Double Bonded Divalent Chalcogen Containing Patents (Class 544/130)
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Patent number: 5204480Abstract: There are described compounds of the formula ##STR1## where n is 1, 2 or 3;R.sub.1 is hydrogen, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl, loweralkyl, arylloweralkyl, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group ##STR3## taken as a whole is ##STR4## R.sub.2 is hydrogen, loweralkyl, loweralkenyl, arylloweralkyl, --CH.sub.2 C.tbd.CH, ##STR5## R.sub.7 and R.sub.8 being independently loweralkyl or alternatively the group ##STR6## taken as a whole is ##STR7## R.sub.3 is hydrogen is loweralkyl; and R.sub.4 is hydrogen or loweralkyl;which compounds are useful as analgesic agents and also for treating various memory dysfunctions.Type: GrantFiled: February 21, 1992Date of Patent: April 20, 1993Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, David M. Fink
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Patent number: 5194608Abstract: A dipeptide derivative of formula (I) is provided, which is capable of inhibiting the enzymatic activity of renin and thereby depressing the renin-angiotensin system and lowering the blood pressure. ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, aryl, or heterocyclic radical;R.sup.2 is carbamoyl, aryl, 5- or 6-membered heterocyclic radical, C.sub.1 -C.sub.12 alkyl-S--, C.sub.1 -C.sub.12 alkyl-S--CH.sub.2 --, or C.sub.3 -C.sub.10 cycloalkyl-S--;R.sup.3 is aryl or 5- or 6-membered heterocyclic radical;R.sup.4 is R.sup.4' --SO.sub.2 or R.sup.4' --CO;R.sup.4' is aryl, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl; C.sub.3 -C.sub.10 cycloalkyl, or heterocyclic radical;X is CH.sub.2, NH, O, or S; andY is CO or NHSO.sub.2, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4' each may be substituted with one to three substituents.Type: GrantFiled: June 24, 1991Date of Patent: March 16, 1993Assignee: Shionogi & Co., Ltd.Inventors: Tatsuo Toyoda, Toshihiro Fujioka, Kunio Hayashi, Masuhisa Nakamura, Naofumi Hashimoto
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Patent number: 5180418Abstract: Cycloalkanecarboxylic acid derivatives of formula I ##STR1## wherein W is ##STR2## and A is CO--R.sub.3 or CN; R.sub.1 is hydrogen or fluorine; R.sub.2 is halogen or cyano; R.sub.3 is chlorine, X--R.sub.5, amino, C.sub.1 -C.sub.4 alkylamino, d-C.sub.1 -C.sub.4 alkylamino, C.sub.2 -C.sub.4 haloalkylamino, di-C.sub.2 -C.sub.4 haloalkylamino, C.sub.1 -C.sub.4 hydroxyalkylamino, di-C.sub.1 -C.sub.4 hydroxyalkylamino, C.sub.3 -C.sub.4 alkenylamino, diallylamino, --N-pyrrolidino, --N-piperidino, --N-morpholino, --N-thiomorpholino, --N-piperidazino, the group --O--N.dbd.C--(R.sub.9)R.sub.10 or the group --N--R.sub.6 (OR.sub.6); each of R.sub.4 and R.sub.14, independently of the other, is hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or trifluoromethyl; R.sub.5 is hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.10 alkylthio-C.sub.1 -C.sub.4 alkyl, di-C.sub.1 -C.sub.4 alkylamino-C.sub.1 -C.sub.4 alkyl, cyano-C.sub.1 -C.sub.Type: GrantFiled: July 19, 1991Date of Patent: January 19, 1993Assignee: Ciba-Geigy CorporationInventors: Georg Pissiotas, Hans Moser, Hans-Georg Brunner, Eginhard Steiner
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Patent number: 5137886Abstract: The invention provides insecticidally active compounds of formula (I): ##STR1## wherein X is nitrogen or carbon bearing a hydrogen atom; R.sup.1 is a group of formula --S(O).sub.n --Y, wherein Y is an optionally substituted heterocyclic ring containing at least one nitrogen atom, the point of attachment of the group Y being at a ring nitrogen atom, and n is 0, 1 or 2; R.sup.2 is a group of formula --OSO.sub.2 R.sup.3 wherein R.sup.3 is selected from C.sub.1-8 alkyl, C.sub.1-4 alkyl substituted by an optionally substituted phenyl or heterocyclic ring, C.sub.1-8 haloalkyl, C.sub.2-6 alkenyl, C.sub.2-4 alkenyl substituted by an optionally substituted phenyl or heterocyclic ring, C.sub.2-4 alkynyl, C.sub.2-4 alkynyl substituted by an optionally substituted phenyl or heterocyclic ring, optionally substituted aryl, and a group of formula --N(R.sup.4)(R.sup.5) wherein R.sup.4 and R.sup.5 are independently selected from hydrogen and C.sub.1-6 alkyl or wherein R.sup.4 and R.sup.5 together represent --(CH.sub.2).sub.Type: GrantFiled: December 6, 1990Date of Patent: August 11, 1992Assignee: Imperial Chemical Industries PLCInventors: Robin A. E. Carr, Donn W. Moseley, Nan C. Sillars
