Additional Hetero Ring Containing Patents (Class 544/55)
-
Patent number: 5488037Abstract: This invention relates to L-Arginine aldehyde derivatives, pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.Type: GrantFiled: March 4, 1994Date of Patent: January 30, 1996Assignee: Eli Lilly and CompanyInventors: Daniel J. Sall, Robert T. Shuman
-
Patent number: 5484921Abstract: This invention relates to a method for the preparation of benzo[b]naphthyridines having the general formula (I) ##STR1## comprising: 1) condensation of an amine having the formula R'--NH--CH.sub.2 --CH.sub.2 --R" with a chlorofluoroquinoline of formula (II) ##STR2## 2) cyclization of the obtained fluoroquinoline of formula (IV) ##STR3## and; 3) oxidation of tetrahydro-1,2,3,4benzo[b]naphthyridine-1,8 of formula (V) ##STR4## is effected, and then, optionally, the ester obtained is transformed into an acid and optionally into a salt.Type: GrantFiled: April 8, 1994Date of Patent: January 16, 1996Assignee: Laboratoire Roger BellonInventors: Christophe Daubie, Jean-Jacques Legrand, Clive Pemberton
-
Patent number: 5478934Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.Type: GrantFiled: November 23, 1994Date of Patent: December 26, 1995Inventors: Jun Yuan, Jan W. F. Wasley
-
Patent number: 5466708Abstract: 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: September 19, 1994Date of Patent: November 14, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Romano Derungs, Hans P. Marki, Henri Stalder, Andre Szente
-
Patent number: 5458814Abstract: Described are novel reversible photochromic naphthopyran compounds, examples of which are compounds having certain substituents at the number 5 and 6 carbon atoms of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: December 9, 1993Date of Patent: October 17, 1995Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, Barry Van Gemert, David B. Knowles
-
Patent number: 5428032Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.Type: GrantFiled: December 20, 1993Date of Patent: June 27, 1995Assignee: Nihon Bayer Agrochem K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
-
Patent number: 5420125Abstract: Nitromethylene compounds of general formula ##STR1## wherein R represents a hydrogen atom or an alkyl group, R.sup.1 represents a hydrogen atom or an alkyl group, n is 0 or 1, and Het represents an optionally substituted 3-pyridyl, 4-pyridyl or 5-isoxazolyl group, processes for their preparation, and their use as insecticides, are described.Type: GrantFiled: March 24, 1994Date of Patent: May 30, 1995Assignee: Shell Research LimitedInventors: David Munro, Bipin Patel
-
Patent number: 5378839Abstract: There are provided 1-(substituted)thioalkylpyrrole compounds of formula I ##STR1## the use thereof for the control of insect, acarid and mollusk pests and methods and compositions for the protection of crops from the ravages of said pests.Type: GrantFiled: January 26, 1994Date of Patent: January 3, 1995Assignee: American Cyanamid CompanyInventors: David G. Kuhn, Venkataraman Kameswaran
-
Patent number: 5328916Abstract: New heterocyclic compounds of the formulaX--W--CR.sup.1 R.sup.2 --CO--Y--NR.sup.3 --CHR.sup.4 --CR.sup.5 --CH.sub.2 --(CR.sup.6 R.sup.7).sub.r --Z--Het Iin which R.sup.1 to R.sup.7, W, X, Y, Z, r and Het have the meanings defined herein, and the salts thereof, inhibit the activity of human plasma renin.Type: GrantFiled: May 2, 1991Date of Patent: July 12, 1994Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Peter Raddatz, Claus J. Schmitges, Klaus-Otto Minck
-
Patent number: 5322847Abstract: A series of imidazo[4,5-c]pyridines which inhibit platelet activating factor (PAF) and also block leukotriene D4 receptors are useful in treating asthma, arthritis, psoriasis, gastrointestinal distress, myocardial infarction, stroke and shock.Type: GrantFiled: November 5, 1992Date of Patent: June 21, 1994Assignee: Pfizer Inc.Inventors: Anthony Marfat, James F. Eggler, Michael J. Fray, Kelvin Cooper
-
