Abstract: An enzymatic reduction method, particularly a stereoselective enzymatic reduction method, for the preparation of compounds useful as intermediates in the preparation of taxanes.
Type:
Grant
Filed:
November 12, 1992
Date of Patent:
May 30, 1995
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Ramesh N. Patel, Amit Banerjee, Clyde G. McNamee, John K. Thottathil, Laszlo J. Szarka
Abstract: A diamine compound having formula (I): ##STR1## wherein R.sup.1 is hydrogen, an alkyl group having 1 to 6 carbon atoms which may have a substituent, an alkoxyl group having 1 to 6 carbon atoms which may have a substituent, an aryl group which may have a substituent, or an alkenyl group having 1 to 6 carbon atoms which may have a substituent; Ar.sup.1 is an aryl group which may have a substituent; Ar.sup.2 is a bivalent group selected from the group consisting of an arylene group and a stilbene group, which may have a substituent; n is an integer of 0 to 2; and X is a group selected from the group consisting of: ##STR2## in which R.sup.2 is hydrogen, an alkyl group having 1 to 6 carbon atoms which may have a substituent, an aryl group or a halogen; R.sup.3 and R.sup.4 each is an alkyl group having 1 to 6 carbon atoms or an aryl group.
Abstract: A method is disclosed for the production of .alpha.-APM HCl by treating an F-.alpha.-AP derivative with a mixed solvent of methanol, hydrochloric acid and water, wherein the solubility of .alpha.-APM HCl is lowered to increase the separation yield thereof.
Abstract: The present invention relates to novel compounds for use as imaging agents. In particular, the present invention relates to imaging agents comprising a heavy metal cluster having 2 to 8 atoms of the same of different heavy metal elements, and at least one coordinating ligand having 1 to 8 atoms which bond to the cluster, and a number of supporting atoms making up the framework of the ligand.
Type:
Grant
Filed:
February 2, 1994
Date of Patent:
May 23, 1995
Assignee:
Mallinckrodt Medical, Inc.
Inventors:
Edward A. Deutsch, Karen F. Deutsch, Dennis L. Nosco
Abstract: Disclosed herein is a process for producing a sulfoneamide represented by the following formula (6) as an intermediate of a 6-haloalkyl-3-phenyluracil derivative, from as a starting material 4-halogeno-3-nitroaniline (9) or 2-halogeno-5-nitroaniline (10): ##STR1## (wherein X and Y independently represent a halogen atom, R represents a C.sub.1 -C.sub.4 alkyl group or a C.sub.1 -C.sub.3 haloalkyl group and R' represents a C.sub.1 -C.sub.4 alkyl group or a phenyl group).
Type:
Grant
Filed:
June 23, 1994
Date of Patent:
May 16, 1995
Assignee:
Nissan Chemical Industries Ltd.
Inventors:
Yasuo Kawamura, Jun Satow, Kenzou Fukuda, Kaoru Itoh, Hiroshi Kita
Abstract: An improved process for the isomerization of saturated alkyl carboxylic acids is obtained by using aluminum iodide or aluminum bromide promoted rhodium or iridium catalysts.
Abstract: A new process and new intermediates are described for the preparation of 2-oximinoactic acid derivatives of the formula (I) ##STR1## in which R.sup.1, R.sup.2, n, Z and Ar have the meaning given in the description and which are used as pesticides.
Type:
Grant
Filed:
May 6, 1994
Date of Patent:
May 2, 1995
Assignee:
Bayer Aktiengesellschaft
Inventors:
Dietmar Kuhnt, Herbert Gayer, Peter Gerdes
Abstract: A process is reported for the preparation of bis(amidocarboxylic acid) involving the steps of:(i) charging a reactor with an acyl halide and an aminocarboxylate compound being formed from and selected from lactams and aminocarboxylic acids;(ii) slowly adding to the reaction medium an alkali at a rate to maintain a pH between 10 and 14; and(iii) recovering the bis(amidocarboxylic acid) from the reaction medium.The recovery procedure advantageously includes acidification of the reaction medium to a pH between 4.5 and 7. The preferred product of the process is N,N'-terephthaloyl-di(6-aminocaproic acid).
Type:
Grant
Filed:
November 12, 1993
Date of Patent:
April 25, 1995
Assignee:
Lever Brothers Company, Division of Conopco, Inc.
Inventors:
Janet L. Coope, AnneMarie Brescia, Stephen A. Madison
Abstract: Mercaptocycloacyl aminoacid inhibitors of endopeptidase of the formula ##STR1## or a pharmaceutically acceptable salt thereof, alone or in combination with an ACE inhibitor or an ANF, in the treatment of cardiovascular disorders such as hypertension, congestive heart failure, edema and renal insufficiency, and treatment of nephrotoxicity pain conditions, and pharmaceutical compositions containing said compounds are disclosed.
Abstract: A compound of formula (I): selected from 1,5-diyne-3-cyclodecene and undecene compounds. ##STR1## in which: R represents a hydrogen atom, a straight-chain or branched (C.sub.1 -C.sub.6) acyl radical or a glycoside radical,R' represents a hydrogen atom ##STR2## n is 1 or 2, and R.sub.1 and R.sub.2 simultaneously represent two hydrogen atoms or, together with the two carbon atoms and the double bond to which they are attached, form a phenyl ring.
Type:
Grant
Filed:
September 30, 1992
Date of Patent:
April 11, 1995
Assignee:
Adir et Compagnie
Inventors:
Jean-Marie Beau, Christophe Crevisy, Ghanem Atassi, Alain Pierre
Abstract: Condensates (K) of(A) oligohydroxy-C.sub.3-8 -alkanes containing at least 3 hydroxy groups and (B) KOH,that contain at least 5% by weight of K.sup.+ and at least one alcoholic hydroxy groupare eminently suitable as oxyalkylation catalysts, in particular for the oxyalkylation of ester group-containing substrates, before all of natural, vegetable or animal fats or oils or their modification products.