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Patent number: 5110585Abstract: The invention relates primarily to quaternized polycyclic compounds having the formula ##STR1## wherein m is an integer having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; R.sub.2 together with the quaternary nitrogen, forms a 5 to 14 membered heterocyclic ring, said ring containing at least 2 hetero atoms selected from the group of nitrogen, sulfur and oxygen; R.sub.1 forms a double bond in the heterocyclic ring of the quaternized nitrogen or is alkyl, alkyleneoxyalkyl, alkylhydroxy, aryl, aralkyl, aralkenyl, alkaryl, alkylamidoalkyl and X.sup.- is an anion. The invention also relates to the preparation and use of said quaternized polycyclic compounds.Type: GrantFiled: March 1, 1989Date of Patent: May 5, 1992Assignee: ISP Investments Inc.Inventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login, Michael W. Helioff
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Patent number: 5093336Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: July 6, 1989Date of Patent: March 3, 1992Assignee: Hoechat-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Bettina Spahl
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Patent number: 5091405Abstract: Pyrazolines and their intermediates, including all geometric and stereoisomers of the pyrazolines and intermediates, agricultural compositions containing the pyrazolines, and methods for use as insecticides.Type: GrantFiled: May 12, 1989Date of Patent: February 25, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thomas M. Stevenson
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Patent number: 5089507Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups, or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom,R.sub.3 is hydrogen, C.sub.1-6 alkyl or phenyl, or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;R.sub.4 and R.sub.5 are independently hydrogen, hydroxyl, halogen, C.sub.1-6 alkyl or aryl, provided both R.sub.4 and R.sub.5 are not simultaneously hydrogen; and p is an integer from 1 to 4,is useful for the treatment of pain or hyponatraemic disease states.Type: GrantFiled: September 25, 1989Date of Patent: February 18, 1992Assignee: Dr. L. Zambeletti SpAInventors: Vittorio Vecchietti, Roberto Colle, Antonio Giordani, Giulio Dondio
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Patent number: 5081246Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: December 20, 1989Date of Patent: January 14, 1992Assignees: Hiroyoshi Hidaka, Tobishi Yakuhin Kogyo Kabushiki KaishaInventors: Horoyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
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Patent number: 5077402Abstract: Compounds of the formula I, II, III and IIIa ##STR1## in which Ar.sup.1 is an unsubstituted or substituted aromatic radical and at least one of the radicals R.sup.1 and R.sup.2 is an alkenyl, cycloalkenyl or arylmethyl group, are effective photoinitiators for photopolymerization of unsaturated compounds. They are particularly suitable for photocuring of pigmented systems.Type: GrantFiled: March 28, 1990Date of Patent: December 31, 1991Assignee: Ciba-Geigy CorporationInventors: Vincent Desobry, Kurt Dietliker, Rinaldo Husler, Werner Rutsch, Manfred Rembold, Franciszek Sitek
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Patent number: 5075452Abstract: Compounds of the formula I ##STR1## in which A and X.sup.1 have the meaning given in patent claim 1 can be prepared in a simple manner, in a one-pot process and in high yields.Type: GrantFiled: December 6, 1989Date of Patent: December 24, 1991Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Richard Kirchlechner, Michael Casutt, Arno Basedow
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Patent number: 5053504Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.Type: GrantFiled: November 29, 1989Date of Patent: October 1, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Wen-Sen Li, John K. Thottathil, Michael Murphy
