A Ring Or Polycyclo Ring System In A Substituent E Is Attached Indirectly To The Carboxamide Nitrogen Or To An Amino Nitrogen In Substituent E By Acyclic Nonionic Bonding Patents (Class 564/219)
  • Patent number: 5276192
    Abstract: A process for preparing phenoxyethanamines from phenols and 2-oxazolines in quantitative yields was discovered. Phosphoric acid hydrolyzes the amide intermediate from the phenol/2-oxazoline reaction without cleaving the amide at the ether linkage and without undesired aromatic ring substitution. Thus, yield to the desired phenoxyethanamines is often 98% or better, requiring no subsequent purification. In contrast, sulfuric and hydrochloric acids give these undesired side reactions. Phenoxyethanamines are useful in thermosetting resins, pharmaceuticals and as surfactants.
    Type: Grant
    Filed: April 22, 1991
    Date of Patent: January 4, 1994
    Assignee: Texaco Chemical Company
    Inventors: Wei-Yang Su, George P. Speranza
  • Patent number: 5250732
    Abstract: 5,6-Dehydronorketamine and derivatives retaining the .alpha.,.beta.-unsaturated carbonyl are disclosed. These and other Michael or Michael-type acceptors and adducts are shown to influence the replication, differentiation or maturation of blood cells, especially platelet progenitor cells. Accordingly, these compounds are used for treatment of thrombocytopenia.
    Type: Grant
    Filed: July 18, 1991
    Date of Patent: October 5, 1993
    Assignee: Genentech, Inc.
    Inventors: Timothy P. Kogan, Todd C. Somers
  • Patent number: 5248823
    Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: December 4, 1992
    Date of Patent: September 28, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5236953
    Abstract: A compound of the formula ##STR1## wherein X has the formula --CR.sup.5 .dbd.CR.sup.6 --, --C.ident.C-- or ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl;wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent or each is hydrogen or alkyl, alkoxy or dialkylamino, provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substituent;wherein R.sup.5 and R.sup.6, each is hydrogen, halogeno or alkyl; wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 has the formula --Y--Q--R.sup.9 wherein Y is straight- or branched-chain alkylene or alkenylene; wherein Q is --O--, --S--, --SO-- or --SO.sub.2 --;and wherein R.sup.9 is alkyl of up to 6 carbon atoms which contains one or more defined substituents, processes for their manufacture and pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 30, 1991
    Date of Patent: August 17, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Leslie R. Hughes, Howard Tucker
  • Patent number: 5233073
    Abstract: Provided are the dialkyl amines: ##STR1## wherein Q is ##STR2## R is --CH.sub.3 or Q and a has a value of 1 to 3.
    Type: Grant
    Filed: March 23, 1992
    Date of Patent: August 3, 1993
    Assignee: The United States of America as represented by the Secretary of the Air Force
    Inventors: Loon-Seng Tan, Fred E. Arnold
  • Patent number: 5225442
    Abstract: Compounds of general formula: ##STR1## in which A and R are defined in the description. Medicaments containing the same and useful for the treatment of melatoninergic disorders.
    Type: Grant
    Filed: January 3, 1992
    Date of Patent: July 6, 1993
    Assignee: Adir et Compagnie
    Inventors: Jean Andrieux, Raymond Houssin, Said Yous, Beatrice Guardiola, Daniel Lesieur
  • Patent number: 5225601
    Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: October 31, 1991
    Date of Patent: July 6, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5220063
    Abstract: Acylamides or amine acylate salts of arylalkanolamines are prepared by reacting an arylisonitrosoalkanone with hydrogen and a carboxylic acid, carboxylic acid anhydride or carboxylic acid ester or mixture thereof in the presence of a transition metal catalyst; optionally the product is converted to the corresponding arylalkanolamine hydrochloride salt by reaction of the acylamide or amine acylate salt of the arylalkanolamine with hydrogen chloride in a C.sub.1 -C.sub.3 alkyl alcohol.
