The Chain Consists Of Two Or More Carbons Which Are Unsubstituted Or Have Acyclic Hydrocarbyl Substituents Only Patents (Class 564/374)
  • Patent number: 5225595
    Abstract: Sulfonyl compounds of the formula ##STR1## where Ar is the radical of a benzene or naphthalene ring,R.sup.1 and R.sup.2 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.4 -alkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, cyano, halogen or hydroxysulfonyl,R.sup.3 is nitro, amino, C.sub.1 -C.sub.4 -alkanoylamino or benzoylamino, andR.sup.4 is a radical of the formula ##STR2## where X.sup.1, X.sup.2 and X.sup.3 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl or substituted or unsubstituted phenyl, andX.sup.4 is a group which is detachable under alkaline conditions,either in the free form or in the form of their salts, are useful for synthesizing reactive dyes.
    Type: Grant
    Filed: November 4, 1992
    Date of Patent: July 6, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Siegel, Claus Marschner, Manfred Patsch
  • Patent number: 5220066
    Abstract: This invention provides a process for directly preparing arylethylamines and their salts from (.alpha.-halo-.alpha.-oximino)acetophenones. The process involves hydrogenation in presence of a transition metal catalyst. The process is illustrated by conversion of 4-hydroxy-(.alpha.-chloro-.alpha.
    Type: Grant
    Filed: March 30, 1992
    Date of Patent: June 15, 1993
    Assignee: Hoechst Celanese Corporation
    Inventors: Ahmed Tafesh, B. Frank Wood, Joseph A. McDonough, Graham N. Mott
  • Patent number: 5220067
    Abstract: This invention provides a process for directly preparing hydrohalide salts of arylethylamines from (.alpha.-chloro-.alpha.-oximino)acetophenones. The process involves hydrogenation in presence of a transition metal catalyst in an organic acid in substantial absence of moisture. The process is illustrated by conversion of 4-hydroxy (.alpha.-chloro-.alpha.
    Type: Grant
    Filed: March 30, 1992
    Date of Patent: June 15, 1993
    Assignee: Hoechst Celanese Corporation
    Inventors: Ahmed Tafesh, B. Frank Wood, Joseph A. McDonough, Graham N. Mott
  • Patent number: 5214156
    Abstract: This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of the formula ##STR1## wherein YR.sub.1 is OR.sub.1 at the 8 position where R.sub.1 is --CH.sub.2 --(C.sub.3-8 cycloalkyl);R.sub.2 is hydrogen or C.sub.1-3 alkyl;R.sub.3 is --CH.sub.2 --(C.sub.3-8 cycloalkyl);R.sub.4 is hydrogen, C.sub.1-8 alkyl, --CH.sub.2 --(C.sub.3-4 cycloalkyl), --(CH.sub.2).sub.m --R.sub.5 or --CH.sub.2 --CH.sub.2 --X--(CH.sub.2).sub.n CH.sub.3 ; n is zero to 3 and m is 2 or 3; X is oxygen or sulfur;R.sub.5 is phenyl, C.sub.1-3 alkoxy, C.sub.1-3 alkyl, 2-thiophene, 3-thiophene, or phenyl substituted with one or two substituent groups selected from chlorine, bromine or fluorine; and with the proviso that when R.sub.3 contains more than four carbon atoms and R.sub.4 is alkyl, said alkyl contains from 1 to 3 carbon atoms.Alternatively, --YR.sub.1 is --S--(C.sub.1-3 alkyl) at the 5, 6, 7 or 8 position of the aromatic ring or OR.sub.1 at the 8 position where R.sub.
    Type: Grant
    Filed: April 10, 1992
    Date of Patent: May 25, 1993
    Assignee: The Upjohn Company
    Inventors: Bengt R. Andersson, Per Arvid E. Carlsson, Kjell A. I. Svensson, Hakan V. Wikstrom
  • Patent number: 5200561
    Abstract: Disclosed is a process for producing an optically active amine represented by the formula (IV) ##STR1## wherein R.sub.7 and R.sub.8 each denote an alkyl group, aryl group or aralkyl group, providing that they do not denote the same group at the same time, and * indicates an asymmetric carbon atom, which comprises reacting an asymmetric reducing agent obtained from (1) an optically active amine derivative represented by the formula (I) ##STR2## wherein R.sub.1 denotes an alkyl group, aryl group or aralkyl group; R.sub.2 denotes a hydrogen atom, alkyl group or aralkyl group; R.sub.3 denotes an aryl group or a substituent represented by the formula (II) ##STR3## wherein R.sub.4 and R.sub.5 each denote a hydrogen atom, aryl group or aralkyl group, and * is as defined above, (2) a metal borohydride and (3) sulfuric acid, with either the syn-isomer or the anti-isomer of an oxime derivative represented by the formula (III) or with a mixture rich in either one of the two isomers ##STR4## wherein R.sub.