Abstract: The invention relates to 9-substituted bicyclo[3.3.0]octane derivatives of formula I, ##STR1## and their salts with physiologically compatible bases, as well as the .alpha.-, .beta.- or .gamma.-cyclodextrin clathrates, as well as the compounds of formula I encapsulated with liposomes, process for their production and their pharmaceutical use.
Type:
Grant
Filed:
June 11, 1993
Date of Patent:
April 11, 1995
Assignee:
Schering Aktiengesellschaft
Inventors:
Ulrich Klar, Helmut Vorbruggen, Hartmut Rehwinkel, Karl Thierauch, Peter Verhallen
Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalyzed reactions.
Type:
Grant
Filed:
July 22, 1993
Date of Patent:
April 11, 1995
Assignees:
Zeneca Limited, Cancer Research Campaign Technology Limited
Inventors:
Philip J. Burke, Robert I. Dowell, Anthony B. Mauger, Caroline J. Springer
Abstract: The present invention relates to disodium 4-chlorophenylmethylenebisphosphonate monohydrate. The invention also relates to a method of preparing this form of the monohydrate, as well as to pharmaceutical compositions in which disodium tiludronate monohydrate is present as the active principle.
Type:
Grant
Filed:
August 4, 1993
Date of Patent:
April 11, 1995
Assignee:
Sanofi
Inventors:
Michel Bonnery, Michel Bouisset, Raphael Sole
Abstract: A derivative of general formula: ##STR1## wherein Y is --SO.sub.2 --or ##STR2## (i) R.sup.1 and R.sup.2, which may the same or different, each represent, (1) --H,(2) C1-16 alkyl or (3) the formula ##STR3## wherein X is single-bond, --SO.sub.2 --, C1-4 alkylene, C1-4 alkylene substituted by --COOH or ##STR4## is a pyridyl or pyrrolyl ring, n is 1.about.5, R.sup.4 is 1 --H or C1-8 alkyl, 2 C1-14 alkoxy 3 C1-6 alkylthio, 4 --OH, halogen, --NO.sub.2 or trihalomethyl, 5 the formula: --NR.sup.41 R.sup.42 wherein R.sup.41 and R.sup.42 each represents halogen or C1-4 alkyl, 6 tetrazole, 7 --SO.sub.3 H or --CH.sub.2 OH, 8 the formula:--SO.sub.2 NR.sup.41 R.sup.42 9 the formula: --Z.sup.41 --COOR.sup.43 wherein Z.sup.41 is single-bond C1-4 alkylene or C2-4 alkenylene, R.sup.43 is --H C1-4 alkyl or benzyl; or non-toxic salt or an acid addition salt thereof possess inhibitory activity on elastase, and therefore is useful for treating pulmonary emphysema, atherosclerosis and rheumatoid arthritis and the like.
Abstract: Intermediates for transforming (2S,3S)-2-amino-3-phenyl-1,3-propanediols into their (2R,3R)-enantiomers are described. The final compounds are useful intermediates for the synthesis of antibiotics like chloramphenicol, Thiamphenicol and Florfenicol.
Type:
Grant
Filed:
September 28, 1993
Date of Patent:
March 28, 1995
Assignee:
Zambon Group S.p.A.
Inventors:
Marco Villa, Claudio Giordano, Silvia Cavicchioli, Silvio Levi
Abstract: A liquid phase process for making perfluorinated organic substances which comprises directly contacting in a temperature-controlled reactor a diluted solution or dispersion of a perfluorinateable, organic substance in a liquid, inert medium with a stoichiometric excess of fluorine gas, optionally diluted with an inert gas, to perfluorinate said organic substance at a temperature and a flow rate of inert gas (if used) sufficient to volatilize the resulting by-product hydrogen fluoride, removing said hydrogen fluoride from the reactor as it is produced, and separately removing from the reactor the resultant solution or dispersion of perfluorinated organic substance.
Type:
Grant
Filed:
February 1, 1994
Date of Patent:
March 21, 1995
Assignee:
Minnesota Mining and Manufacturing Company
Inventors:
Michael G. Costello, George G. I. Moore
Abstract: The average molecular weight of polyoxyalkylene glycols and polyoxyalkylene glycol derivatives is adjusted in the heteropolyacid-catalyzed polymerization of cyclic ethers and/or acetals with ring cleavage in the presence of proton donors by a process in which the amount of the relevant proton donor present in the reaction system is regulated in the course of the reaction by the measurement of the electrical conductivity.
Type:
Grant
Filed:
August 20, 1993
Date of Patent:
March 7, 1995
Assignee:
BASF Aktiengesellschaft
Inventors:
Hans-Juergen Weyer, Rolf Fischer, Gerhard Jeschek, Herbert Mueller
Abstract: This invention relates to a process for obtaining 10-deacetylbaccatin III from various parts of yew (Taxus sp.) by extraction and selective crystallization starting with a methanolic extract of the vegetable matter.
Abstract: A process is reported for the preparation of bis(amidocarboxylic acid) involving reacting an ester with an aminocarboxylate compound, the latter being formed from lactams or aminocarboxylic acids and salts thereof. The ester and aminocarboxylate compound are present in a weight ratio of about 1:1 to about 1:4, and reaction is conducted in a mono- or polyhydric alcohol solvent.
Type:
Grant
Filed:
April 26, 1994
Date of Patent:
February 28, 1995
Assignee:
Lever Brothers Company, Division of Conopco, Inc.
Inventors:
Janet L. Coope, AnneMarie Brescia, Michael I. Hill, Martina Santoso, Stephen A. Madison