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Patent number: 5047406Abstract: Substituted cyclohexanols and cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.Type: GrantFiled: May 2, 1990Date of Patent: September 10, 1991Assignee: Warner-Lambert Co.Inventors: Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
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Patent number: 5043443Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.Type: GrantFiled: July 24, 1990Date of Patent: August 27, 1991Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Randall K. Carlson, Chung-Ho Park, Walter A. Gregory
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Patent number: 5041454Abstract: Substituted N-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides, their N-oxide forms, their pharmaceutically acceptable acid addition salts and stereochemically isomeric forms having gastrointestinal motility stimulating properties, compositions containing the same, and methods of treating warm-blooded animals suffering from motility disorders of the gastrointestinal system.Type: GrantFiled: April 19, 1990Date of Patent: August 20, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Michel A. J. De Cleyn
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Patent number: 5037822Abstract: The invention relates to the products of formula ##STR1## in which R represents the radical ##STR2## in which R.sub.1 at any position on the benzene ring represents a linear, branched or cyclic alkyl, alkenyl or alkynyl containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, which may be identical or different, represent a hydrogen atom or a linear alkyl, alkenyl or alkynyl containing up to 8 carbon atoms or form, together with the nitrogen atom to which they are attached, a carbonaceous heterocyclic radical optionally containing another hetero form, or the radical OR', R' representing hydrogen, a linear, branched or cyclic alkyl radical containing up to 8 carbon atoms or an aryl radical containing up to 14 carbon atoms, or the radical SR.sub.4 or S(O)R.sub.5, R.sub.4 and R.sub.5 representing a linear, branched or cyclic alkyl, alkenyl or alkynyl containing up to 8 carbon atoms, or R represents naphthyl optionally substituted with a radical R'.sub.1, R'.sub.Type: GrantFiled: February 21, 1990Date of Patent: August 6, 1991Assignee: Roussel-UclafInventors: Emilio Toja, Fernando Barzaghi, Giulio Galliani
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Patent number: 5030729Abstract: Compounds of formula (I) ##STR1## in which R.sub.1 is hydrogen, O.degree., CN, NO, cyanomethyl, C.sub.1 -C.sub.12 -alkyl, C.sub.3 -C.sub.12 -alkenyl or C.sub.3 -C.sub.12 -alkynyl subject to the proviso that the carbon atom attached to the nitrogen atom is a primary carbon atom, C.sub.7 -C.sub.12 -aralkyl, C.sub.1 -C.sub.12 -acyl, 2,3-epoxypropyl, OH-monosubstituted C.sub.2 -C.sub.6 -alkyl or 2,3-dihydroxypropyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.18 -alkyl, C.sub.5 -C.sub.18 -cycloalkyl, C.sub.6 -C.sub.18 -aryl or C.sub.7 -C.sub.18 -aryalkyl, R.sub.3 is C.sub.6 -C.sub.18 -aryl or a group of the formula (II) ##STR2## in which R.sub.1 is as defined above, n is an integer from 1 to 4 and R.sub.4 is an organic or inorganic radical of a valency equal to n are useful for stabilizing organic material against oxidative, thermal and/or light induced degradation.Type: GrantFiled: March 1, 1990Date of Patent: July 9, 1991Assignee: Ciba-Geigy CorporationInventors: Giuseppe Cantatore, Valerio Borzatta
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Patent number: 5021420Abstract: This invention relates to a compound ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or an alkyl, hydroxy or alkoxy radical, (c) a 3-indolyl radical, (d) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (e) a 3-(5-hydroxyindolyl) radical.a 1-piperazinyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by an alkoxy, alkyl, hydroxy, nitro or amino radical or a halogen atom, (c) a 1,2-benzisothiazol-3-yl radical, (d) a 1,2-benzisoxazol-3-yl radical or (e) a 2-pyridyl radical.Type: GrantFiled: July 6, 1989Date of Patent: June 4, 1991Assignee: Rhone-Poulenc SanteInventors: Marie-Iherese Comte, Claude Gueremy, Jean-Luc Malleron, Serge Mignani, Jean-Francois Peyronel, Alain Truchon
