The Hetero Ring Has At Least Seven Members Patents (Class 514/431)
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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: 5264441Abstract: The invention provides new ureas and thioureas derivatives of general formula (I) ##STR1## and pharmaceutically acceptable salts thereof, which are useful as therapeutic agents such as for the prevention of coronary heart disease and as antidyslipidaemic agents.Type: GrantFiled: February 18, 1992Date of Patent: November 23, 1993Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Paolo Cozzi, Danielle Fancelli, Dino Severino, Augusto Chiari, Giancarlo Ghiselli
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Patent number: 5260310Abstract: Novel compounds of the formula ##STR1## wherein Q, R.sup.1 and R.sup.2 are described herein, are disclosed along with pharmaceutical compositions, methods of use, and process for producing compounds of formula I which starts from the corresponding .beta.-hydroxycarboxylic acids.Type: GrantFiled: August 12, 1992Date of Patent: November 9, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Romano Derungs, Hans P. Marki, Henri Stalder, Andre Szente
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Patent number: 5242912Abstract: The following cyclic anthranilic acid derivative, their acid addition salts or alkali salts thereof represented by a general formula [I] are useful for antirheumatic drug, autoimmune disease curing drug and metabolic bone disease curing drug. ##STR1## wherein R.sup.1 to R.sup.6 and X are as defined in claim 1.Type: GrantFiled: April 25, 1991Date of Patent: September 7, 1993Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Mitsutomo Miyashita, Yasushi Kohno, Eisuke Kojima, Koji Saito
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Patent number: 5192765Abstract: Amines of the following formula: ##STR1## where the variables are defined in the specification are useful in the treatment of diseases associated with altered motility and/or tone of smooth muscle.Type: GrantFiled: June 6, 1991Date of Patent: March 9, 1993Assignee: Pfizer Inc.Inventors: David Alker, Robert J. Bass, Peter E. Cross
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Patent number: 5190971Abstract: The invention relates to substituted dibenz-oxa-thiocinone-12-oxides and -12,12-dioxides of the general formula I ##STR1## in which R.sup.1 to R.sup.6 and Y have the meaning indicated in the description, to processes for their preparation and to their use in medicaments, in particular in circulation-influencing medicaments.Type: GrantFiled: November 26, 1991Date of Patent: March 2, 1993Assignee: Bayer AktiengesellschaftInventors: Peter Fey, Klaus Frobel, Jan-Bernd Lenfers, Andreas Knorr, Johannes-Peter Stasch, Erwin Bischoff, Hans-Georg Dellweg, Martin Beuck
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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: 5164387Abstract: 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.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)=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: May 28, 1991Date of Patent: November 17, 1992Assignee: Hoffmann-LaRoche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
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Patent number: 5158943Abstract: A sulfur-containing hetrocyclic compound of the formula (I) ##STR1## wherein the ring A is an optionally substituted benzene ring, R is a hydrogen atom or an optionally substituted hydrocarbon residue, B is a carboxyl group which may be esterified or amidated, X is --CH(OH)-- or --CO--, and n is an integer of 0, 1 or 2, or its salt, which is useful in the prevention or treatment of osteoporosis.Type: GrantFiled: May 23, 1991Date of Patent: October 27, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Iwao Yamazaki
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Patent number: 5153225Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine or a group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andx denotes oxygen, sulphur or NR.sup.5,and their salts.Type: GrantFiled: April 9, 1991Date of Patent: October 6, 1992Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 5139785Abstract: Pesticides containing at least one compound of the formula I ##STR1## where M denotes carbon or silicon,X denotes CH.sub.2, O, S, NR.sup.6,R.sup.1 denotes (C.sub.2 -C.sub.18)alkyl, (C.sub.5 -C.sub.7)cycloalkyl, (C.sub.2 -C.sub.8)alkenyl, phenyl, naphthyl, pyridyl, pyrimidyl, pyridazinyl, pyrazinyl, 1,2,4-triazinyl or 1,2,4,5-tetrazinyl, it being possible for all these substituents to be monosubstituted or polysubstituted,R.sup.2, R.sup.3 independently of one another denote (C.sub.1 -C.sub.3)alkyl, (C.sub.2 -C.sub.8)alkenyl or phenyl, or R.sup.2 and R.sup.3 denote an alkylene chain which--together with the quaternary central atom (M)--form an unsubstituted or fluorine-substituted ring having four to six ring members (where M=Si) or having three to six ring members (where M=C),R.sup.4 denotes --H, --CN, --CCl.sub.3, --C.tbd.CH, (C.sub.1 -C.sub.4)alkyl, F, ##STR2## R.sup.5 denotes pyridyl, furyl or thienyl, each of which can be substituted, phthalimidyl, di(C.sub.1 -C.sub.Type: GrantFiled: February 19, 1991Date of Patent: August 18, 1992Assignee: Hoechst AktiengesellschaftInventors: Anna Waltersdorfer, Manfred Kern, Werner Knauf, Hans H. Schubert