    Type: Grant
    Filed: October 7, 1991
    Date of Patent: April 6, 1993
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Naoto Konya, Yukio Yoneyoshi, Yoji Sakito, Shinji Nishii, Gohfu Suzukamo, Hiroko Sakane
  • Patent number: 5198587
    Abstract: Phenethylamine derivatives shown by the general formula ##STR1## wherein Ro represents a lower alkyl group; R.sub.1 represents a lower alkyl group or a lower alkoxy group; R.sub.2 represents hydrogen atom or a hydroxyl group; R.sub.3 and R.sub.4 each represents hydrogen atom or a lower alkyl group; R.sub.5 represents hydrogen atom or a lower alkoxy group; X represents oxygen atom or a methylene group; m is an integer of 1-3; and n is an integer of 0-2 and the acid addition salts thereof.These compounds exhibit a strong .alpha.-adrenergic blocking action and are useful as an antihypertensive agent.
    Type: Grant
    Filed: July 30, 1991
    Date of Patent: March 30, 1993
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kazuo Imai, Kunihiro Niigata, Takashi Fujikura, Shinichi Hashimoto, Toichi Takenaka, Kazuo Honda
  • Patent number: 5196454
    Abstract: The invention relates to novel 2,5-diaminotetralines of the formula: ##STR1## wherein R1, R2, R3 and R4 are defined herein, processes for preparing them and their use in pharmaceutical compositions. The novel 2,5-diaminotetralines are useful in treating diseases caused by disorders of the dopaminergic systems.
    Type: Grant
    Filed: June 15, 1990
    Date of Patent: March 23, 1993
    Assignee: Boehringer Ingelheim KG
    Inventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
  • Patent number: 5189065
    Abstract: The use of products of formula (I) is described, wherein X and Y represent hydrogen, hydroxy or alkoxy; and R.sub.1 and R.sub.2 represent H, alkyl, alkenyl or alkynyl, arylalkyl, acyl or R.sub.1 and R.sub.2 together with nitrogen form a heterocycle for preparing an antitumoral drug.
    Type: Grant
    Filed: October 17, 1991
    Date of Patent: February 23, 1993
    Assignee: Roussel Uclaf
    Inventors: Jorg Czech, Hans H. Sedlacek, Lucien Nedelec, Jacques Guillaume, Christian Marchandeau
  • Patent number: 5175368
    Abstract: Arylalkylamines (as the hydrochloride salt), e.g. tyramine hydrochloride, are prepared by hydrogenating substituted or unsubstituted aryl-.alpha.-oximinoalkyl ketones, e.g. p-hydroxyisonitroacetophenone, in either in an aqueous reaction medium comprising hydrochloric acid, essentially without the presence of a lower alkyl alcohol in said reaction medium, or in an aqueous reaction medium comprising water, hydrochloric acid, and a lower alkyl alcohol, wherein the alcohol comprises less than about 90% by volume of the reaction medium. A substituent on the aryl portion of the aryl-.alpha.-oximinoalkyl ketone must be on a position which activates the aromatic ring.
    Type: Grant
    Filed: June 29, 1992
    Date of Patent: December 29, 1992
    Assignee: Hoechst Celanese Corporation
    Inventors: Ahmed M. Tafesh, Joseph A. McDonough, Graham N. Mott
  • Patent number: 5166438
    Abstract: A charge transporting material comprising a 1,3-pentadiene derivative having formula (I):A--CH.dbd.CH--CH.dbd.CH--CH.sub.2 --A (I)wherein A represents a 9-anthryl group which may have a substituent, a N-substituted carbazolyl group which may have a substituent, a N-substituted phenothiazinyl group which may have a substituent or ##STR1## in which Ar represents an arylene group which may have a substituent, R.sup.1 and R.sup.2 each represent an alkyl group which may have a substituent, an aralkyl group which may have a substituent, or an aryl group which may have a substituent; an electrophotographic photoconductor comprising an electroconductive support and a photoconductive layer formed thereon, which comprises as an effective component at least one of the 1,3-pentadiene derivatives of the above formula (I); and novel 1,3-pentadiene derivatives of the formula (I), provided that in the formula (I), R.sup.1 and R.sup.2 cannot be a methyl group at the same time, are disclosed.
    Type: Grant
    Filed: August 23, 1991
    Date of Patent: November 24, 1992
    Assignees: Ricoh Company, Ltd., Hodogaya Chemical Co., Ltd.
    Inventors: Mitsuru Hashimoto, Masaomi Sasaki, Tomoyuki Shimada, Nobuo Suzuki, Takayuki Sakai, Susumu Suzuka
  • Patent number: 5155274
    Abstract: New complexes of the elements of Groups VIIA, VIIIA, and IB of the Periodic Table* with the trisodium salt of tris(m-sulfophenyl)phosphane as a complex ligand. The complexes are used as catalysts for hydrogenations for the water gas reactions, hydrocarbonyls, hydroformylations, oxidations, carbon-carbon cross-linking reactions (e.g. allene/alkine coupling), and additions of secondary amines to carbon-carbon double bonds.