    Type: Grant
    Filed: May 10, 1991
    Date of Patent: June 15, 1993
    Assignee: Hoechst Celanese Corporation
    Inventors: Ahmed M. Tafesh, Olan S. Fruchey, Charles B. Hilton
  • Patent number: 5185465
    Abstract: Novel 4-phenyl-1,3-benzodiazepines and 2-amino-.alpha.-phenylphenethylamines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants. The 2-amino-.alpha.-phenylphenethylamines are useful as anticonvulsant and neuroprotective agents.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: February 9, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Manfred Worm, Charles A. Crichlow
  • Patent number: 5144074
    Abstract: Carboxamides having the structural formula:R.sup.1 CHR.sup.2 CH(OR.sup.3)NHCR.sup.4 Owherein:R.sup.1 is H, C.sub.1 -C.sub.6 alkyl or aryl;R.sup.2 is H, C.sub.1 -C.sub.6 alkyl;R.sup.3 is benzyl, C.sub.1 -C.sub.8 alkyl or hydroxyalkyl; andR.sup.4 is H, C.sub.1 -C.sub.6 alkyl or aryl;are synthesized by reacting an aldehyde having the structural formula: R.sup.1 CHR.sup.2 CHO wherein R.sup.1 and R.sup.2 are as defined above, with an alcohol having the structural formula: R.sup.3 OH, wherein R.sup.3 is as defined above, and an amide having the structural formula: R.sup.4 CONH.sub.2 wherein R.sup.4 is as defined above, in the presence of a strong acid catalyst at a temperature in the range of 0.degree.-200.degree. C.
    Type: Grant
    Filed: February 24, 1988
    Date of Patent: September 1, 1992
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Mark L. Listemann, Ronald Pierantozzi, John N. Armor
  • Patent number: 5130472
    Abstract: The present invention relates to a new process for the preparation of Erbstatin and Erbstatin analogs, which can be represented by the following formula (I) ##STR1## wherein R is hydrogen, a lower alkyl or a lower alkanoyl group;n is an integer of 1 to 3;A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --;R.sub.1 is hydrogen or a lower alkyl group, andR.sub.2 is a hydrogen or halogen atom.
    Type: Grant
    Filed: November 2, 1990
    Date of Patent: July 14, 1992
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Franco Buzzetti, Angelo Crugnola, Paolo Lombardi
  • Patent number: 5130484
    Abstract: Tertiary amides having utility as antioxidants are compounds corresponding to the formula:(p--HO--C.sub.6 R.sub.n H.sub.4-n --R"--CZZ').sub.2 N--C(O)--R'wherein R and R' are independently selected from alkyl, aryl, and benzyl groups, R" is an alkylene group containing 1-4 carbons, Z and Z' are independently selected from hydrogen and alkyl, and n is an integer of 1-3.
    Type: Grant
    Filed: March 15, 1991
    Date of Patent: July 14, 1992
    Assignee: Ethyl Corporation
    Inventor: Vincent J. Gatto
  • Patent number: 5122537
    Abstract: The invention relates to new arylvinylamide derivatives of formula ##STR1## wherein Y is a bicyclic ring system chosen from (A), (B), (C), (D), and (E); ##STR2## in which m is zero, 1 or 2; R is hydrogen, a C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl group;R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen, cyano or C.sub.1 -C.sub.6 alkyl; andn is an integer of 1 to 3; and wherein each of the substituents --CH.dbd.CHNHCOR.sub.1, OR and R.sub.2 may be independently on either of the aryl and heteroaryl moieties of the bicyclic ring system (A), (C), (D) and (E); whereas only the benzene ring may be substituted in the bicyclic ring system (B),which are useful as tyrosine kinase inhibitors.
    Type: Grant
    Filed: November 2, 1990
    Date of Patent: June 16, 1992
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Franco Buzzetti, Angelo Crugnola
  • Patent number: 5120792
    Abstract: Organic materials which are normally susceptible to oxidative deterioration are stabilized with tertiary amide antioxidants corresponding to the formula:(p--HO--C.sub.6 R.sub.n H.sub.4-n --R").sub.2 N--C(O)--R'wherein R and R' are independently selected from alkyl, aryl, and benzyl groups, R" is an alkylene group containing 1-5 carbons, and n is an integer of 1-3.