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Patent number: 5118701Abstract: Novel tricyclic compound represented by formula (I): ##STR1## possess a TXA.sub.2 biosynthesis inhibiting activity and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: November 14, 1990Date of Patent: June 2, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 5098928Abstract: The ketenedithioacetal derivatives of formula (I) have a potent hypolipidemic and anti-arteriosclerotic effect and are useful for prophylaxis and treatment of arteriosclerosis or hyperlipidemia.Type: GrantFiled: October 25, 1990Date of Patent: March 24, 1992Assignee: Nihon Nohyaku Co., Ltd.Inventors: Masashi Nagamine, Kunikazu Hiraga, Atsushi Sakai, Matazaemon Uchida
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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: 5071841Abstract: The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon group which may be substituted; B is a carboxyl group which may be esterified or amidated; X is --CH(OH)-- or --CO--; k is 0 or 1; and k' is 0, 1 or 2 or a pharmaceutically acceptable salt thereof.Also, it provides a process for producing the compound (I) or a salt thereof and a pharmaceutical preparation for use in the treatment of osteoporosis comprising the compound (I) or salt thereof.The compounds (I) and salts thereof show excellent bone resorption inhibitory activity.Type: GrantFiled: December 28, 1989Date of Patent: December 10, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Masao Tsuda, Iwao Yamazaki
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Patent number: 5066649Abstract: The invention relates to a new group of 8,9-annelated-1,2,3,4-tetrahydro-.beta.-carbolines of the formula ##STR1## and the salts and prodrugs thereof. The meanings of R.sub.1, n, Z, R.sub.2, R.sub.3, and R.sub.4 are defined within the body of the specification.It has been found that the compounds have good fibrinolytic properties and can be used in particular as orally active fibrinolytics.Type: GrantFiled: January 16, 1990Date of Patent: November 19, 1991Assignee: Duphar International Research B.V.Inventors: Derk Hamminga, Ineke van Wijngaarden, Johannes W. C. M. Jansen
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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: 5036067Abstract: Compounds having the formula I: ##STR1## are inhibitors of the 5-lipoxygenase enzyme. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: March 14, 1990Date of Patent: July 30, 1991Assignee: Merck & Co., Inc.Inventors: Yves Girard, Pierre Hamel, Daniel Delorme
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Patent number: 5026857Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine or a group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andx denotes oxygen, sulphur or NR.sup.5,and their salts.Type: GrantFiled: July 12, 1989Date of Patent: June 25, 1991Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 5023252Abstract: The rate of absorption of drugs across skin and other body membranes such as mucous membranes and the blood brain barrier is enhanced by adding to the drug composition a compound which enhances the rate. This compound may be macrocyclic ester, diester, amide, diamide, amidine, diamidine, thioester, dithioester, thioamide, ketone or lactone. The macrocyclic ketone contains at least 12 carbon atoms.Type: GrantFiled: December 8, 1989Date of Patent: June 11, 1991Assignee: Conrex Pharmaceutical CorporationInventor: Dean Hseih
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Patent number: 5001144Abstract: Disclosed are novel 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.Phamaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.Type: GrantFiled: April 17, 1990Date of Patent: March 19, 1991Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: John R. Regan, Kent W. Neuenschwander
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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: 4959385Abstract: This invention relates to thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Ar represents optionally substituted phenyl, Y represents an ethylene or methylene radical or a valency bond, and n represents 0 or 1, bioprecursors thereof and pharmaceutically acceptable salts thereof which possess useful pharmacological properties, processes for their preparation and compositions containing them.Type: GrantFiled: January 19, 1989Date of Patent: September 25, 1990Assignee: May & Baker LimitedInventors: David C. Cook, Terance W. Hart, Iain M. McLay, Malcolm N. Palfreyman, Roger J. Walsh, Jean-Claude Aloup
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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: 4938797Abstract: The invention relates to a process for the preparation of microcapsules having a capsule wall of polyurea and encapsulating a water-immiscible pesticide. The process comprises first dispersing a solution of a polyisocyanate in the sparingly water-soluble pesticide, in the presence of an anionic dispersant and at least one nonionic protective colloid and/or a nonionic surfactant, and subsequently reacting the dispersion with a polyamine, to give a stable aqueous suspension of microcapsules which can be used either direct or after dilution with water as pesticidal composition.Type: GrantFiled: June 7, 1988Date of Patent: July 3, 1990Assignee: Ciba-Geigy CorporationInventors: Hans W. Hasslin, Michael J. Hopkinson