Patent number: 5276037Abstract: The invention concerns an aryl derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a heterocyclic moiety, and X.sup.1 is oxy, thio, sulphinyl, sulphonyl, difluoromethylene, imino, (1-4C)alkylimino or optionally substituted (1-4C)alkylene, or X.sup.1 is a group of the formula--X.sup.4 --CR.sub.2 -- or --CR.sub.2 --X.sup.4 --whereinX.sup.4 is oxy, thio, sulphinyl, sulphonyl or carbonyl and each R is hydrogen, methyl or ethyl;each of Ar.sup.2 and Ar.sup.3 is optionally substituted phenylene;X.sup.2 is oxy, thio, sulphinyl or sulphonyl;R.sup.1 is (1-4C)alkyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X.sup.3 --A.sup.2 -- which together with the carbon atom to which A.sup.1 and A.sup.2 are attached define a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X.sup.Type: GrantFiled: April 14, 1993Date of Patent: January 4, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Robert I. Dowell, Philip N. Edwards, Keith Oldham
-
Patent number: 5264440Abstract: Compounds having the formula (I): ##STR1## in which any two of K, L and M are nitrogen and the other is CE; X and Y are independently hydrogen, halogen, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, C.sub.2-4 alkynyloxy, phenyl, benzyloxy, cyano, isocyano, isothiocyanato, nitro, NR.sup.1 R.sup.2, NR.sup.1 OR.sup.2,N.sub.3, NHCOR.sup.1, NR.sup.1 CO.sub.2 R.sup.2, NHCONR.sup.1 R.sup.2, N.dbd.CHNR.sup.1 R.sup.2, NHSO.sub.2 R.sup.1, OR.sup.1, OCOR.sup.1, OSO.sub.2 R.sup.1, SR.sup.1, SOR.sup.1, SO.sub.2 R.sup.1, SO.sub.2 OR.sup.1, SO.sub.2 NR.sup.1 R.sup.2, COR.sup.1, CR.sup.1 .dbd.NOR.sup.2, CHR.sup.1 CO.sub.2 R.sup.2, CO.sub.2 R.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2, CH.sub.3 O.sub.2 C.C:CH.OCH.sub.Type: GrantFiled: July 20, 1992Date of Patent: November 23, 1993Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Ian T. Streeting, Rex Cheetham
-
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
-
Patent number: 5250521Abstract: Novel substituted pyrazolopyrimidines of formula (I) which are useful as angiotensin II antagonists, are disclosed.Type: GrantFiled: November 25, 1991Date of Patent: October 5, 1993Assignee: Merck & Co., Inc.Inventors: Eric E. Allen, William J. Greenlee, Prasun K. Chakravarty, Malcolm MacCoss, Arthur A. Patchett, Thomas F. Walsh
-
Patent number: 5239070Abstract: There are provided alkyl esters of 5-heterocyclic-pyridine-2,3-dicarboxylic acids useful as intermediates for the preparation of highly effective 5-heterocyclic-2-(2-imidazolin-2-yl)pyridine herbicidal agents and methods for the preparation thereof.Type: GrantFiled: June 11, 1991Date of Patent: August 24, 1993Assignee: American Cyanamid CompanyInventor: John M. Finn
-
Patent number: 5219824Abstract: Disclosed herein are herbicidal pyridine compounds substituted at the 3- and/or 5-position with a carboxylic acid-derived heterocyclic moiety, as well as herbicidal compositions and use of these compounds.Type: GrantFiled: October 21, 1991Date of Patent: June 15, 1993Assignee: Monsanto CompanyInventors: Yuen-Lung L. Sing, Len F. Lee
-
Patent number: 5212307Abstract: The invention describes light-sensitive bis-trichloromethyl-s-triazines of the general formula I ##STR1## wherein A denotes the ring members required to complete a 5- or 6-membered heterocyclic ring which may be substituted or may carry a substituted or unsubstituted fused benzene ring,R denotes a substituted or unsubstituted alkyl group andX denotes CH or N.The compounds are readily prepared in high yields. They are suitable for use as light-sensitive free-radical and acid donors in light-sensitive compositions.Type: GrantFiled: April 5, 1990Date of Patent: May 18, 1993Assignee: Hoechst AktiengesellschaftInventor: Wojciech A. Wilczak
-
Patent number: 5180717Abstract: Bivalent ligand compounds synthesized from a tether composition joining two heterocyclic groups comprising furochromones, furobenzoxazinones, and benzobisdifurans. These compounds show pharmacological activity in blocking ACAT enzymes which are major regulators of cholesterol metabolism. The compounds also show activity in lowering plasma triglycerides and elevating HDL cholesterol. They are useful in the prevention or treatment of the constriction or obstruction of arterial vessels, atherosclerosis, hyperlipidemia, hypertriglyceridemia, chylomicronemia, and pancreatitis.Type: GrantFiled: May 7, 1991Date of Patent: January 19, 1993Assignee: The Upjohn CompanyInventors: Ronald B. Gammill, Frank P. Bell