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Patent number: 5017214Abstract: Tetrazole-substituted benzenesulfonamides are useful as agricultural chemicals and, in particular, as growth regulants and herbicides.Type: GrantFiled: November 15, 1989Date of Patent: May 21, 1991Inventor: George Levitt
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Patent number: 5013732Abstract: 3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalkyl- or haloalkyl-1H-indole with an amine.Type: GrantFiled: July 30, 1990Date of Patent: May 7, 1991Assignee: Sterling Drug Inc.Inventor: Malcolm R. Bell
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Patent number: 5006527Abstract: Novel N-(4-piperindyl)bicyclic condensed 2-imidazolamine derivatives and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.Type: GrantFiled: December 4, 1989Date of Patent: April 9, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Frans E. Janssens, Joseph L. G. Torremans, Gasto S. M. Diels
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Patent number: 5004813Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.Type: GrantFiled: August 24, 1989Date of Patent: April 2, 1991Assignee: Ciba-Geigy CorporationInventors: Rox Phaff, Davor Bedekovic
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Patent number: 5001137Abstract: A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.Type: GrantFiled: September 14, 1989Date of Patent: March 19, 1991Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
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Patent number: 4996318Abstract: The amino-9,10-secosteroids ##STR1## of the present invention contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain and are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc.Type: GrantFiled: September 19, 1989Date of Patent: February 26, 1991Assignee: The Upjohn CompanyInventors: Martin Gall, Robert I. Higuchi
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Patent number: 4994450Abstract: A compound, or a solvate or salt thereof, of formula (I) ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups, or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom, provided that R.sub.1 and R.sub.2 are not simultaneously hydrogen;R.sub.3 is hydrogen, C.sub.1-6 alkyl, preferably methyl or ethyl, or phenyl, or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;p is 1, 2, 3 or 4, andR is a group of formula (II) ##STR2## in which the group --(CHR.sub.4).sub.n --X-- is in the meta- or para-position with respect to YR.sub.5 or R.sub.6, R.sub.4 is hydrogen or C.sub.1-6 alkyl, preferably hydrogen;n is 0, 1 or 2, preferably 1;X is a direct bond, or O, S or NR.sub.a in which R.sub.a is hydrogen or C.sub.1-6 alkyl, and is preferably a direct bond;Y is >C.dbd.O, >CHOH, --S.dbd.O or --SO.Type: GrantFiled: February 10, 1989Date of Patent: February 19, 1991Assignee: Dr. Lo. Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Antonio Giordani
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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: 4980349Abstract: The invention relates to new compounds corresponding to formula I: ##STR1## in which: W represents C=O, CH.sub.2 or CHOH,Z represents ##STR2## R.sub.1 and R.sub.2 represent especially Cl or F, R, R' and R" represent especially H,X represents especially CH.sub.2,Y represents especially COOH,u and v are two integers ranging from 0 to 10,p and q take the value 0 or 1,n and m are two integers ranging 0 to 10 andt is 0 or 1the total number of carbon atoms in the chain ##STR3## ranging from 2 to 20, and to their physiologically acceptable salts obtained with organic or inorganic acids.These compounds are useful for preparing medicinal products which have, especially, anti-inflammatory properties.Type: GrantFiled: November 12, 1987Date of Patent: December 25, 1990Assignee: SANOFIInventors: Pierre Roger, Jean-Paul Fournier, Alain Martin, Jean Choay