    Type: Grant
    Filed: March 15, 1991
    Date of Patent: June 9, 1992
    Assignee: Ethyl Corporation
    Inventor: Vincent J. Gatto
  • Patent number: 5118846
    Abstract: Disclosed is a method which comprises introducing into a reaction zone a feed which comprises a hydroxyl compound reactant, R"OH at least one amide reactant selected from R--CONH.sub.2 and R--CONHR', and a Lewis base as catalyst, thereby reacting R"OH with said amide reactant to produce a reaction mixture containing at least one disubstituted amide selected from R--CONR".sub.2 and R--CONR'R", whereineach of R, R' and R" contains no acetylenic unsaturation and 1 to 30 carbon atoms;each of R, R' and R" is selected from a hydrocarbyl groups and a hydrocarbyl group that is substituted with a group selected from carbamoyl, hydrocarbylcarbamoyl, dihydrocarbylcarbamoyl, and hydroxyl.
    Type: Grant
    Filed: April 27, 1990
    Date of Patent: June 2, 1992
    Assignee: The Standard Oil Company
    Inventor: Mark C. Cesa
  • Patent number: 5114975
    Abstract: The invention relates to novel substituted aryloxyphenylthioureas, aryloxyphenylisothioureas and aryloxyphenylcarobodiimides of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted by one or more halogen atoms and/or C.sub.1 -C.sub.6 alkoxy groups; C.sub.3 -C.sub.8 cycloalkyl, unsubstituted or substituted by one or more C.sub.1 -C.sub.3 alkyl groups; or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl,R.sub.2 and R.sub.3 are each C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen, methyl or --CHO,R.sub.5 is halogen; C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted by one or more halogen atoms; C.sub.1 -C.sub.4 alkoxy, unsubstituted or substituted by one or more halogen atoms; or is a --CH.dbd.CH).sub.2, --CH.sub.2).sub.3 or --CH.sub.2).sub.4 bridge in 2,3- or 3,4-position,n is 0, 1, 2, 3 or 4,Z is --NH--CS--NH--, --N.dbd.C(SR.sub.6)--NH-- or --N.dbd.C.dbd.N--; andR.sub.6 is C.sub.1 -C.sub.
    Type: Grant
    Filed: April 3, 1991
    Date of Patent: May 19, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Manfred Boger, Jozef Drabek, Josef Ehrenfreund
  • Patent number: 5087743
    Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: January 23, 1990
    Date of Patent: February 11, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5053548
    Abstract: There is disclosed a biphenyl derivative of the formula (B): ##STR1## wherein R.sup.1, R.sup.3, R.sup.4, R.sup.5 and R.sup.c are as defined or its salt, a composition for nerve cell degeneration repairing or protecting agent containing a phenyl derivative selected from compounds (1) to (4) and (B) as defined, and a process for preparing a phenyl derivative contained in the composition.
    Type: Grant
    Filed: February 8, 1990
    Date of Patent: October 1, 1991
    Assignee: Otsuka Pharmaceutical Company, Ltd.
    Inventors: Tatsuyoshi Tanaka, Yoji Sakurai, Hiroshi Okazaki, Takashi Hasegawa, Yoshiyasu Fukuyama
  • Patent number: 5021414
    Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --,wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.
    Type: Grant
    Filed: December 18, 1989
    Date of Patent: June 4, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
  • Patent number: 5011854
    Abstract: A hydroxamic acid compound represented by the general formula (I) or a salt thereof; ##STR1## wherein R.sup.1 represents a hydrogen atom, or a substituted or unsubstituted alkanoyl group, R.sup.2 represents an unsubstituted alkanoyl, substituted lower alkanoyl or substituted lower alkyl group, and m represents an integer of 3 to 7, which are useful for the prevention and/or treatment of diseases caused by lipoxygenase-mediated metablites.
    Type: Grant
    Filed: December 7, 1989
    Date of Patent: April 30, 1991
    Assignee: Kyowa Hakko Kogyo Co. Ltd.
    Inventors: Mitsuru Takahashi, Shigeto Kitamura, Hiroshi Kase, Masaji Kasai, Isao Kawamoto, Takao Iida, Hiroshi Sano, Hiromitsu Saito, Koji Yamada, Chikara Murakata
  • Patent number: 4992588
    Abstract: O-acrylaminomethylbenzyl halides (I) ##STR1## in which X is Cl or Br and R.sup.1 is alkyl or aryl, are obtained by reacting an o-aminomethylbenzyl alkyl ether (II) ##STR2## with an acylating agent, and then reacting the resulting acid amide, preferably without intermediate isolation, with an aqueous hydrohalic acid.