-
Patent number: 5179091Abstract: Compounds of general formula (I): in which: ##STR1## R.sub.1, X, Y, Z, T, R.sub.2, R.sub.3 and R.sub.4 are defined in the description. Medicinal products.Type: GrantFiled: June 3, 1991Date of Patent: January 12, 1993Assignee: Adir et CompagnieInventors: Daniel Lesieur, Daniel H. Caignard, Isabelle Lesieur, Michelle Devissaguet, Beatrice Guardiola
-
Patent number: 5162325Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.Type: GrantFiled: May 7, 1991Date of Patent: November 10, 1992Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Malcolm MacCoss, Nathan Mantlo, Thomas F. Walsh
-
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
-
Patent number: 5135563Abstract: The present invention relates to a pyrimidine derivative having the formula ##STR1## (wherein the variables are defined in the full text of the patent), a method for producing the same, and its use as a herbicide.Type: GrantFiled: July 5, 1991Date of Patent: August 4, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saitoh, Hideyuki Shibata
-
Patent number: 5136034Abstract: Thioacids, thiols, an acid, and an aldehyde are used to produce chiral thioacetals of the general formula. ##STR1## The compounds are leukotriene antagonists.Type: GrantFiled: October 5, 1990Date of Patent: August 4, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Michel Therien, Jacques-Yves Gauthier, Robert Zamboni, Michel L. Belley
-
Patent number: 5120843Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).Type: GrantFiled: October 23, 1989Date of Patent: June 9, 1992Assignee: UpjohnInventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
-
Patent number: 5096914Abstract: Benzopyran derivatives of the general formula I ##STR1## wherein the substituents are as defined herein are provided. The compounds show vasodilating and vascular spasmolytic activity and are useful in treating hypertension.Type: GrantFiled: November 30, 1990Date of Patent: March 17, 1992Assignee: Beiersdorf AktiengesellschaftInventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
-
Patent number: 5084459Abstract: There is provided a pest control composition containing a compound represented by the formula, ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and independently mean a hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted and X means an electron attracting group or a salt thereof.The compounds are of minimal toxicity to man, domestic animals and fish and selectively display remarkable control effect on pests.Type: GrantFiled: October 25, 1989Date of Patent: January 28, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideki Uneme, Isao Minamida, Tetsuo Okauchi, Noriko Higuchi
-
Patent number: 5071871Abstract: New benz[b]pyranes and pyranopyridines of formula I, ##STR1## wherein the significances of substituents V, T, W, R.sub.3 to R.sub.5, R.sub.9, R.sub.10, m, X, Y and Z are given in claim 1 and their N-oxides and their salts and their use in the treatment of raised blood pressure in the treatment of vascular disorders and other disorders in which a reduction in tension of the smooth muscles is therapeutically useful, as well as in the treatment of hair loss and baldness. Further the compounds are useful in the treatment of asthma and obstructive disorders of the respiratory system as well as in the prophylactic treatment of obstructive or inflammatory airways disease, for example asthma, as well as novel pharmaceutical compositions comprising said K.sup.+ channel activators suitable for such use.Type: GrantFiled: July 10, 1990Date of Patent: December 10, 1991Assignee: Sandoz Ltd.Inventors: Stefan Blarer, John Morley, Ian D. Chapman
-