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Patent number: 4980355Abstract: Novel substituted isonicotinic acid amides of the general formula ##STR1## in which X in ortho/ortho'-position are equal and represent fluorine, chlorine, bromine or iodine;Q.sub.1 is unsubstituted pyridimin-4-yl, or pyrimidin-4-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.2 is unsubstituted pyrimidin-2-yl, or pyrimidin-2-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.3 is unsubstituted pyrimidin-5-yl, or pyrimidin-5-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.4 is pyridin-2-yl, pyridin-3-yl or pyridin-4-yl each of which is unsubstituted or substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.5 is pyridazin-3-yl or pyridazin-4-yl each of which is unsubstituted or substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.6 is unsubstituted pyrazin-2-yl, or pyrazin-2-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;R.sub.1, R.sub.2, R.sub.3 are hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl having from 1 to 3 halogen atoms, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.Type: GrantFiled: March 3, 1989Date of Patent: December 25, 1990Assignee: Ciba-Geigy CorporationInventors: Helmut Zondler, Alfred Meyer, Wolfgang Eckhardt, Walter Kunz
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Patent number: 4978663Abstract: There are described compounds of the formula ##STR1## where n is 1,2 or 3;R.sub.1 is hydrogen, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl, loweralkyl, arylloweralkyl, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group ##STR3## taken as a whole is ##STR4## R.sub.2 is hydrogen, loweralkyl, loweralkenyl, arylloweralkyl, --CH.sub.2 C.tbd.CH, R.sub.7 and R.sub.8 being independently loweralkyl or alternatively the group ##STR5## taken as a whole is ##STR6## R.sub.3 is hydrogen or loweralkyl; and R.sub.4 is hydrogen or loweralkyl;which compounds are useful as analgesic agents and also for treating various memory dysfunctions.Type: GrantFiled: August 16, 1989Date of Patent: December 18, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, David M. Fink
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Patent number: 4976889Abstract: 4-Formylaminopiperidine derivatives of the formula (I) ##STR1## where n is 1 or 2, R.sup.1 to R.sup.4 are each alkyl or R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4 are tetra- or pentamethylene, R.sup.5 is hydrogen or alkyl, R.sup.6 is hydrogen, unsubstituted or substituted alkyl, alkenyl, aralkyl or acyl, and, when n is 1, Y is hydrogen, unsubstituted or substituted alkyl, alkenyl, cycloalkyl, bicycloalkyl, aralkyl, aryl, alkyl containing heterocyclic radicals, or ##STR2## or, when n is 2, Y is alkylene, cycloalkylene, aralkylene or arylene or is alkylene which is interrupted by oxygen, nitrogen, sulfur or a 5-membered or 6-membered heterocyclic structure, and their acid addition salts have very good stabilizing properties in plastics.Type: GrantFiled: November 14, 1988Date of Patent: December 11, 1990Assignee: BASF AktiengesellschaftInventors: Alexander Aumueller, Peter Neumann, Hubert Trauth
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Patent number: 4975439Abstract: Substituted N-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides, their N-oxide forms, their pharmaceutically acceptable acid addition salts and stereochemically isomeric forms having gastrointestinal motility stimulating properties, compositions containing the same, and methods of treating warm-blooded animals suffering from motility disorders of the gastrointestinal system.Type: GrantFiled: September 2, 1988Date of Patent: December 4, 1990Assignee: Janssen Pharmaceutical N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Michel A. J. De Cleyn
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Patent number: 4968714Abstract: Fungicidal substituted 3-amino-2-pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 represents unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl or alkinyl, or unsubstituted or substituted cycloalkyl or cycloalkenyl,R.sup.2 represents hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl or alkinyl, unsubstituted or substituted cycloalky or cycloalkenyl, unsubstituted or substituted aryl or unsubstituted or substituted heterocyclyl, or represents one of the radicals --CX--YR.sup.3, --CXNR.sup.4 R.sup.5, ##STR2## --SO.sub.2 NR.sup.4 R.sup.5 or --SO.sub.2 R.sup.7, R.sup.3 represents unsubstituted or substituted alkyl or unsubstituted or substituted alkenyl or alkinyl,R.sup.4 and R.sup.Type: GrantFiled: February 16, 1990Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Winfried Lunkenheimer, Gerd Hanssler