    Type: Grant
    Filed: July 31, 1985
    Date of Patent: February 12, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Josef Mueller, Walter-Weilant Wiersdorff, Werner Kirschenlohr, Gerd Schwantje
  • Patent number: 4988730
    Abstract: The invention relates to novel diphenylpropylamine derivatives of the general formula (I). ##STR1## R.sup.1 stands for hydrogen or a methyl group; R.sup.2 stands for hydrogen, a methyl or n-decyl group;Z means a phenyl group substituted by R.sup.3, R.sup.4 and R.sup.5, whereinR.sup.3 means hydrogen, fluorine, chlorine or bromine, or a nitro, C.sub.1-12 alkyl, C.sub.1-4 alkoxy, phenoxy or benzyloxy group;R.sup.4 and R.sup.5 represent hydrogen, chlorine or a hydroxy, alkoxy, benzyloxy, acetamino or carboxy group; orR.sup.4 and R.sup.5 together form a methylendioxy group;orZ may stand for a 4-methoxynaphtyl or 4-ethoxy-naphthyl group; andR.sup.6 stands for hydrogen or fluorine, with the proviso that each of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 cannot simultaneously stand for hydrogen, as well as their physiologically acceptable acid addition salts.The invention also relates to a process for the preparation of these compounds and to the pharmaceutical compositions containing these compounds.
    Type: Grant
    Filed: July 21, 1989
    Date of Patent: January 29, 1991
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyar RT
    Inventors: Dezso Korbonits, Pal Kiss, Laszlo Szekeres, Gyula Papp, Gabor Kovacs, Andrea Santane Csutor, Sandor Virag, Eva Udvari, Imre Bata, Katalin Marmarosi nee Kellner, Laszlo Tardos, Peter Kormoczy, Vera Gergely, Zoltan Vargai
  • Patent number: 4983630
    Abstract: There are provided new 2,2-difluorocyclopropylethane derivatives of general formula I ##STR1## in which A, B and R.sup.1-5 have the meanings given in the description and processes for their preparation. The compounds of the invention can be used as pesticides, especially against insects and mites.
    Type: Grant
    Filed: November 28, 1988
    Date of Patent: January 8, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Peter Wegner, Hartmut Joppien, Gunter Homberger, Arnim Kohn
  • Patent number: 4980366
    Abstract: Novel 4'-hydroxybenzylamine derivatives of the formula ##STR1## pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, succh as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.
    Type: Grant
    Filed: March 16, 1989
    Date of Patent: December 25, 1990
    Assignee: Warner-Lambert Co.
    Inventors: Graham Johnson, Michael F. Rafferty
  • Patent number: 4950795
    Abstract: Compounds of the formula I ##STR1## in which n is 1-30 and X, Y, R, Ar.sup.1 and Ar.sup.2 are as defined in claim 1 can be prepared by reaction of a benzil dialkyl ketal with a diol. Depending on the molar ratio of the two reaction components, products having a different polycondensation degree n are obtained. The compounds can be used as photoinitiators.
    Type: Grant
    Filed: August 18, 1988
    Date of Patent: August 21, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Rinaldo Husler, Rudolf Kirchmayr, Werner Rutsch, Manfred Rembold
  • Patent number: 4933493
    Abstract: Novel 4-phenyl-1,3-benzodiazepines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: June 12, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Manfred Worm, Charles A. Crichlow
  • Patent number: 4925877
    Abstract: The present invention provides new physiological active substance erbstatin analogue compounds of a general formula (I), which have excellent tyrosine-specific protein-kinase inhibitory activity, antitumor activity and antimicrobial activity. ##STR1## (in which R.sup.1 represents a hydrogen atom, a lower alkanoyl group or a lower alkyl group; n represents a positive integer of 1 to 3;X represents a hydrogen atom or a halogen atom;Y represents a group of formula --CH.dbd.CH--NC, --CH.dbd.CH--NHR.sup.2 or --CH.sub.2 --CH.sub.2 --NHR.sup.2(where R.sup.2 represents a formyl group or a lower alkanoyl group; with the exception of the cases where X is hydrogen atom, (R.sup.1 O).sub.n group is 2,5-dihydroxy group and Y is --CH.dbd.CH--NHCHO or --CH.sub.2 --CH.sub.2 --NHCHO).The present invention further provides a tyrosine-specific protein-kinase inhibitor, tumoricide or bactericide containing at least one compound of the said formula (I).