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Patent number: 4925657Abstract: The invention provides insecticidal compositions for combatting aphids, which compositions contain an aphid insecticide in an amount lower than the minimum usual percentage for said insecticide in an aphicidal composition and an alarm pheromone for aphids. The compositions of the invention are less toxic because of the reduced insecticide content but they are not less effective than the insecticidal compositions which do not contain an alarm pheromone.Type: GrantFiled: June 29, 1987Date of Patent: May 15, 1990Assignee: Denka International B.V.Inventors: Antonie A. Den Braber, Evert R. Slootweg
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Patent number: 4904688Abstract: The present invention deals with dibenzo-oxocin-, dibenzo-thiocin-, dibenzo-azocin- and dibenzocyclo-octenamine derivatives suitable for use as antipsychotic compounds without extra-pyrimidal side-effects.Type: GrantFiled: March 8, 1989Date of Patent: February 27, 1990Assignee: Akzo N.V.Inventors: Duncan R. Rae, James Cairns
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Patent number: 4882351Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formula (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.Type: GrantFiled: October 11, 1988Date of Patent: November 21, 1989Assignee: Roussel UclafInventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 4870103Abstract: The invention relates to plant protection agents based on aqueous microemulsions which contain, as emulsifiers, ethoxylated and phosphorylated, styryl-substituted phenols or salts thereof in combination with one or more non-phosphorylated emulsifiers belonging to the group comprising salts of (C.sub.10 -C.sub.16)-alkyl-monoglycol to -hexaglycol ether-sulfates, salts of .alpha.-(C.sub.14 -C.sub.19)-alkenol sulfates, salts of optionally chlorinated (C.sub.13 -C.sub.18)-alkanesulfonic acids, salts of dodecylphenylsulfonic acid, amine oxethylates or .alpha.(C.sub.9 -C.sub.20)-alkyl-.omega.-hydroxypolyoxyethylenes containing 2 to 22 moles of ethylene oxide.Type: GrantFiled: July 21, 1987Date of Patent: September 26, 1989Assignee: Hoechst AktiengesellschaftInventors: Hans Rochling, Konrad Albrecht
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Patent number: 4863922Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.Type: GrantFiled: June 15, 1988Date of Patent: September 5, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
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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: 4775683Abstract: Novel aminoalkylthiodibenzothiepins and related compounds, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as antidepressant, analgetic, and anticonvulsant agents.Type: GrantFiled: February 13, 1987Date of Patent: October 4, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
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Patent number: 4775682Abstract: Novel aminoalkylthiodibenzothiepins and related compounds, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as antidepressant, analgetic, and anticonvulsant agents.Type: GrantFiled: February 13, 1987Date of Patent: October 4, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
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Patent number: 4766143Abstract: Novel aminoalkylthiodibenzothiepins and related compounds, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as antidepressant, analgetic, and anticonvulsant agents.Type: GrantFiled: February 12, 1987Date of Patent: August 23, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
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Patent number: 4710512Abstract: Liquid formulations of the pesticide amitraz are stabilized by the addition of one or more aluminum alkoxides.Type: GrantFiled: October 14, 1986Date of Patent: December 1, 1987Assignee: Schering Agrochemicals LimitedInventor: Michael A. Webb
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Patent number: 4699919Abstract: This invention relates to bicyclic catechol derivatives having the general formulae I and II ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and Z represent various substituents, to a preparation process of the same comprising reacting a compound of formula III ##STR2## wherein R.sub.1 and R.sub.2 have the meanings given above with an appropriately substituted propionic or butyric acid (or an ester or a salt of the same) of formula IV ##STR3## wherein R.sub.3 has the meaning given above, and to therapeutical compositions wherein the active ingredient is one of these compounds.Type: GrantFiled: September 16, 1986Date of Patent: October 13, 1987Assignee: Societe de Conseils de Recherches et d'Applications ScientifiquesInventors: Michel Follet, Marc Bonato
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Patent number: 4677115Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.Type: GrantFiled: May 14, 1986Date of Patent: June 30, 1987Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Marcia E. Christy, Gerald S. Ponticello