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Patent number: 4968341Abstract: Novel substituted aryloxyureas, processes for their production, and herbicides comprising them as active ingredients are provided.The substituted aryloxyureas exhibit an excellent herbicidal efficacy against weeds when applied, for example, to the weeds in a wide range of period from a preemergence stage to a growth stage.The substituted aryloxyureas of the invention have the excellent advantage of maintaining high safety on crops or crop plants in spite of their herbicidal efficacy.Type: GrantFiled: August 16, 1988Date of Patent: November 6, 1990Assignees: Kumiai Chemical Industry Co., Mitsui Petrochemical Industries, Ltd.Inventors: Isao Hashimoto, Tatsuyodihi Ishida, Kazutaka Tsuru, Yuji Yamada, Takeshige Miyazawa, Yasuo Nakamura, Susumu Katou, Katsuya Takahashi
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Patent number: 4960784Abstract: Certain substituted indazoles, including all geometric and stereoisomers thereof, agricultural compositions containing the indazoles and use of the indazoles as insecticides.Type: GrantFiled: October 2, 1989Date of Patent: October 2, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventor: George P. Lahm
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Patent number: 4958021Abstract: Benzopyran derivatives of the formula ##STR1## where X is the radical ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and also the ring A have defined meanings are used in pressure- or heat-sensitive layers.Type: GrantFiled: July 19, 1988Date of Patent: September 18, 1990Assignee: BASF AktiengesellschaftInventors: Andreas Guentner, Udo Mayer, Andreas Oberlinner
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N-substituted derivatives of 1-desoxynojirimycin and 1-desoxymannonojirimycin and pharmaceutical use
Patent number: 4940705Abstract: N-substituted derivatives of 1-desoxynojirimycin and 1-desoxymannojirimycin of the formula ##STR1## in which one of R and R' are hydroxyl and the other is hydrogenn is a number from 1 to 6R.sup.1 is hydrogen, alkyl or benzyl andR.sup.2 is alkyl which is optionally substituted by an optionally substituted aryl or by pyridyl, thienyl, furyl, pyrimidyl, pyrazinyl or quinolyl or R.sub.1 is cycloalkyl or R.sup.2 is optionally substituted by aryl or R.sup.2 is a saturated bridged heterocycle or R.sup.1 and R.sup.2 together can form a heterocyclic ring which is optionally substituted. These compounds are useful in the treatment of and prophylaxis of viral infections.Type: GrantFiled: October 26, 1988Date of Patent: July 10, 1990Assignee: Bayer AktiengesellschaftInventors: Horst Boshagen, Bodo Junge, Arnold Paessens, Matthias Schuller -
Patent number: 4937242Abstract: 1,4-Dihydropyridine derivatives of the general formula: ##STR1## wherein X.sup.1 and X.sup.2 independently represent hydrogen, fluoromethyl, fluoromethoxy, halogen, cyano, or nitro; R.sup.1 represents a lower alkyl; R.sup.2 represents acyl, alkoxycarbonyl, acylalkyl, an N-alkyl-substituted carbamoylalkyl, alkoxyalkyl, alkoxycarbonylalkyl, acyloxyalkyl, nitratoalkyl, cyanoalkyl, heterocycle-alkyl, haloalkyl, alkenyl, or alkynyl; A represents an alkylene comprising a carbon atom to which 2 alkyls are bonded and having in total at least 5 carbon atoms; m represents the integer 1, 2 or 3; acid addition salts thereof; a method of production thereof; and pharmaceutical compositions containing such compound(s).Such compounds have pharmacological activities, in particular potent and long lasting hypotensive activity, coronary vasodilatation, cerebral vasodilatation, peripheral vasodilatation, renal vasodilatation and platelet aggregation inhibitory activity.Type: GrantFiled: March 8, 1988Date of Patent: June 26, 1990Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Hiroshi Matsui, Fumio Fukata, Takayoshi Mori, Nobuharu Kakeya, Kazuhiko Kitao
