Hydroxy, Bonded Directly To Carbon, Or Ether In Substituent Q (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/170)
  • Patent number: 5130483
    Abstract: Isoprenoid derivatives represented by the general formula (I) ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, X represents --CH.sub.2 --, --O-- or --NH--, n represents number of the double bond in trans-configuration and is 1 or 2, and m is an integer from 0 to 3.The compounds have a 5-lipoxygenase-inhibiting activity and are useful as a therapeutic agent for such diseases as allergy, nephritis, hepatitis, rheumatism and gastric ulcer.
    Type: Grant
    Filed: May 18, 1990
    Date of Patent: July 14, 1992
    Assignee: Terumo Kabushiki Kaisha
    Inventors: Hiroyuki Ohnishi, Shingo Koyama, Ryoichi Nanba, Syozo Miyaoka, Akira Masuda, Yoshiyuki Shikata, Hideto Ushijima, Seiitsu Murota
  • Patent number: 5128488
    Abstract: The asymmetric hydrogenation of carbonyl compounds is carried out in the presence of at least one transition metal complex MZq(M=metal of group VIII of the Periodic Classication; Z=ligand selected among the atoms and the molecules which may complex the metal M; and q=degree of corrdination of M) and of at least one chiral phosphorous-containing ligand having formula (I), wherein R is hydrocarbonated radical (alkyl, cycloalkyl and aryl); R.sup.1 is H, hydrocarbonated radical or PR.sub.2 ; R.sup.2 is H or hydrocarbonated radical R.sup.3,R.sup.4, necessarily different, are H and optionally functionalized hydrocarbonated radicals; R.sup.5 and R.sup.6 are H and optionally functionalized hydrocarbonated radicals; one of the radicals R.sup.3 and R.sup.4 possibly carrying a function - OPR.sub.2 or NPR.sub.2, R.sup.5 and R.sup.6 being in this case H when R.sup.1 is PR.sub.2 ; R.sup.2 and R.sup.3 and the atoms of N and C which cary them respectively forming a heterocycle; or R.sup.2 and R.sup.
    Type: Grant
    Filed: April 27, 1990
    Date of Patent: July 7, 1992
    Assignee: Societe Chimique des Charbonnages S.A.
    Inventors: Andre Mortreux, Francis Petit
  • Patent number: 5116994
    Abstract: Deacylating agent represented by the formula (I): ##STR1## wherein R represents an insoluble polymer substituent, and R' and R" each represents an alkyl group, and a deacylation method using the above deacylating agent.
    Type: Grant
    Filed: April 17, 1990
    Date of Patent: May 26, 1992
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Mitsunori Ono
  • Patent number: 5112868
    Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.
    Type: Grant
    Filed: May 2, 1990
    Date of Patent: May 12, 1992
    Assignee: Warner-Lambert Company
    Inventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
  • Patent number: 5106407
    Abstract: The present invention discloses the antimicrobial utility of certain iodonium ylide compounds. The particular iodonium ylide compounds are phenyl iodonium ylides having an ortho substituent that stabilizes the positive charge on the polyvalent iodine by a nonbonded electrostatic interaction. The polyvalent iodine is further stabilized by a cyclic 1,3-dicarbonyl anion.
    Type: Grant
    Filed: December 4, 1989
    Date of Patent: April 21, 1992
    Assignee: The Dow Chemical Company
    Inventors: Attila G. Relenyi, Gerald F. Koser, Richard W. Walter, Jr., William J. Kruper, Jr., Ravi B. Shankar, Anthony P. Zelinko
  • Patent number: 5079263
    Abstract: R.sup.2 is H or OH;R.sup.3 is H, OH, OCH.sub.3, CH.sub.3 or NH.sub.2 ;Rhu 4 is H, OH, OCH.sub.3, NH.sub.2 or ##STR2## The compounds of the formula I are prepared by fermentation of the strain Streptomyces parvulus DSM 40722 in the presence of substituted benzoic acids of the general formula II ##STR3## where R.sup.1 is H or OH;R.sup.2 is H or OH;R.sup.3 is H, OH, OCH.sub.3, CH.sub.3 or NH.sub.2 ;R.sup.4 is H, OH, OCH.sub.3 or NH.sub.2,and they inhibit Leukocyte elastase and can be used as pharmaceuticals.
    Type: Grant
    Filed: December 2, 1988
    Date of Patent: January 7, 1992
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Axel Zeeck, Ralf Thiericke, Hans Zahner, Gerhard Dickneite, Hans H. Sedlacek
  • Patent number: 5066680
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is aryl which may have one or more suitable substituent(s),R.sup.2 is aryl which may have one or more suitable substituent(s), lower alkyl or cyclo(lower)alkyl,R.sup.3 is hydrogen, hydroxy, halogen, lower alkenyl, amino or protected amino,R.sup.4 is a group of the formula: ##STR2## wherein R.sup.5 is lower alkyl which may have one or more suitable substituent(s), cyclo(lower)alkyl, aryl, ar(lower)alkyl which may have one or more suitable substituent(s), andR.sup.6 is hydrogen or lower alkyl; or N-containing heterocyclic group which may have one or more suitable substituent(s), andA is lower alkylene or lower alkynylene, in which R.sup.1 and R.sup.2 may be linked through oxygen atom, their preparation and use in treatment of dysuria, and starting materials for their preparation.
    Type: Grant
    Filed: February 5, 1990
    Date of Patent: November 19, 1991
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Youichi Shiokawa, Kazuo Okumura, Kazuhiko Take, Kazunori Tsubaki
  • Patent number: 5059624
    Abstract: Guanidine derivatives of the following formulas (1) and (2): ##STR1## wherein: R.sup.1 is hydrogen or optionally substituted cinnamoyl,R.sup.2 is hydrogen, alkyl or alkenyl, with the proviso that R.sup.1 and R.sup.2 cannot be both hydrogen,n is an integer from 1 to 8, or: ##STR2## wherein R.sup.3 is truxinoyl or a truxilloyl each optionally substituted, andR.sup.2 and n are as defined above;pharmaceutical compositions containing such compounds and a process for their extraction and purification from plant material, in particular from Verbesina caracasana.