    Type: Grant
    Filed: February 20, 1987
    Date of Patent: May 15, 1990
    Assignee: Zaidanhojin Biseibutsu Kagaku Kenkyukai
    Inventors: Hamao Umezawa, deceased, Tomio Takeuchi, Kuniaki Tatsuta, Kunio Isshika, Masaya Imoto
  • Patent number: 4922016
    Abstract: N-(sulfonylmethyl)formamides are obtained by reacting a sulfinic acid, formaldehyde and formamide in the presence of a second acid and a controlled amount of water. The formamides can be converted to the corresponding sulfonylmethylisocyanides.
    Type: Grant
    Filed: July 26, 1989
    Date of Patent: May 1, 1990
    Assignee: Gist-Brocades N.V.
    Inventor: Nicolaas C. M. E. Barendse
  • Patent number: 4886911
    Abstract: The invention concerns compounds of formula I ##STR1## wherein: X and Y are independently selected from the group consisting of hydrogen, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 haloalkyl, and the group wherein X and Y together from a three or four-membered carbon bridge the bridge optionally comprising one or both of a double bond and a carbonyl group;Z is selected from the group consisting of hydrogen, halogen, C.sub.1 to C.sub.4 alkyl and C.sub.1 to C.sub.4 alkanoyl;R.sup.1 is selected from the group consisting of: hydrogen; an acyl group; and an inorganic or organic cation;R.sup.2 is selected from the group consisting of: C.sub.1 to c.sub.6 alkyl; C.sub.2 to C.sub.6 alkenyl; C.sub.2 to C.sub.6 haloakenyl; C.sub.2 to C.sub.6 alkynyl; and substituted C.sub.1 to C.sub.
    Type: Grant
    Filed: June 12, 1987
    Date of Patent: December 12, 1989
    Assignee: ICI Australia Limited
    Inventors: Keith G. Watson, Craig G. Lovel
  • Patent number: 4859706
    Abstract: Carboxamides of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.3 -C.sub.10 -cycloalkyenyl or C.sub.4 -C.sub.10 -cycloalkenylalkyl, and R.sup.2 and R.sup.3 are each hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.3 -haloalkyl. C.sub.1 -C.sub.3 -haloalkoxy or methylthio, and their use for combating pests.
    Type: Grant
    Filed: August 6, 1987
    Date of Patent: August 22, 1989
    Assignee: BASF Aktiengesellschaft
    Inventors: Rainer Buerstinghaus, Peter Hofmeister, Christoph Kuenast
  • Patent number: 4855498
    Abstract: Disclosed are platinum (IV) chelates derived from substituted amides. The chelates result from the reaction under mild conditions of potassium chloroplatinate (II) and the appropriate amide. The chelate transdichloro-cis-bis(dimethylacetamide-C,O) was prepared, fully characterized and exemplified in preparation of the antihistamine diphenhydramine hydrochloride.
    Type: Grant
    Filed: February 22, 1988
    Date of Patent: August 8, 1989
    Assignee: University of Delaware
    Inventors: Rosette M. Roat, Seymour Yolles
  • Patent number: 4762548
    Abstract: Herbicidally active thiolcarbamates are employed in combination with a certain amide extender compound, the latter in sufficient quantity to minimize soil degradation and to prolong the soil life of the former. As a result, the herbicidal effectiveness of the thiolcarbamate herbicide is significantly enhanced and prolonged, rendering a single application or multiple applications of the herbicide effective over a longer period of time. Such herbicidal compositions can optionally contain a non-phytotoxic antidotally effective amount of thiolcarbamate herbicide antidote.
    Type: Grant
    Filed: August 12, 1985
    Date of Patent: August 9, 1988
    Assignee: Stauffer Chemical Co.
    Inventors: Reed A. Gray, Ferenc M. Pallos
  • Patent number: 4716175
    Abstract: Certain substituted amides of saturated fatty acids are potent inhibitors of the enzyme acyl-CoA:cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol.