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Patent number: 4933338Abstract: Benzimidazole-2-sulfonamide and imidazopyridine-2-sulfonamide derivatives corresponding to the general formula I: ##STR1## and their pharmaceutically acceptable salts, especially those of the formula in which:Z.sup.1 to Z.sup.4 represent a nitrogen atom or a substituted or unsubstituted carbon atom;R.sup.1 and R.sup.2 represent a hydrogen atom or an alkyl, alkylaryl, alkylcarbonylalkyl, alkylcarbonylaryl, alkylcarbonylheteroaryl, cycloalkyl, carboxyalkyl, acyl or nitro radical, or alternativelyR.sup.1 and R.sup.2 can together form a linkage represented by a group X;R.sup.Type: GrantFiled: April 15, 1987Date of Patent: June 12, 1990Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Jordi F. Constansa, Juan P. Corominas, Agusto C. Pinol
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Patent number: 4914227Abstract: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.Type: GrantFiled: May 16, 1986Date of Patent: April 3, 1990Assignee: Banyu Pharmaceutical Company, Ltd.Inventors: Tetsuji Miyano, Kunio Suzuki, Ryosuke Ushijima, Susumu Nakagawa
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Patent number: 4910200Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## B is ##STR3## R.sup.1 is hydrogen; halogen, cyano or optionally substituted C.sub.1-4 alkyl; andQ is NR.sup.8 R.sup.9 or ##STR4## where R.sup.2 to R.sup.11 are substituents of various types. The compounds are useful as fungicides.Type: GrantFiled: October 9, 1986Date of Patent: March 20, 1990Assignee: Celamerck GmbH & Co. KGInventors: Jurgen Curtze, Helmut Pieper, Josef Nickl, Heinz-Manfred Becher, Guido Albert, Christo Drandarevski, Sigmund Lust, Ludwig Schroder
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Patent number: 4898977Abstract: The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, and R.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonisation of the resulting .gamma.,.delta.-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group. Compounds of the formula I are starting materials for the preparation of renin-inhibitors which have an anti-hypertensive action.Type: GrantFiled: August 13, 1987Date of Patent: February 6, 1990Assignee: Ciba-Geigy CorporationInventors: Peter Herold, Christof Angst
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Patent number: 4876357Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.Type: GrantFiled: October 26, 1987Date of Patent: October 24, 1989Assignee: Ciba-Geigy CorporationInventors: Rox Phaff, Davor Bedekovic
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Patent number: 4876262Abstract: A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: ##STR1## in which R1 is a lower alkyl or a tolyl, R2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is --CO--, --CH2-- or --CHOH--, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, --CH2COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, ##STR2## 1 being 1 or 2, --A--B, A being --(CH2)n--, n being an integer of 1 to 5, a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkane having lower alkyl, phenyl or hydroxyl group(s) bonded directly to one or more carbon atoms constituting said alkane by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof,a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalentType: GrantFiled: February 18, 1987Date of Patent: October 24, 1989Assignee: Eisai Co., Ltd.Inventors: Hitoshi Oinuma, Motosuke Yamanaka, Kazutoshi Miyake, Tomonori Hoshiko, Norio Minami, Tadao Shoji, Yoshiharu Daiku, Kohei Sawada, Kenichi Nomoto
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Patent number: 4874756Abstract: The present invention provides compounds of the general formula ##STR1## wherein the variables are as defined herein. The present invention also provides processes for the preparation thereof, pharmaceutical compositions containing them and intermediates for the preparation thereof.Type: GrantFiled: August 29, 1986Date of Patent: October 17, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Wolfgang von der Saal, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