Patent number: 5017586Abstract: Derivatives of 5-aminomethyl-2-furanomethanol represented by formula (I), or pharmaceutically acceptable salts thereof, which possess calcium-antagonistic activity and are effective in lowering blood pressure, and a process for preparing and using the same: ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.2 ' each represent a lower alkyl group containing 1 to 4 carbon atoms, with the proviso that R.sub.2 and R.sub.2 ', together with N, may form a 5- or 6-membered saturated heterocyclic ring which may contain an additional heteroatom, selected from the group consisting of as O, N and S, or R.sub.2 ' represents an aralkyl group;wherein R.sub.3 and R.sub.4 are each selected from the group consisting of a hydrogen atom, a halogen, a nitro group and a methoxy group; andwherein R.sub.5 is selected from the group consisting of a halogen, a difluoromethoxy group, a trifluoromethyl group, a nitro group, a carbamylmethoxy group, a cyanomethoxy group and a mesyloxy group.Type: GrantFiled: May 12, 1989Date of Patent: May 21, 1991Assignee: Gerot-Pharmazeutika Gesellschaft m.b.H.Inventor: Ludwig H. Schlager
-
Patent number: 5001138Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.Type: GrantFiled: May 4, 1989Date of Patent: March 19, 1991Assignee: Nihon Tokushu Noyaku Seizo, K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
-
Patent number: 4997822Abstract: There are disclosed compounds of the formula ##STR1## The compounds have antitumour and AIDS treatment activity.Type: GrantFiled: February 20, 1987Date of Patent: March 5, 1991Assignee: Asta Pharma AktiengesellschaftInventors: Hans-Jurgen Hohorst, Ludmilla Bielicki, Georg Voelcker, Ulf Niemeyer
-
Patent number: 4994569Abstract: Compounds of formula: ##STR1## in which R.sub.1 denotes 2-indolyl, 2-thienyl, 3-furyl, naphthyl, phenyl, or phenyl substituted with one or two halogen atoms, with alkoxy, alkyl, nitro, acylamino, alkylthio, acyl, trifluoromethoxy, morpholino, piperidino, amino, mono- or dialkylamino or, at the 3- and 4-positions, with methylenedioxyR.sub.2 denotes phenyl or phenyl substituted with one or two halogen atoms, with one or two alkyl radicals, with alkoxy, nitro, trifluoromethyl or hydroxy or, at the 3- and 4-positions, with methylenedioxy andeither X denotes oxygen andR.sub.3 denotes phenyl R.sub.4, R.sub.5 and R.sub.6 denote hydrogen, orR.sub.3 and R.sub.4 denote hydrogen, R.sub.5 denotes hydrogen or methyl and R.sub.6 denotes phenyl or one of R.sub.3 and R.sub.4 denotes methyl and the other hydrogen, R.sub.5 denotes hydrogen and R.sub.6 denotes phenyl,or X denotes sulphur, R.sub.3 denotes phenyl and R.sub.4, R.sub.5 and R.sub.Type: GrantFiled: November 1, 1989Date of Patent: February 19, 1991Assignee: Rhone-Poulenc SanteInventors: Jean-Dominique Bourzat, Claude Cotrel, Claude Guyon, Philippe Pitchen
-
Patent number: 4988384Abstract: Disclosed herein are herbicidal pyridine compounds substituted at the 3- and/or 5-position with a carboxylic acid-derived heterocyclic moiety, as well as herbicidal compositions and use of these compounds.Type: GrantFiled: December 24, 1987Date of Patent: January 29, 1991Assignee: Monsanto CompanyInventors: Yuen-Lung L. Sing, Len F. Lee
-
Patent number: 4988723Abstract: Benzopyran derivatives of formula (I) wherein the substituents are as defined herein are provided. The compounds possess vasodilating activity and are useful in the treatment of hypertension. Pharmaceutical compositions and methods of treating hypertension are also provided.Type: GrantFiled: May 17, 1989Date of Patent: January 29, 1991Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Koichi Takimoto, Kohei Takenaka, Takeshi Kato
-
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
-
Patent number: 4960908Abstract: Novel isoflavone derivatives are provided which have the formula ##STR1## and which exhibit cancerocidal and immunosuppressive activity. The invention also provides pharmaceutical compositions containing the derivatives, methods of use and processes for their preparation.Type: GrantFiled: October 21, 1988Date of Patent: October 2, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Hiroshi Ogawara, Shunichi Watanabe
-