    Type: Grant
    Filed: February 24, 1987
    Date of Patent: December 29, 1987
    Assignee: Warner-Lambert Company
    Inventors: Milton L. Hoefle, Ann Holmes, Bruce D. Roth
  • Patent number: 4686308
    Abstract: Disclosed is a novel physiologically active substance, MH435, represented by the formula: ##STR1## wherein R represents either of the following groups A and B A: --CH.dbd.CH--NHCHOB: --CH.sub.2 --CH.sub.2 --NHCHO.The substance MH435 has an inhibitory activity against tyrosine specific protein kinase, and the 50% inhibitory concentrations of the substances MH435-A and MH435-B are respectively 0.55 .mu.g/ml and 6.0 .mu.g/ml.
    Type: Grant
    Filed: June 26, 1986
    Date of Patent: August 11, 1987
    Assignee: Microbial Chemistry Research Foundation
    Inventors: Hamao Umezawa, Tomio Takeuchi, Masa Hamada, Hiroshi Naganawa, Tsutomu Sawa, Masaya Imoto, Hironobu Iinuma, Takeshi Uchida, Kunio Isshiki
  • Patent number: 4661632
    Abstract: Halogenopropargylformamides of the formula ##STR1## in which R is hydrogen, alkyl, halogenoalkyl, cycloalkyl, halogenoalkyl, cycloalkyl, alkenyl, alkinyl, halogenoalkinyl, optionally substituted aralkyl and optionally substituted aryl, andHal is halogen.which possess fungicidal and bactericidal properties.
    Type: Grant
    Filed: October 31, 1985
    Date of Patent: April 28, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Oeckl, Paul Reinecke, Wilhelm Brandes, Karl-Heinz Kuck, Wilfried Paulus, Hermann Genth
  • Patent number: 4657929
    Abstract: There are provided pharmaceutical compounds useful in treating hypertension, heart diseases and renal failure. These compounds are 4-hydroxy phenethylamines wherein the 3 position on the phenyl nucleus is occupied by either an amino, amide, carbamyl, urea sulfonamide, substituted alkyl or fluorine atom, and the amine group is further linked to another phenyl radical through an alkylene radical which may contain nitrogen, oxygen, sulfur or cyclic hydrocarbon radicals as intervening groups.
    Type: Grant
    Filed: October 18, 1984
    Date of Patent: April 14, 1987
    Assignee: Fisons plc
    Inventors: Francis Ince, Alan C. Tinker
  • Patent number: 4582905
    Abstract: Convenient intermediates for preparing 3-substituted-2-hydroxypropyl aryl ether .beta.-blockers, a reaction to the intermediates of the following formula and a conversion to obtain the said .beta.-blockers are disclosed. ##STR1## (wherein X is hydrogen or halogen; Y is halogen, hydroxy, lower acyloxy, amino, lower alkylamino, lower aralkylamino, lower acylamino, di-lower alkylamino, lower alkyleneamino, N-lower alkyl-N-lower aralkylamino, di-lower acylamino, N-lower alkyl-N-lower acylamino or N-tri-lower alkylsilylamino;one of P and R combined together with Q represents lower alkylene or alkenylene optionally interrupted by O, N or S and optionally substituted by lower alkyl, lower aralkyl, lower carboxylic acyl, carboxy, protected carboxy; hydroxy, lower alkoxy, lower acyloxy, oxo; amino, lower alkylamino, lower acylamino, nitro, nitroso, lower alkylthio, lower sulfonic acyl or halogen;and the remaining R or P is hydrogen or halogen;and dotted line represents the presence of one or two double bonds).
    Type: Grant
    Filed: December 20, 1984
    Date of Patent: April 15, 1986
    Assignee: Shionogi & Co., Ltd.
    Inventor: Makiko Sakai
  • Patent number: 4582918
    Abstract: A novel sequence of highly selective chemical reactions for conversion of 3-Aryl-2-propyn-1-ols into cis-1-Aryl-3-fluoro-1-propene and into D,L-(threo)-1-Aryl-2-acylamido-3-fluoro-1-propanols is disclosed. Preparation of D-(threo)-1-Aryl-2-acylamido-3-fluoro-1-propanol antibacterial agents including the D-(threo)-3-fluoro-3-deoxy derivatives of chloramphenicol and thiamphenicol is also disclosed.