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Patent number: 4672064Abstract: Novel 1,5-benzoxathiepin derivatives of the formula: ##STR1## [wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl or optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom; X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated; Y is ##STR2## (wherein R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl); m is an integer of 0 to 2; n is an integer of 1 to 6] and salts thereof exhibit serotonin S.sub.Type: GrantFiled: December 10, 1985Date of Patent: June 9, 1987Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Minoru Hirata
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Patent number: 4668695Abstract: Novel aminoalkylthiodibenzothiepins and related compounds, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as antidepressant, analgetic, and anticonvulsant agents.Type: GrantFiled: October 28, 1983Date of Patent: May 26, 1987Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
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Patent number: 4645758Abstract: The invention concerns:Novel dibenz/b,e/oxepin and dibenz/b,e/thiepin compounds having the general formula: ##STR1## wherein X is O or S,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are each selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulponyl, halogen, trifluoromethyl, trifluoromethylthio, lower dialkylsulphonamido, nitro, hydroxy, cyano, carbamyl, carboxy, lower alkoxycarbonyl, amino, N-lower alkylamino, N,N-diloweralkylamino, lower acylamido, lower alkanesulfonamido and lower acyl and, when on adjacent carbon atoms at the positions 2 and 3 and/or 8 and 9, two of the substituents R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4 taken together may form a methylenedioxy group;R.sup.5 and R.sup.Type: GrantFiled: January 17, 1986Date of Patent: February 24, 1987Inventors: Nils-Erik Willman, Bengt C. H. Sjogren, Lennart G. Nordh, Gustav L. Persson, Goran H. Sjoholm
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Patent number: 4640930Abstract: A compound of the formula ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 lower alkoxy groups, or 1 to 3 halogens; R.sub.2 is hydroxy or lower alkanoyloxy; R.sub.3 and R.sub.4 are each independently lower alkyl or together form a pyrrolidine or piperidine ring; and n is 2 to 4, and pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I are active as calcium channel blockers and accordingly, are useful as agents for lowering blood pressure, and as agents for treating ischemia.Type: GrantFiled: March 24, 1986Date of Patent: February 3, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Erno Mohacsi, Jay P. O'Brien
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Patent number: 4605665Abstract: Shock induced by splanchnic ischemia can be treated or prevented by the administration of an effective cyclooxygenase and lipoxygenase inhibiting amount of a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof to a mammal in need of the same.Type: GrantFiled: February 28, 1985Date of Patent: August 12, 1986Assignee: Ciba-Geigy CorporationInventors: Hui L. Liauw, Howard H. Oei, Edmond C. Ku
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Patent number: 4596822Abstract: Certain novel heterocyclic compounds, their preparation, and their use in inhibiting serine proteases with chymotrypsin-like, elastase-like, and trypsin-like specificity and in the treatment of diseases such as emphysema which involve tissue proteolysis.Type: GrantFiled: August 20, 1984Date of Patent: June 24, 1986Assignee: Georgia Tech Research CorporationInventors: James C. Powers, Wade Harper
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Anti-asthmatic 6H-dibenz-[b,e] [1,4]oxathiepin derivatives, compositions, and method of use therefor
Patent number: 4582842Abstract: Novel 6H-dibenz[b,e] [1,4]oxathiepin derivatives of the formula I and Ia are employed in the treatment and control of allergic conditions such as allergic asthma.Type: GrantFiled: September 26, 1983Date of Patent: April 15, 1986Assignees: Merck & Co., Inc., Merck Frosst CanadaInventors: Edward J. Cragoe, Jr., Clarence S. Rooney -
Patent number: 4582850Abstract: Psoriasis is treated by the topical or oral administration of an effective endogenous lipoxygenase inhibiting amount of a compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof to a patient in need of the same.Type: GrantFiled: February 28, 1985Date of Patent: April 15, 1986Assignee: Ciba-Geigy CorporationInventors: Hui-Lian Liauw, Howard H. Oei, Edmond C. Ku
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Patent number: 4571404Abstract: Substituted benzopentathiepins, their preparation from 1,2,3-benzothiadiazoles and elemental sulfur, selected 1,2,3-benzothiadiazoles; the benzopentathiepins being useful as biologically active compounds or as intermediates to 1,2-benzenedithiols.Type: GrantFiled: June 7, 1984Date of Patent: February 18, 1986Assignee: E. I. Du Pont de Nemours and CompanyInventor: Bertrand L. Chenard
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Patent number: 4536507Abstract: Prostaglandin antagonists are disclosed which are 7- and 8-substituted-dizenzo[b,f]thiepins of the structural formula: ##STR1##Type: GrantFiled: July 8, 1982Date of Patent: August 20, 1985Assignees: Merck & Co., Inc., Merck Frosst Canada, Inc.Inventors: Joshua Rokach, Clarence S. Rooney, Edward J. Cragoe, Jr.