Patent number: 4954509Abstract: 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 and R.sub.1 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 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group; R.sub.4 and R.sub.5, which may be the same or different and may be attached to the same or different carbon atoms of the isoquinoline nucleus, are each hydrogen, halogen, hydroxy, C.sub.1-6 alkyl, aryl, or R.sub.4 together with R.sub.5 form a --(CH.sub.2).sub.p -- group, where p is an integer of from 1 to 5 and one or more of the --(CH.sub.2)-- moieties is optionally substituted by a C.Type: GrantFiled: February 17, 1989Date of Patent: September 4, 1990Assignee: Dr. Lo. Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Giuseppe Giardina
-
Patent number: 4931444Abstract: 4-(4-phenyl-1-piperazinyl)phenols for use as 5-lipoxygenase inhibitors and a method of treating warm-blooded animals suffering from leukotriene mediated diseases and disorders using the same. Pharmaceutical compositions containing the same as active ingredient. Novel compounds used in said method and processes for preparing said novel compounds.Type: GrantFiled: January 12, 1989Date of Patent: June 5, 1990Assignee: Janssen Pharmaceutica N.V.Inventors: Jean P. F. Van Wauwe, Jan Heeres, Leo J. J. Backx
-
Patent number: 4916124Abstract: Novel indoloquinoxalines having substituents in 6-position containing cyclic groups, of the general formula I ##STR1## wherein R.sub.1 represents hydrogen or one or several preferably 1 to 4, similar or different substituents in the positions 1-4 and/or 7-10, selected from halogen, lower alkyl-/alkoxy group having not more than 4 carbon atoms, trifluoromethyl group, trichloromethyl group;X is a group ##STR2## wherein Y is CH.sub.2, NH, O or S and a is 2, 3 or 4 and wherein also the bond --C.dbd.N-- can be saturated; Z is alkyl having 1-6 carbon atoms, Cl, Br or CF.sub.3 andR.sub.3 represents hydrogen, lower alkyl-/cycloalkyl group having not more than 4 carbon atoms,and the physiologically acceptable addition products of the compounds with acids and halogen adducts are described. Also methods for preparing said compounds by reaction of a compound of the formula II ##STR3## with a reactive compound containing the residue --CHR.sub.Type: GrantFiled: November 18, 1987Date of Patent: April 10, 1990Assignee: Lief LundbladInventors: Jan O. E. Bergman, Stig G. Akerfeldt
-
Patent number: 4904660Abstract: Novel compounds of the following formula (I) and their salts: A compound of the formula (I) ##STR1## These compounds are expected to be useful for renin inhibitors. Thus, the compounds are useful medical agents, in particular, anti-hypertensive agents.Type: GrantFiled: February 25, 1988Date of Patent: February 27, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kohji Nakano, Takashi Fujikura, Ryuichiro Hara, Masato Ichihara, Yukiko Fukunaga, Masayuki Shibasaki
-
Patent number: 4861879Abstract: Substituted [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H -imidazoles and 1H-1,2,4-triazoles having antimicrobial properties and being particularly useful in the treatment of vaginal candidosis.Type: GrantFiled: February 9, 1988Date of Patent: August 29, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Heeres, Raymond A. Stokbroekx, Leo J. J. Backx
-
Patent number: 4851406Abstract: The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.Type: GrantFiled: September 4, 1986Date of Patent: July 25, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Wolfgang von der Saal, Walter-Gunar Friebe, Bernd Muller-Beckmann, Gisbert Sponer
-
Patent number: 4849432Abstract: Novel heterocyclic compounds of the formula ##STR1## wherein, R.sup.1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group ##STR2## in which R.sup.2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R.sup.3 represents a hydrogen atom or an alkyl group, and Z represents an optionally sibstituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group.The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: February 24, 1987Date of Patent: July 18, 1989Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hattori
-