    Type: Grant
    Filed: September 19, 1984
    Date of Patent: April 15, 1986
    Assignee: Schering Corporation
    Inventors: Tattanahali L. Nagabhushan, Stuart W. McCombie
  • Patent number: 4569689
    Abstract: Aniline derivatives of the formula ##STR1## where R.sup.1 is alkoxy, alkylthio, unsubstituted or substituted cycloalkoxy or the radical --NR.sup.2 R.sup.3, X is --CH.sub.2 --, --CH(OH)-- or --CO--, A is an unsubstituted or substituted alkylene chain, B is unsubstituted or substituted methylene or dimethylene, Z is hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy, and n is 1, 2 or 3, are used for controlling undesirable plant growth.
    Type: Grant
    Filed: June 14, 1984
    Date of Patent: February 11, 1986
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulrich Schirmer, Norbert Goetz, Bruno Wuerzer
  • Patent number: 4552981
    Abstract: The present invention is directed to a process for preparing 5-nitro-acet-2,4-xylidine comprising:(a) dissolving acet-2,4-xylidine in an aqueous sulfuric acid solution, said aqueous solution containing from 86 to 92% by weight of sulfuric acid, the weight ratio of sulfuric acid to acet-2,4-xylidine being from 3.5:1 to 6.5:1;(b) nitrating the resultant solution at a temperature of from 0.degree. to 15.degree. C. in a mixed acid containing nitric acid, sulfuric acid, and from 10 to 25% by weight water; and(c) recovering 5-nitro-acet-2,4-xylidine.
    Type: Grant
    Filed: November 27, 1981
    Date of Patent: November 12, 1985
    Assignee: Mobay Chemical Corporation
    Inventors: Karl W. Thiem, Daniel P. Vanderpool
  • Patent number: 4543424
    Abstract: In the process of preparing substituted formamides by the catalytic oxidation of substituted tertiary amines, in which a metal halide catalyst is used in conjunction with an alkali metal halide corrosion inhibitor, pitting of equipment can be inhibited by including in the reaction medium a primary alkylamine, urea or a substituted urea, or thiourea or a substituted thiourea.
    Type: Grant
    Filed: April 9, 1984
    Date of Patent: September 24, 1985
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Harold E. Bellis
  • Patent number: 4540817
    Abstract: A process for the preparation of 5-amino-2,4-dimethylacetanilide by reduction of 5-nitro-2,4-dimethylacetanilide with hydrogen is disclosed characterized in that a crude mixture containing 5-nitro-2,4-dimethylacetanilide in admixture with at least one of its position isomers is hydrogenated in a water-miscible organic solvent which optionally contains water. The 5-amino-2,4-dimethylacetanilide is separated off from the reaction mixture by means of crystallization employing a mixture of water-miscible organic solvent and water.
    Type: Grant
    Filed: July 25, 1983
    Date of Patent: September 10, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Horst Behre, Heinz U. Blank, Alfred Seyberlich, Ferdinand Hagedorn
  • Patent number: 4535186
    Abstract: This invention provides a group of hydroxycycloalkanephenethyl amine antidepressant derivatives of the following structural formula: ##STR1## in which A is a moiety of the formula ##STR2## where the dotted line represents optional unsaturation;R.sub.1 is hydrogen or alkyl;R.sub.2 is alkyl;R.sub.4 is hydrogen, alkyl, formyl or alkanoyl;R.sub.5 and R.sub.6 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, trifluoromethyl or, taken together, methylenedioxy;R.sub.7 is hydrogen or alkyl; andn is 0, 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 26, 1983
    Date of Patent: August 13, 1985
    Assignee: American Home Products Corporation
    Inventors: G. E. Morris Husbands, John P. Yardley, Eric A. Muth
  • Patent number: 4532349
    Abstract: A method of modulating the immune response system in a warm-blooded animal by the administration of N-substituted-phenylthioanilines, N-substituted-phenylsulfinylanilines, and N-substituted-phenylsulfonylanilines, certain of which are new compounds.