    Type: Grant
    Filed: January 21, 1992
    Date of Patent: October 13, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang A. Herrmann, Jurgen Kulpe, Jurgen Kellner, Herbert Riepl
  • Patent number: 5141962
    Abstract: A compound selected from the group consisting of N-pentyl-N-phenethyl-3-hydroxyphenethylamine of the formula ##STR1## and its non-toxic, pharmaceutically acceptable acid addition salts having a remarkably dissociated antagonist affinity for kappa opiate receptor.
    Type: Grant
    Filed: April 27, 1990
    Date of Patent: August 25, 1992
    Assignee: Roussel Uclaf
    Inventors: Philippe Cosquer, Francoise Delevallee, Serge Droux, Michel Fortin, Francis Petit
  • Patent number: 5099019
    Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
    Type: Grant
    Filed: August 8, 1988
    Date of Patent: March 24, 1992
    Assignee: Upjohn Company
    Inventors: John M. McCall, Donald E. Ayer, E. Jonathan Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
  • Patent number: 5087753
    Abstract: Process for recovering .alpha.-aminoalcohols by extraction from aqueous solutions, in which process an aromatic aldehyde is added at elevated pH to an aqueous solution of an aminoalcohol in an at least equimolar amount in respect of the aminoalcohol, the resulting mixture is converted with formation of the Schiff base of the aldehyde and the aminoalcohol and the aqueous solution is subsequently extracted using a water-immiscible organic solvent, upon which the Schiff base in the resulting extract is hydrolized and the .alpha.-aminoalcohol or a salt thereof is recovered.
    Type: Grant
    Filed: September 19, 1990
    Date of Patent: February 11, 1992
    Assignee: Stamicarbon B.V.
    Inventors: Wilhelmus H. J. Boesten, Catharina H. M. Schepers, Mathieu J. A. Roberts
  • Patent number: 5073648
    Abstract: This invention relates to an optically active (+)-secondary amine of the formula: ##STR1## wherein R.sup.1 is a lower alkyl, and to a process for preparing a useful intermediate for the production of the optically active dopamine derivatives, namely, optically active (+)-primary amine of the formula: ##STR2## wherein R.sup.1 is a lower alkyl, characterized by the reduction of said optically active (+)-secondary amine.
    Type: Grant
    Filed: January 25, 1991
    Date of Patent: December 17, 1991
    Assignee: Shionogi & Co., Ltd.
    Inventors: Sanji Hagishita, Kaoru Seno
  • Patent number: 5057624
    Abstract: New process for the synthesis of the N-methyl-3,4-dimetoxyphenylethylamine of formula ##STR1## intermediate in the synthesis of the drug internationally known as verapamil. The process starts from the 3,4-dimethoxybenzaldehyde which, by means of a Darzens condensation, gives an epoxyester that, by alkaline hydrolysis and subsequent decarboxylation, gives the 3,4-dimethoxyphenylacetaldehyde. This aldehyde gives the amine of formula I by reaction with monomethylamine followed by reduction with sodium borohydride.
    Type: Grant
    Filed: March 30, 1990
    Date of Patent: October 15, 1991
    Assignee: ALFA Wassermann S.p.A.
    Inventors: Vincenzo Cannata, Giancarlo Tamerlani, Graziano Zagnoni
  • Patent number: 5057623
    Abstract: An organic fluorine compound represented by the general formulaR.sub.f -(X).sub.h -R-Mwherein R.sub.f is a group selected from the following (a) and (b); ##STR1## X denotes a linking group selected from --O--, --S--, and --COO--, h denotes 0 or 1, R is a hydrocarbon chain comprising a phenylene group having an alkylene group with a total carbon number of 10 or more, or the derivative thereof, or an aliphatic alkylene group of a carbon number of 10 or more, and M is a group selected from --OH, --COOH, --SH, and --CONH.sub.2.The organic fluorine compound of the present invention greatly improves the dispersibility of magnetic powders in magnetic coating materials, has also an excellent rust prevention effect on metallic magnetic powders, and exhibits a marked dispersing effect even on fluorocarbon resin fine powders, which can be difficultly dispersed with conventional dispersing agents.
    Type: Grant
    Filed: October 13, 1989
    Date of Patent: October 15, 1991
    Assignee: Matsushita Electric Industrial Co., Ltd.
    Inventors: Yoshiaki Kai, Takashi Suzuki
  • Patent number: 5051409
    Abstract: 2-Aminodecalin derivatives of the formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are H or methyl,A is H, OH, O-alkylcarbonyl, O-benzoyl or O-CH.sub.3,R.sup.4 is H, cyclopropyl, alkyl, alkenyl, or alkynyl,R.sup.5 is alkyl, alkenyl or alkynyl which is substituted or unsubstituted,cycloalkyl or cycloalkenyl whic is substituted or unsubstituted, substituted phenylalkyl, substituted cycloalkyl-alkyl, substituted 5-membered heterocyclic ring, bicycloalkyl-alkyl orR.sup.4 and R.sup.5, together with the nitrogen atom, are a substituted or unsubstituted, saturated or unsaturated piperidine radical,their plant-tolerated salts and N-oxides, and fungicides containing these compounds.