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Patent number: 4874759Abstract: Hydroxyindole-3-carboxylic acid amide compounds of the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, the same or different, respectively a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or a heteroaryl group, or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4 are respectively groups which are combined to each other taken together with the adjacent nitrogen atom to form a heterocyclic group, R.sup.5 is an alkyl group, R.sup.6 is a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group or an aralkyl group and X is a hydrogen atom, a halogen atom or a lower alkanoyl group, or their acid addition salts.These compounds are of use as diuretics or a therapeutic medicine for circulation system diseases.Type: GrantFiled: September 23, 1988Date of Patent: October 17, 1989Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tetsuya Tahara, Tsuguo Ikebe, Ichiro Hakamada, Osamu Yaoka
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Patent number: 4873253Abstract: A phenylalanine derivative having the formula (I): ##STR1## wherein A represents ##STR2## B represents ##STR3## wherein m is 0, 1, or 2 and n is 3, 4, or 5; X represents (a) hydroxy, (b) nitro, (c) amino, (d) phenoxy which may be substituted with (i) halogen or (ii) nitro, (e) c.sub.1 -C.sub.4 alkyloxy which may be substituted wit (i) phenyl or (ii) benzoyl, (f) benzoyl, (g) pyridyloxy which may be substituted with (i) halogen or (ii) nitro, or (h) c.sub.1 -C.sub.4 alkyl which may by substituted with halogen;Y represents ##STR4## or --OR.sup.3 wherein R.sup.1 R.sup.2 are independently (a) hydrogen, (b) phenyl which may be substituted with (i) benzoyl, (ii) C.sub.1 -C.sub.4 alkylcarbonyl, (iii) C.sub.1 -C.sub.4 alkyl which may be further substituted with C.sub.1 -C.sub.4 alkoxycarbonyl or hydroxycarbonyl, (iv) C.sub.2 -C.sub.5 alkenyl which may be further substituted with hydroxycarbonyl or C.sub.1 -C.sub.4 alkoxycarbonyl, (v) C.sub.1 -C.sub.Type: GrantFiled: March 30, 1987Date of Patent: October 10, 1989Assignees: Shosuke Okamoto, Showa Denko Kabushiki KaishaInventors: Shosuke Okamoto, Yoshio Okada, Akiko Okunomiya, Taketoshi Naito, Yoshio Kimura, Morihiko Yamada, Norio Ohno, Yasuhiro Katsuura, Hiroshi Nojima, Takashi Shishikura
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Patent number: 4861777Abstract: A novel pyrazole derivative and an insecticidal or miticidal composition containing the derivative as the effective ingredient are disclosed.The pyrazole derivative of the present invention has an excellent controlling effect also against harmful insects and mites exhibiting resistance to conventional insecticides and does not disturb the ecosystem since it is less toxic and less residual.Type: GrantFiled: September 7, 1988Date of Patent: August 29, 1989Assignee: Mitsubishi Kasei CorporationInventors: Itaru Okada, Shuko Okui, Mana Nishimata, Yoji Takahashi, Toshiki Fukuchi
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Patent number: 4837350Abstract: Benzoin esters of aromatic sulfonic acids can be obtained in high yield from benzoin and the respective sulfonyl halide in molar amounts of a base by carrying out the reaction at low temperature in an organic solvent with the addition of water. Aqueous NaOh or KOH can be used as base in this process.Type: GrantFiled: December 7, 1987Date of Patent: June 6, 1989Assignee: Ciba-Geigy CorporationInventors: Werner Rutsch, Rinaldo Husler
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Patent number: 4824853Abstract: Antidiarrheal active .alpha.,.alpha.-diaryl-4-aryl-4-hydroxy-1-piperidinebutanamide, N-oxides, compositions containing the same and methods of treating diarrhea.Type: GrantFiled: July 23, 1986Date of Patent: April 25, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Lourens Wals, Ludwig P. Cooymans
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Patent number: RE33125Type: GrantFiled: July 11, 1986Date of Patent: December 5, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Henry F. Campbell, Thomas H. Scholtz, George H. Douglas