    Type: Grant
    Filed: June 3, 1983
    Date of Patent: July 30, 1985
    Assignee: American Cyanamid Company
    Inventors: Stanley A. Lang, Jr., Thomas L. Fields, Raymond G. Wilkinson, Soon M. Kang, Yang-I Lin
  • Patent number: 4521243
    Abstract: A compound having the following structural formula ##STR1## wherein R is nitro, chlorine or hydroxy, preferably nitro; R.sup.1 is C.sub.1 -C.sub.4 alkyl, preferably cyclopropyl or ethyl or alkylthio, preferably methylthio; and R.sup.2 is hydrogen or chlorine.
    Type: Grant
    Filed: December 15, 1983
    Date of Patent: June 4, 1985
    Assignee: Stauffer Chemical Company
    Inventors: Don R. Baker, Teresa M. Tam
  • Patent number: 4508735
    Abstract: 9-(N-alkanoylaminoalkyl)-fluorenes are anti-arrhythmic agents.
    Type: Grant
    Filed: September 21, 1983
    Date of Patent: April 2, 1985
    Assignee: Eli Lilly and Company
    Inventors: William B. Lacefield, Terry D. Lindstrom
  • Patent number: 4473586
    Abstract: Disclosed herein are 1-aminoalkyl-3,4-dihydronaphthalenes represented by the formula ##STR1## wherein n is 1 or 2; R, R.sub.1, and R.sub.2 are independently selected from hydrogen, hydroxy, loweralkoxy of 1 to 3 carbon atoms, loweralkenyloxy of 1 to 3 carbon atoms, thiomethyl, halo, or ##STR2## wherein R.sub.5 and R.sub.6 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula ##STR3## wherein R.sub.7 is loweralkyl of 1 to 4 carbon atoms; or R and R.sub.1, or R.sub.1 and R.sub.2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R.sub.1 or R.sub.2 must be other than hydrogen; and R.sub.3 and R.sub.4 are independently selected from hydrogen; loweralkyl of 1 to 4 carbon atoms; halo-substituted loweralkyl of 1 to 4 carbon atoms; arylalkyl of the formula ##STR4## wherein m is 0, 1 or 2, p is 0 or 1, R.sub.8 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R.sub.9 and R.sub.
    Type: Grant
    Filed: May 3, 1982
    Date of Patent: September 25, 1984
    Assignee: Abbott Laboratories
    Inventors: John F. Debernardis, David L. Arendsen, Martin Winn
  • Patent number: 4460399
    Abstract: N-(2-[4-(4-trifluoromethylphenoxy)-phenoxy]propyl)-N-methylformamide. The base compound is prepared via formylation of the corresponding amine intermediate. The compounds are useful as fungicides, herbicides and plant-growth regulators and especially as cotton defoliants or desiccants.
    Type: Grant
    Filed: January 26, 1982
    Date of Patent: July 17, 1984
    Assignee: Chevron Research Company
    Inventor: David C. K. Chan
  • Patent number: 4448991
    Abstract: Cyclohexenes of the formula ##STR1## wherein R.sup.1 is hydroxy or lower alkoxy; n is 1 or 2; R.sup.2 is lower alkyl; and R.sup.3 is hydrogen, lower alkyl, lower alkenyl or lower cycloalkylmethyl,and their pharmaceutically acceptable acid addition salts are disclosed. The compounds of formula I have analgesic activity and are useful for the control of pains.
    Type: Grant
    Filed: March 24, 1982
    Date of Patent: May 15, 1984
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Albert E. Fischli, Rudolf Pfister
  • Patent number: 4374067
    Abstract: The invention relates to compounds of the formula ##STR1## where Y is --OH; halogen; ##STR2## R.sub.1 SO.sub.3 --, where R.sub.1 is a straight chain or branched chain alkyl group having 1 to 5 carbon atoms, or aryl; and R.sub.2 is --C(CH.sub.3).sub.3 or --O--C(CH.sub.3).sub.3. Processes for preparing the compounds are provided. The compounds are useful as intermediates in the preparation of 4-phenyl-1,3-benzodiazepins, which exhibit activity as antidepressants, analgetics and anticonvulsants.
    Type: Grant
    Filed: December 23, 1981
    Date of Patent: February 15, 1983
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Thomas B. K. Lee, George E. Lee