    Type: Grant
    Filed: November 1, 1989
    Date of Patent: September 24, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Zipplies, Bernhard Zipperer, Hubert Sauter, Norbert Goetz, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5047592
    Abstract: A relatively simple, economical process for the synthesis of epinine and related compounds is described. The process involves subjecting adrenalone, epinephrine or their respective congeners to selective hydrogenolysis using hydrogen and a metal hydrogenolysis catalyst such as palladium, platinum, rhodium or nickel. Preferably the reaction is conducted in a non-oxidizing acidic liquid reaction medium, such as in aqueous hydrochloric acid.
    Type: Grant
    Filed: August 21, 1989
    Date of Patent: September 10, 1991
    Assignee: Ethyl Corporation
    Inventor: Joel F. Carpenter
  • Patent number: 5041669
    Abstract: Arylalkylamines (as a sulfate salt) e.g. tyramine sulfate, are prepared by reacting substituted or unsubstituted arylalkylketones with a lower alkylnitrite in the presence of hydrogen chloride in a dipolar aprotic solvent, then combining the reaction mixture with water and extracting it with a lower alkyl ester or alcohol to recover an aryl-.alpha.-oximinoalkylketone extract. The extract, combined with a supported hydrogenation catalyst (e.g. palladium on carbon) in a nonaqueous reaction medium of a major proportion of a mildly protic carboxylic acid (e.g. acetic acid) and a minor proportion of a strong inorganic acid (e.g. sulfuric acid), which is effective in the presence of the catalyst for secondary alcohol dehydration and active as an absorbant for water produced in the dehydration reaction, is hydrogenated to produce the arylalkylamine sulfate sale.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: August 20, 1991
    Assignee: Hoechst Celanese Corporation
    Inventors: Ahmed M. Tafesh, Graham M. Mott
  • Patent number: 5032616
    Abstract: 4-trans-substituted cyclohexylamine derivatives of the formula ##STR1## where R.sup.1 is the group CR.sup.5 R.sup.6 R.sup.7, in which R.sup.5, R.sup.6 and R.sup.7 are hydrogen, unsubstituted or substituted alkyl, alkoxy, alkylthio or cycloalkyl, with the proviso that not more than one of the substituents R.sup.5, R.sup.6 and R.sup.7 may by hydrogen, or in which R.sup.6 and R.sup.7 together with the included carbon atom form a three-membered to six-membered carbocyclic aliphatic ring,R.sup.2 and R.sup.3 are hydrogen, alkyl, alkenyl or alkynyl or cycloalkyl or cycloalkenyl, which in turn may be substituted, with the proviso that the sum of the carbon atoms and hetero atoms (O, S and halogen) of R.sup.2 and R.sup.3 together is not less than 8,R.sup.4 is hydrogen, alkyl, cycloalkyl or alkoxy, and m is 1 to 4, and the bond is a single or a double bond,salts thereof, and their use as fungicides.
    Type: Grant
    Filed: August 28, 1987
    Date of Patent: July 16, 1991
    Inventors: Hubert Sauter, Matthias Zipplies, Norbert Goetz, Eberhard Ammermann, Ernst-Heinrich Pommer
  • Patent number: 5011996
    Abstract: Reaction products of oxo compounds and amines or ammonia, in which at least one substituent is aromatic and monosubstituted to trisubstituted by halogen, can be catalytically hydrogenated to the respective amines, the halogen essentially being completely retained if an Ni-containing or Co-containing catalyst is employed and the reaction is carried out in the presence of organic sulphur compounds.
    Type: Grant
    Filed: July 5, 1989
    Date of Patent: April 30, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Kiel, Heinz Ziemann
  • Patent number: 5006561
    Abstract: Novel 5-alkanesulphonamido-2-[N-(4-alkanesulphonamidophenoxyalkyl)-N-methylamino ]indane and 5-alkanesulphonamido-2-[N-(4-alkanesulphonamidophenyl-alkyl)-N-methylamino ]indane compounds have been prepared, including their pharmaceutically acceptable salts and various key novel intermediates therefor. These compounds are useful in therapy as anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrhythmias. The most preferred member compouned is 5-methanesulphonamido-2-[N-(4-methanesulphonamidophenethyl)-N-methylamino] indane. Methods for preparing these compounds from known starting materials are provided.
    Type: Grant
    Filed: April 17, 1990
    Date of Patent: April 9, 1991
    Assignee: Pfizer Inc.
    Inventors: John E. Arrowsmith, Peter E. Cross
  • Patent number: 4996316
    Abstract: A process for the preparation of tertiary N,N-dimethylamines by the reaction of primary amines, formaldehyde, and hydrogen under pressure and at elevated temperature in the presence of a nickel-containing hydrogenation catalyst in the liquid phase. The hydrogenation catalyst is suspended in a solvent, the nickel concentration is 0.1 to 10% by weight, based on the primary amine. The starting materials are separate from each other, brought to 80.degree. to 150.degree. C. and 1 to 15 MPa and fed into the catalyst suspension simultaneously with stirring and reacted in one step to form the tertiary N,N-dimethylamines.