Patent number: 4839356Abstract: The invention provides thiazinone derivatives of general formula I: ##STR1## wherein X is O, S or NH, and R represents an optionally substituted alkyl, alkenyl, heterocyclic or aryl group; a process for the preparation of such compounds; compositions containing them and their use as fungicides.Type: GrantFiled: May 13, 1987Date of Patent: June 13, 1989Assignee: Shell Internationale Research Maatschappij B.V.Inventor: Mandy E. Coombs
-
Patent number: 4835280Abstract: The present invention provides Indolines of the formula: ##STR1## ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.Type: GrantFiled: July 14, 1987Date of Patent: May 30, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Martens, Jens-Peter Holck, Herbert Berger, Bernd Muller-Beckman, Klaus Strein, Egon Roesch
-
Patent number: 4832732Abstract: Novel herbicidal 1-methyl-1H-imidazole -5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Further the invention also relates to a process for making these novel compounds.Type: GrantFiled: December 17, 1987Date of Patent: May 23, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: William R. Lutz, Guy R. E. Van Lommen, Victor Sipido, Wim G. Verschueren
-
Patent number: 4831032Abstract: The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.Type: GrantFiled: July 3, 1986Date of Patent: May 16, 1989Assignee: Boehringer Mannheim GmbHInventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
-
Patent number: 4824472Abstract: Novel herbicidal 1-cyclyl or polycyclyl substituted 1H-imidazole-5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Processes for making these novel compounds.Type: GrantFiled: December 23, 1987Date of Patent: April 25, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Guy R. E. Van Lommen, Victor Sipido, Wim G. Verschueren, William R. Lutz
-
Patent number: 4820842Abstract: The present invention provides a process for preparing a 5-cyano-2-substituted-1,4-dihydropyridine compound having cardiovascular activity.Type: GrantFiled: September 11, 1987Date of Patent: April 11, 1989Assignee: Warner-Lambert CompanyInventors: Kevin R. Anderson, Ila Sircar
-
Patent number: 4818754Abstract: A compound of the formula (1) or a salt or solvate thereof: ##STR1## in which: R.sub.0 is hydrogen or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 are both hydrogen; orR.sub.1 is hydrogen, C.sub.1-6 alkyl; and R.sub.2 is CN; CR.sub.5 R.sub.6 Y where R.sub.5 and R.sub.6 are independently selected from hydrogen and C.sub.1-4 alkyl and Y is selected from hydrogen, OR.sub.7 or SR.sub.7 where R.sub.7 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, and NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkanoyl or together are C.sub.4-6 polymethylene; or COR.sub.10 is OH or C.sub.1-4 alkyl, or COR.sub.10 is a pharmaceutically acceptable ester or amide; orR.sub.2 is hydrogen, C.sub.1-6 alkyl, or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; and R.sub.1 is CN, CR.sub.5 R.sub.6 Y or COR.sub.10 as defined for R.sub.2 above; orR.sub.1 and R.sub.2 together form C.sub.3 -C.sub.Type: GrantFiled: April 16, 1987Date of Patent: April 4, 1989Assignee: Beecham Group p.l.c. of Beecham HouseInventors: Robert W. Ward, Roger E. Markwell, Ian Hughes
-
Patent number: RE34299Abstract: The present invention relates to novel indole derivatives which have interesting pharmacodynamic effects indicating pronounced activity in the treatment of psychic disorders, especially psychoses and, at the same time, a low degree of undesired side effects.Moreover, the invention relates to methods for the preparation of said indole derivatives, pharmaceutical compositions containing same, and methods for the treatment of psychic disorders, especially psychoses, by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings.The novel indole derivatives of the present invention are represented by the following formula; ##STR1## wherein R is phenyl, optionally substituted with halogen.[., lower alkyl or trifluoromethyl,.]. or a hetero aromatic group, such as 2-thienyl, 3-thienyl, .[.2-furoyl, 3-furoyl, 2-thiazol, 2-oxazol, 2-imidazole, 2-pyridyl, 3-pyridyl.]. .Iadd.2-oxazolyl, 2-imidazolyl, 2-pyridyl 3-pyridyl.Iaddend.or 4-pyridyl; R.sup.Type: GrantFiled: September 13, 1991Date of Patent: June 29, 1993Assignee: H. Lundbeck A/SInventor: Jens K. Perregaard