Abstract: An intermediate useful in the synthesis of milbemycin derivatives having an ether bond at the 13-position and which is represented by the general formula (IIId): ##STR1## wherein R represents a methyl group, an ethyl group, an isopropyl group or a sec-butyl group, and R.sup.5 and R.sup.6' each individually represents a hydrogen atom or a protecting group,and related precursors as well as to a process for producing these intermediates.
Type:
Grant
Filed:
May 11, 1995
Date of Patent:
April 29, 1997
Assignee:
Sankyo Company, Limited
Inventors:
Mitsugi Shibano, Mutsuo Suzuki, Shunshi Kojima
Abstract: Benzodifurantriones of Formula (1): ##STR1## in which W is unsubstituted or substituted aryl, a process for their preparation via dioxo intermediates and processes for their conversion into benzodifuranone dyes and compounds of Formula (7): ##STR2## are provided wherein R.sup.3 is --H, --COR.sup.2, --SO.sub.2 R.sup.2 -- which R.sup.2 is alkyl, cycloalkyl, aryl or aralkyl and R.sup.4 is --COOR.sup.2, --CONRR.sup.1 in which R and R.sup.1 each independently is --H, alkyl, cycloalkyl, aryl or aralkyl; --COOH or the alkali metal, alkaline earth metal or ammonium salts thereof; or --COX.sup.2 -- which X.sup.2 is halo.
Abstract: A process for the manufacture of Form 1 ranitidine hydrochloride (N-[2-[[[5-(Dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl-N'-methyl-2- nitro-1,1-ethenediamine) hydrochloride, is described. A process to convert ranitidine hydrochloride Form 2 to Form 1 is also described.
Type:
Grant
Filed:
June 24, 1994
Date of Patent:
April 15, 1997
Assignee:
Ranbaxy Laboratories Limited
Inventors:
Jag M. Khanna, Naresh Kumar, Brij Khera, Mahavir S. Khanna
Abstract: A process for producing 3-methyltetrahydrofuran, wherein in a first step, prussic acid is reacted with methyl methacrylate to produce methyl 3-cyanoisobutyrate. The methyl 3-cyanoisobutyrate is then reacted with water and sulfuric acid to produce a resultant product which is reacted with a C.sub.1 -C.sub.8 aliphatic alcohol to produce a methylsuccinic acid ester. The methylsuccinic acid ester is catalytically hydrogenated to prepare the 3-methyltetrahydrofuran. Alternatively, the methyl 3-cyanoisobutyrate is hydrated to produce methyl 3-carbamoylisobutyrate, which is then reacted with a formic acid ester to form a methylsuccinic acid ester and formamide and the resultant methylsuccinic acid ester is catalytically hydrogenated. The 3-methyltetrahydrofuran is produced in high selectivity and in a commercially advantageous manner from inexpensive reactants. The 3-methyltetrahydrofuran is useful as a commoner for producing polyether glycol, which is utilized as starting raw material for preparing spandex fiber.
Abstract: Compounds of Formula 1 ##STR1## where R.sub.1 -R.sub.7 are hydrogen, lower alkyl of 1-6 carbons, or halogen;Y is phenyl, pyridyl, furyl, thienyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl;A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds;B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.14, CR.sub.14 (OR.sub.12).sub.2, or CR.sub.14 OR.sub.13 O, where R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.
Type:
Grant
Filed:
April 10, 1995
Date of Patent:
April 8, 1997
Assignee:
Allergan
Inventors:
Roshantha A. Chandraratna, Richard L. Beard
Abstract: Described are stelleramacrin A and stelleramacrin B represented by the following formulas (I) and (II), respectively: ##STR1## a process for the preparation thereof; and anticancer agents containing either of them as an active ingredient.Therapeutics for solid cancer, said therapeutics containing either of gnidimacrin or pimelea factor P.sub.2 as an active ingredient, are also described.
Abstract: Triggerable dioxetanes with a fluorescent substituent bonded or tethered in the dioxetane so as to produce fluorescence from the group are described. The compounds are of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are carbon containing groups and wherein one of R.sub.1, R.sub.2 and R.sub.3 is a tethered fluorescent substitutent. The compounds are useful in immunoassays and in probes using enzymes or other chemicals for triggering the dioxetanes to produce light from the fluorescent molecule in the group as a signal.