    Type: Grant
    Filed: December 24, 1988
    Date of Patent: February 26, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jurgen Weber, Detlef Kampmann, Claus Kniep
  • Patent number: 4996235
    Abstract: The present invention provides 3,4-diphenylbutanamines capable of selectively inhibiting the uptake of serotonin and norepinephrine.
    Type: Grant
    Filed: November 25, 1987
    Date of Patent: February 26, 1991
    Assignee: Eli Lilly and Company
    Inventors: David W. Robertson, David T. Wong
  • Patent number: 4990669
    Abstract: The invention relates to new optically active .alpha.-amino aldehydes of the formulae ##STR1## in which R.sub.1 represents an optionally substituted alkyl, alkenyl, aralkyl or aryl radical, andR.sub.2 and R.sub.3, independently of one another, denote an optionally substituted alkyl, alkenyl, cycloalkyl or aralkyl group, together form an optionally substituted phenylene-(1,2)-bis-methylene radical, or R.sub.2 is an optionally substituted, alkyl, cycloalkyl or aralkyl radical, and R.sub.3 forms together with R.sub.1 a 1,3-propylene radical.a process for the preparation thereof, and the use thereof for the stereoselective preparation of optically active .beta.-amino alcohols.
    Type: Grant
    Filed: March 23, 1988
    Date of Patent: February 5, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Manfred T. Reetz, Mark W. Drewes
  • Patent number: 4960939
    Abstract: N-benzyl-N-methyl-3,4-dimethoxyphenethylamine is prepared by reacting 3,4-dimethoxyphenethylamine with a mixture of benzaldehyde and formaldehyde in the presence of hydrogen and a catalyst such as palladium on carbon.
    Type: Grant
    Filed: June 13, 1984
    Date of Patent: October 2, 1990
    Assignee: Farmos-Yhtyma Oy
    Inventor: Maire M. Eloranta
  • Patent number: 4960797
    Abstract: The invention relates to the new N-[2-/4-fluorophenyl/-1-methyl]-ethyl-N-methyl-N-propynyl amine of the Formula I ##STR1## and isomers and salts thereof. The compound of the formula I is useful as a selective MAO inhibitor.
    Type: Grant
    Filed: February 15, 1989
    Date of Patent: October 2, 1990
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Zoltan Ecsery, deceased, Jozsef Knoll, Eva Somfai, Zoltan Torok, Eva Szinnyei, Karoly Mozsolics
  • Patent number: 4959488
    Abstract: Polyfunctional hexasubstituted benzene derivatives wherein at least three of the substituents are saturated carbon chains having from 1 to 21 carbon atoms and functional groups containing hetero functionalities at the ends of the carbon chains and the remainder of the 6 substituents are either saturated carbon chains containing from 1 to 21 carbon atoms or saturated carbon chains containing from 1 to 21 carbon atoms having a functional group including a hetero functional group containing N, O, S, P, or Si at the end of the chains. These derivatives are made by reacting a disubstituted alkyne wherein one or both of the substituents are saturated carbon chains having 1 to 21 carbon atoms to which hetero functional groups are attached with a palladium catalyst and isolating the resulting hexasubstituted benzene derivative.
    Type: Grant
    Filed: May 17, 1989
    Date of Patent: September 25, 1990
    Assignee: Henkel Research Corporation
    Inventors: James M. Renga, Alan G. Olivero, Mark Bosse
  • Patent number: 4956389
    Abstract: Compound of general formula I ##STR1## and its addition salts with a pharmaceutically acceptable acid is described. The compound is prepared by reacting bis-(2-(3,4-dimethoxy-phenyl)ethyl)amine with formaldehyde in a reducing medium. The compound is effective in the treatment of cardiovascular diseases and disturbances in cerebral circulation.
    Type: Grant
    Filed: January 14, 1985
    Date of Patent: September 11, 1990
    Assignees: Yason S.R.L., SIR International S.A.
    Inventors: Giuseppe Quadro, Jean Cahn
  • Patent number: 4914133
    Abstract: Amino compounds of the formula ##STR1## where R.sup.1 is alkyl, A is alkylene or alkenylene, and Ar is aryl, and their acid addition salts, and fungicides containing these compounds.
    Type: Grant
    Filed: April 14, 1988
    Date of Patent: April 3, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Walter Himmele, Hubert Sauter, Hardo Siegel, Eberhard Ammermann, Ernst-Heinrich Pommer
  • Patent number: 4912259
    Abstract: A pentadiene compound of the formula: ##STR1## wherein each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a C.sub.1 -C.sub.4 alkyl group or a substituted or unsubstituted aryl or aralkyl group, R.sub.5 is an alkyl group, and X is a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group or a halogen atom.
