(2,4-dimethylphenyl)-2,4-hexadiyne-1,6-diol.A method which uses it for preventing the fouling of a water system is also disclosed.Type: GrantFiled: January 22, 1987Date of Patent: October 25, 1988Assignee: Kurita Water Industries Ltd.Inventors: Ayako Sekikawa, Hideo Sugi, Kenji Tahara, Fumio Toda
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Patent number: 4740522Abstract: Novel oxolabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: August 28, 1986Date of Patent: April 26, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Nicholas J. Hrib
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Patent number: 4691027Abstract: Compounds formula (I): ##STR1## in which: R.sup.1 represents a hydrogen atom, an alkyl group, a substituted alkyl group, a C.sub.2 -C.sub.6 alkenyl group, an aryl group, a substituted aryl group or an alkoxycarbonyl group wherein the alkoxy part has from 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.3 or C.sub.4 alkenyl group; R.sup.3 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.4 represents a hydroxy group, a C.sub.1 -C.sub.21 aliphatic acyloxy group or a carbocyclic aryl carboxylic acyloxy group; R.sup.5 represents a C.sub.1 -C.sub.12 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a hydroxy group, a C.sub.1 -C.sub.7 aliphatic acyloxy group or a carbocyclic aryl carboxylic acyloxy group; R.sup.6 represents a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.1 -C.sub.6 alkoxy group; and n is 0, 1, or 2; and pharmaceutically acceptable salts thereof are valuable in the treatment of circulatory disorders and allergies.Type: GrantFiled: March 26, 1985Date of Patent: September 1, 1987Assignee: Sankyo Company, LimitedInventors: Takao Yoshioka, Eiichi Kitazawa, Mitsuo Yamazaki, Yoshio Iizuka
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Patent number: 4677103Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: October 20, 1986Date of Patent: June 30, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
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Patent number: 4666904Abstract: Novel aminoacyllabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: October 20, 1986Date of Patent: May 19, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
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Patent number: 4626529Abstract: The present invention discloses a homogeneous oily composition essentially consisting of a dermatological active principle, an oily compound and an oil-soluble surface-active component, the oil-soluble surface-active component comprising an anionic surface-active agent, the acid group of which has been neutralized by an amine, generally comprising 0.01 to 15% by weight of active principle, 5 to 85% by weight of oily compound and 15 to 95% by weight of oil-soluble surface-active agent.Type: GrantFiled: November 20, 1984Date of Patent: December 2, 1986Assignee: L'orealInventor: Jean F. Grollier
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Patent number: 4542130Abstract: MIcrobicidally active 5-aminomethyl-1,3-oxathiolanes of the formula ##STR1## in which R.sup.1 is tetrahydronaphthyl, decahydronaphthyl or optionally substituted naphthyl, optionally substituted cycloalkyl or cycloalkenyl, optionally substituted phenyl, or alkyl which is substituted by phenyl, phenoxy, phenylthio, cyclohexyl, cyclohexyloxy or cyclohexylthio, each of which is optionally substituted,R.sup.2 is hydrogen or methyl,R.sup.3 is alkyl, andR.sup.4 is alkyl, alkenyl or optionally substituted aralkyl, orR.sup.3 and R.sup.4, together with the nitrogen atom to which they are bonded, form an optionally substituted saturated heterocyclic structure which can contain further heteroatoms,or a plant-tolerated addition product thereof with an acid or metal salt.Type: GrantFiled: June 27, 1984Date of Patent: September 17, 1985Assignee: Bayer AktiengesellschaftInventors: Joachim Weissmuller, Wolfgang Kramer, Dieter Berg, Paul Reinecke, Wilhelm Brandes, Gerd Hanssler
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Patent number: RE32868Abstract: The invention concerns cyclic imides, diones, reduced diones and analogs thereof which are useful as antihyperlipidemic agents to reduce serum cholesterol and trigylcerides.Type: GrantFiled: July 26, 1985Date of Patent: February 14, 1989Assignee: Research CorporationInventors: Iris H. Hall, George H. Cocolas, James H. Chapman, Jr.