Type:
Grant
Filed:
December 27, 1988
Date of Patent:
April 1, 1997
Assignee:
Board of Governors of Wayne State University
Abstract: Preparation process for 2-coumaranone in which glyoxylic acid, in vapor phase, is reacted with cyclohexanone, in the presence of a dehydrogenation catalyst.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
April 1, 1997
Assignee:
Societe Francaise Hoechst
Inventors:
Jean-Claude Vallejos, Alain Perrard, Yani Christidis, Pierre Gallezot
Abstract: A compound of formula (I) ##STR1## wherein X is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, trifluoromethyl, or C.sub.1 -C.sub.3 alkoxy;Y is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, or C.sub.1 -C.sub.3 alkoxy;R is hydroxyl, methoxy, or amine; or a pharmaceutically acceptable acid addition salt thereof, useful for treating various neurological conditions.
Type:
Grant
Filed:
December 28, 1995
Date of Patent:
March 25, 1997
Assignee:
Synthelabo
Inventors:
Benoit Marabout, Mireille Sevrin, Jacques Froissant, Emmanuelle Dachary
Abstract: 13-Substituted milbemycin derivatives having the formula (I): ##STR1## wherein: R.sup.1 is methyl, ethyl, isopropyl or sec-butyl;R.sup.2 is hydrogen or alkyl;X is (.alpha.-hydroxyimino- or .alpha.-alkoxyimino-substituted)-arylmethyl or (.alpha.-hydroxyimino- or .alpha.-alkoxyimino-substituted)-heterocyclylmethyl, N-substituted-aminophenyl or N-substituted-aminophenoxy;m is 0 or 1; and n is 0 or 1;are valuable as agricultural and horticultural anthelmintic, acaricidal and insecticidal agents.
Abstract: Process for the enzymatic production of isomerically pure compounds having the general formulae I and II ##STR1## in which the substituents R have the meanings stated in the claims, as well as their use for the production of isomerically pure isosorbide-2-nitrate having the formula V and isosorbide-5-nitrate having the formula VI, ##STR2## which are both important as therapeutic agents for coronary diseases.
Abstract: The invention relates to the process for the preparation of new derivatives of amino-ascorbic acid, their acid and alkali salts, processes for preparation and action.According to this invention derivatives of amino-ascorbic acid are prepared by three types of reactions: 1. reductive alkylation of amino-ascorbic acid; 2. alkylation of primary and secondary amines with halogen-ascorbic acid and 3. acylation of amino-ascorbic acid.
Type:
Grant
Filed:
September 18, 1995
Date of Patent:
March 11, 1997
Assignee:
Pliva, farmaceutska, kemijska, prehrambena i kozmeticka industrija dionicko drustvo
Inventors:
Bo zidar Su skovi c, Vanja Vela, Mira Bun ci c
Abstract: The present invention relates to a new 3-aryl-4-hydroxy-.DELTA..sup.3 -dihydrofuranone derivatives of the general formula (I) ##STR1## in which the radicals A, B, G, X, Y, Z and n have the meaning given in the description, to a plurality of processes for their preparation, and to their use as pesticides.
Type:
Grant
Filed:
September 9, 1994
Date of Patent:
March 11, 1997
Assignee:
Bayer Aktiengesellschaft
Inventors:
Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kr uger, Hans-Joachim Santel, Markus Dollinger, Ulrike Wachendorff-Neumann, Christoph Erdelen
Abstract: N-Acylpiperidines of general structure ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
Abstract: Cyclohexane derivatives of the formula I ##STR1## in which the radicals are as defined in the description, and processes for the preparation of these compounds, are described. Also described are novel intermediates for the preparation of the compounds of the formula I.
Abstract: An enantioselective multi-stage process is described which uses as a starting material an .alpha.,.beta.-unsaturated olefin of formula (1):Ar--CH.dbd.C(R.sup.4)COAux (1)where Ar and R.sup.4, which may be the same or different, is each a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; and Aux is the residue of a chiral (R- or S-) auxiliary.In the process, the olefin is converted to a chiral triarylethane which is of use in medicine.
Type:
Grant
Filed:
December 21, 1994
Date of Patent:
March 4, 1997
Assignee:
Celltech Therapeutics Limited
Inventors:
Rikki P. Alexander, Graham J. Warrellow, John C. Head, Ewan C. Boyd, John R. Porter