    Type: Grant
    Filed: August 5, 1988
    Date of Patent: March 27, 1990
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventors: Kazuo Kaneko, Masahiko Yamaguchi, Michihiro Gonda, Kensaku Okano, Kazuyuki Wakasugi
  • Patent number: 4912258
    Abstract: Fluorinated aniline derivatives of the general formula I are described ##STR1## in which R.sup.1 represents H or (CH.sub.2).sub.n -X, n is a whole number from 1 to 3, X is H, OH, NH.sub.2, CH.sub.3 CONH, CH.sub.3 SO.sub.2 NH, SO.sub.3 H or ArSO.sub.3 H, Ar is optionally substituted arylene radical, R.sup.1 is alternatively also a --(CH.sub.2).sub.3 -- group, which is bonded to the free o-position next to the N-atom, Y is H, --O--, --NH--, --S-- or a C--C single bond, R.sup.2, in the event that Y=H, is the same as or different from R.sup.1 and means one of the radicals shown for R.sup.1, and in the event that Y is a C--C single bond or --O--, --NH-- or --S--, is an alkylene group having 1 to 3 carbon atoms linked with Y, and R.sup.3 =H, alkyl having 1 to 3 carbon atoms, OCH.sub.3, CH.sub.3 CONH, CO.sub.2 H or SO.sub.3 H.
    Type: Grant
    Filed: February 5, 1988
    Date of Patent: March 27, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Hans-Georg Batz, Rupert Herrmann
  • Patent number: 4898986
    Abstract: Disclosed is a novel inosose compound represented by the general formula: ##STR1## wherein X.sup.1 and X.sup.2 are both halogen; X.sup.1 is hydrogen and X.sup.2 is halogen; or X.sup.1 is --SQ.sup.1 and X.sup.2 is --SQ.sup.2 (each of Q.sup.1 and Q.sup.2 is lower alkyl or Q.sup.1 and Q.sup.2 may form lower alkylene), R.sup.1 is a protective group for hydroxyl and Y is .dbd.O, .dbd.N--Z (Z is hydroxyl which may be protected) or ##STR2## (A is hydrogen or an amine residue), particularly to the compound wherein the symbol Y is oxygen.The inosose compound is useful as intermediates for production of valiolamine and the N-substituted derivatives thereof, which have potent .alpha.-glucosidase inhibiting activities and are useful as preventives or therapeutics for symptoms of hyperglycemia and various diseases derived therefrom in human and animals, such as diabetes, obesity and hyperlipemia.
    Type: Grant
    Filed: August 31, 1987
    Date of Patent: February 6, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Satoshi Horii, Hiroshi Fukase
  • Patent number: 4898889
    Abstract: Acetylene compounds of the formula (I): ##STR1## wherein Y, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The compounds possess antihypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.
    Type: Grant
    Filed: March 27, 1989
    Date of Patent: February 6, 1990
    Assignee: McNeilab, Inc.
    Inventor: John R. Carson
  • Patent number: 4897425
    Abstract: Cyclohexylamines of the formula ##STR1## where X is a single bond or an alkylene chain, Y is hydrogen or an aryl, cyclohexyl, 4-cyclohexylcyclohexyl, perhydro-1- or 2-naphthyl or piperidyl radical, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, cycloalkyl, cycloalkenyl or arylalkyl, or R.sup.1 and R.sup.2 together form an alkylene group and, togehter with the N atom, form a ring, and acid addition salts thereof, with the exception of compounds in which X is a single bond, Y is cyclohexyl, R.sup.1 and R.sup.2 are hydrogen or methyl, and the compounds in which X is C.sub.6 -, C.sub.7 - and C.sub.8 -alkyl, Y is hydrogen and R.sup.1 and R.sup.2 together with the N atom whose substituents they are form a 2,6-dimethylmorpholine radical, and fungicides containing such cyclohexylamines.
    Type: Grant
    Filed: November 16, 1987
    Date of Patent: January 30, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernhard Zipperer, Ernst Buschmann, Norbert Goetz, Ulrich Schirmer, Eberhard Ammermann, Ernst-Heinrich Pommer
  • Patent number: 4876284
    Abstract: Compounds of the formula ##STR1## wherein R.sup.3 and the NR.sup.1 R.sup.2 group are in a cis-position to each other and wherein Y is OH, R.sup.4 COO, (R.sup.5).sub.2 NCOO or R.sup.6 O either in position 5 or position 7, whereby R.sup.4 is an alkyl group having 1-5 carbon atoms or a possibly substituted phenyl group, R.sup.5 is an alkyl group having 1-5 carbon atoms and R.sup.6 is an allyl or benzyl group, R.sup.1 is hydrogen or an alkyl group having 1-3 carbon atoms, R.sup.2 is an alkyl group having 1-6 carbon atoms, a phenylalkyl- or m-hydroxyphenylalkyl group with 2-4 carbon atoms in the alkyl part, or an alkenyl group with 3-6 carbon atoms other than 1-alkenyl, and R.sup.3 is an alkyl group having 1-3 carbon atoms, processes and intermediates for their preparation, pharmaceutical preparations and methods of treatment employing such compounds. The compounds are useful for therapeutic purposes, especially for treatment of disorders in the central nervous system.
    Type: Grant
    Filed: January 11, 1988
    Date of Patent: October 24, 1989
    Assignee: Per Arvid Emil Carlsson
    Inventors: Folke L. E. Arvidsson, Per A. E. Carlsson, Uli A. Hacksell, John S. M. Hjorth, Anette M. Johansson, Per L. Lindberg
  • Patent number: 4847303
    Abstract: The present invention involves compounds having the structure: ##STR1## wherein: (a) --A.sup.1 is selected from the group consisting of --OH, --H, and --O.sub.2 CR;(b) --A.sup.2 is selected from the group consisting of unsubstituted or substituted, saturated or unsaturated, straight, branched and cyclic alkyl having from 1 to about 10 carbon atoms;(c)--A.sup.3 is selected from --C(CH.sub.3).sub.3, --Si(CH.sub.3).sub.3, and --CF.sub.3 ; and(d) --Y is selected from certain low molecular weight alkyl chains which terminate in specific unsaturated functional groups: ##STR2## and aldehydes in the form of their acetals; pharmaceutical compositions comprising such compounds; and methods for treating inflammation by administering such compounds.
    Type: Grant
    Filed: November 23, 1987
    Date of Patent: July 11, 1989
    Assignee: The Procter & Gamble Company
    Inventors: Maurice E. Loomans, Randall S. Matthews, Joseph A. Miller
  • Patent number: 4845292
    Abstract: There are disclosed compounds of the formula ##STR1## R is --CH.sub.2 OH or --CO.sub.2 R.sup.3 ; R.sup.1 is hydrogen, lower alkyl, lower alkoxy or hydroxybenzyl;R.sup.2 is hydroxyloweralkyl or diloweralkoxyalkyl;R.sup.3 is hydrogen or lower alkyl;R.sup.4 is alkyl of 10-20 carbons atoms, phenylalkyl of 11-18 carbon atoms or phenoxyalkyl of 11-18 carbon atoms; orn is 1-3;or a pharmaceutically acceptable salt thereof, and their use in the prevention and/or treatment of conditions such as allergic rhinitis, allergic bronchial asthma and other naso-bronchial obstructive air-passageway conditions, other immediate hypersensitivity reactions such as allergic conjunctivitis and various inflammatory conditions.
    Type: Grant
    Filed: January 13, 1988
    Date of Patent: July 4, 1989
    Assignee: American Home Products Corporation
    Inventors: William H. McGregor, Lisa A. Marshall, John H. Musser
  • Patent number: 4814507
    Abstract: A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylkene; Y is -(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.
    Type: Grant
    Filed: September 14, 1987
    Date of Patent: March 21, 1989
    Assignee: Mitsubishi Chemical Industries, Limited
    Inventors: Akihiro Tobe, Shinichiro Fujimori, Tomoshi Yamazaki, Mamoru Sugano, Ryoji Kikumoto, Issei Nitta
  • Patent number: 4803225
    Abstract: There are provided compounds of formula I, ##STR1## and pharmaceutically acceptable derivatives thereof. There are also described the use of the compounds of formula I as pharmaceuticals, methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.
    Type: Grant
    Filed: December 2, 1987
    Date of Patent: February 7, 1989
    Assignee: Fisons, plc
    Inventors: John Dixon, Francis Ince
  • Patent number: 4794197
    Abstract: All-cis-1,3,5-Triamino-2,4,6-trihydroxycyclohexane derivatives corresponding to the general formula I ##STR1## wherein the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are identical or different and represent hydrogen atoms, alkyl groups or --CO-alkyl groups wherein the alkyl in the alkyl or --CO-alkyl group has 1 to 18 carbon atoms and the alkyl and --CO-alkyl groups may contain, independently of one another, one or more identical or different functional groups, and at least one of the groups R.sub.1 to R.sub.6 is one of the above mentioned unsubstituted or substituted alkyl groups or --CO-alkyl groups, and their salts with pharmacologically conventionally used inorganic or organic acids and their quaternary ammonium salts, processes for their preparation and their use, and pharmaceutical preparations containing these compounds.
    Type: Grant
    Filed: January 31, 1986
    Date of Patent: December 27, 1988
    Inventors: Walter Schneider, Isidor Erni, Hans K. Hegetschweiler
  • Patent number: 4792628
    Abstract: Indane derivatives and their salts represented by the general formula (1), ##STR1## wherein R.sup.1 is an amino group which may have lower alkyl groups as the substituents, a hydroxylimino group, an alkanoylamino group having 1 to 10 carbon atoms which may have halogen atoms as the substituents, a lower alkylsulfonylamino group, a phenylsulfonylamino group which may have lower alkyl groups as the substituents on the phenyl ring, a benzoylamino group having lower alkyl groups as the substituents on the phenyl ring, and a phenyl-lower alkylamino group having a hydroxyl groups or a lower alkyl groups as the substituents on the phenyl ring, R.sup.2 is a hydrogen atom, a lower alkyl group, a halogen atom, a nitro group, an amino group, an amino-lower alkyl group, a lower alkanoylamino group, a lower alkanoylamino-lower alkyl group which may have halogen atoms as the substituents, a lower alkylthio group, a 1-piperidinesulfonyl group, or a lower alkenyl group; R.sup.
    Type: Grant
    Filed: April 16, 1987
    Date of Patent: December 20, 1988
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
  • Patent number: 4777294
    Abstract: A compound of the formula: ##STR1## wherein A is a chain hydrocarbon group having 1 to 10 carbon atoms optionally substituted by hydroxyl, phenoxy, thienyl, furyl, pyridyl, cyclohexyl or an optionally substituted phenyl group, or a cyclic hydrocarbon group having 3 to 7 carbon atoms optionally substituted by hydroxyl, B is hydrogen or hydroxyl, and their production and use.These compounds exhibit excellent inhibitory activity against .alpha.-glucoside hydrolase, thus are useful for hyperglycemic symptoms and various disorders caused by hyperglycemia.
    Type: Grant
    Filed: April 17, 1987
    Date of Patent: October 11, 1988
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Satoshi Horii, Yukihiko Kameda, Hiroshi Fukase
  • Patent number: 4772755
    Abstract: A method for synthesizing a tri-substituted phenyl compound (I) by using a 1,2-addition followed by a 1,4-addition to 1,4-benzoquinone (II): ##STR1## wherein X is hydroxy, alkoxy or alkanoyloxy, Ar.sup.1 is an organic group and R is an unsubstituted or substituted alkyl group.
    Type: Grant
    Filed: March 19, 1987
    Date of Patent: September 20, 1988
    Assignee: McNeilab, Inc.
    Inventors: Dennis C. Liotta, Cynthia A. Maryanoff, Vasken Paragamian
  • Patent number: 4725602
    Abstract: Acetylenes of the following formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, R.sup.3, n and R.sup.4 are defined herein and R.sup.5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and antihypertensives.
    Type: Grant
    Filed: October 24, 1985
    Date of Patent: February 16, 1988
    Assignee: McNeilab, Inc.
    Inventor: John R. Carson
  • Patent number: 4720586
    Abstract: There are provided compounds of formula I, ##STR1## in which R.sub.1 represents OH,R.sub.2 and R.sub.3, which may be the same or different, each independently represent hydrogen, fluorine, chlorine, bromine, alkyl C1 to 6, nitro, nitrile, (CH.sub.2).sub.p R.sub.9 or SR.sub.9,W represents a single bond, a 1,2; 1,3; or 1,4-disubstituted benzene ring; a --CH.dbd.CH--group or a 1,4-cyclohexanediyl group;X respresents NH, O, S, SO.sub.2, CO, CH.sub.2, CONH or --COO;Y represents (CH.sub.2)q, CO, CS, SO.sub.2 and R.sub.20 represents hydrogen,or Y represents CR.sub.15 R.sub.16 CR.sub.17 R.sub.18,wherein the carbon atom bearing R.sub.15 and R.sub.16 is adjacent to X and in whichR.sub.15 and R.sub.18, together with the carbon atom to which they are attached form a carbonyl group, and R.sub.15, R.sub.16 and R.sub.20 each represent hydrogen, orR.sub.15 and R.sub.20 together form a chain --CH.sub.2 --, and R.sub.16, R.sub.17 and R.sub.18 each represent hydrogen, orR.sub.15, R.sub.16, R.sub.17 and R.sub.
    Type: Grant
    Filed: October 18, 1984
    Date of Patent: January 19, 1988
    Assignee: Fisons, plc
    Inventors: John Dixon, Francis Ince
  • Patent number: 4720585
    Abstract: Aminopeptidase inhibitory activity is exhibited by compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl, carboxyalkyl, halo-substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl or heteroaryl; andR.sub.2 and R.sub.3 are each independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, aminoalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl.
    Type: Grant
    Filed: September 18, 1985
    Date of Patent: January 19, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jollie D. Godfrey Jr., Eric M. Gordon
  • Patent number: 4709096
    Abstract: Stilbene derivatives of the formula (I) ##STR1## and distyryl derivatives of the formula (II), ##STR2## as defined in the specification, and an electrophotographic photoconductor comprising an electroconductive support material and a photosensitive layer overlayed thereon comprising at least one of the above derivatives, are disclosed.
    Type: Grant
    Filed: February 22, 1985
    Date of Patent: November 24, 1987
    Assignee: Ricoh Company, Ltd.
    Inventor: Masaomi Sasaki
  • Patent number: 4708966
    Abstract: The present invention relates to novel specifically-substituted phenyl compounds, especially substituted di-tert-butyl phenol derivatives, which are effective as anti-inflammatory, analgesic and/or antipyretic agents. These phenyl compounds are substituted with a low molecular weight alkyl chain which terminates in a specific unsaturated functional group. These unsaturated functionalities are --C.tbd.CH, C.dbd.CH.sub.2, C.dbd.C.dbd.CH.sub.2, and aldehydes in the form of their acetals.The present invention further relates to pharmaceutical compositions which contain an anti-inflammatory agent of the present invention and a pharmaceutically-acceptable carrier.Finally, the present invention relates to methods for treating diseases characterized by inflammation, such as rheumatoid arthritis and osteoarthritis, in humans or lower animals.
    Type: Grant
    Filed: June 27, 1986
    Date of Patent: November 24, 1987
    Assignee: The Procter & Gamble Company
    Inventors: Maurice E. Loomans, Randall S. Matthews, Joseph A. Miller