    Type: Grant
    Filed: February 24, 1989
    Date of Patent: October 22, 1991
    Assignee: Consiglio Nazionale Delle Ricerche
    Inventors: Giuliano D. Monache, Franco D. Monache, Marco Carmignani, Stella C. Bonnevaux, Romulo Espinal, Carlo De Luca, Bruno Botta
  • Patent number: 5059438
    Abstract: Resorcinol derivatives are disclosed as inhibitors of enzymatic browning in foods and beverages such as shrimp, apples, fruit juices and wines.
    Type: Grant
    Filed: June 13, 1990
    Date of Patent: October 22, 1991
    Assignee: Enzytech, Inc.
    Inventors: Arthur J. McEvily, Radha Iyengar, Akiva Gross
  • Patent number: 5047410
    Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.
    Type: Grant
    Filed: July 12, 1989
    Date of Patent: September 10, 1991
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Arturo Donetti, Marco Turconi, Massimo Nicola, Rosamaria Micheletti
  • Patent number: 5041653
    Abstract: A method for sensitizing hypoxic tumor cells to radiation using derivatives of benzamide are disclosed. Some of the compounds useful in the method of the invention are novel.
    Type: Grant
    Filed: September 24, 1990
    Date of Patent: August 20, 1991
    Assignee: SRI International
    Inventors: William W. Lee, Edward W. Grange, J. Martin Brown
  • Patent number: 5037837
    Abstract: Novel phenoxypropylamine derivative having the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 represent a hydrogen atom, a hydroxy group, a lower alkyl group or a lower alkoxy group, and R.sub.3 and R.sub.4 represent a lower alkyl group, or R.sub.3 and R.sub.4 taken together represent a group having the formula (CH.sub.2).sub.m wherein m represents 4 or 5, and n represents an integer of from 2 to 6 or a pharmaceutically acceptable salt thereof.The compounds are useful as a 5-lipoxygenase inhibitor and an antiulcer agent.
    Type: Grant
    Filed: November 1, 1990
    Date of Patent: August 6, 1991
    Assignee: Terumo Kabushiki Kaisha
    Inventors: Yoshiyuki Shikata, Ryoichi Nanba, Isamu Endo, Masashi Isozaki, Tadashi Okumura, Masazumi Miyakoshi, Shingo Koyama
  • Patent number: 5013759
    Abstract: Substituted phenylacetic acid amide compounds, and pharmaceutically-acceptable salts thereof, of the formula: ##STR1## wherein X is O or S; R.sub.1 is H, OH or CH.sub.3 ; R.sub.2 is straight chain alkenyl, branched chain or cyclic hydrocarbon having from about 7 to about 24 carbon atoms; R.sub.3 is OH, OSO.sub.3.sup.-, OPO.sub.3.sup.-- or a short chain ester with from about 1 to about 6 carbon atoms.
    Type: Grant
    Filed: January 31, 1990
    Date of Patent: May 7, 1991
    Assignee: The Procter & Gamble Company
    Inventors: Elizabeth F. Berman, Brian L. Buckwalter, Thomas L. Cupps, Joseph H. Gardner
  • Patent number: 5001261
    Abstract: Cyclohexenone derivatives of the formula ##STR1## where R.sup.1, R.sup.2 R.sup.3, R.sup.4 and R.sup.5 have the meanings given in the disclosure, and their use for controlling unwanted plant growth.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: March 19, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Michael Keil, Rainer Becker, Dieter Jahn, Norbert Goetz, Ulrich Schirmer, Bruno Wuerzer
  • Patent number: 4978523
    Abstract: A melanin inhibitor comprising as the reactive component a cinnamic acid derivative of the formula (I) or (II): ##STR1## in which R' represents an acyl group having 2 to 6 carbon atoms, R.sub.1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a cycloalkyl group or an alkenyl group, and R.sub.2 represents a hydrogen atom, an alkyl group having 1 to 24 carbon atoms, a cycloalkyl group or an alkenyl group.The melanin inhibitors according to the invention are locally applied to affected portions such as of freckles and pigmentary deposits after sunburn without giving any stimulative or allergic troubles to the skin.
    Type: Grant
    Filed: December 24, 1985
    Date of Patent: December 18, 1990
    Assignee: Kao Corporation
    Inventors: Itsuro Motegi, Michio Kawai, Genji Imokawa, Koichi Nakamura, Naotake Takaishi
  • Patent number: 4971997
    Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, or --CH.dbd.CH--;wherein Z is OR.sup.1 or --NR.sup.4 R.sup.5 ;wherein R.sup.1 is hydrogen, lower alkyl, or a pharmaceutically acceptable cation;wherein R.sup.2 is H, --CH.sub.3 or --C.sub.2 H.sub.5 ;wherein R.sup.3 is OH, H or .dbd.O;wherein R.sup.4 and R.sup.5 may independently be hydrogen, or lower alkyl having 1-6 carbon atoms, or R.sup.4 and R.sup.5 may act together with N to form a cyclic amide of the formula: ##STR2## wherein n is an integer from 4-5; and m is an integer from 0-4. More particularly, this invention relates to compounds of the above formula which have utility as LTB.sub.4 antagonists.
    Type: Grant
    Filed: August 7, 1989
    Date of Patent: November 20, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Richard A. Haack, Stella S. Yu
  • Patent number: 4943652
    Abstract: There is disclosed a process for asymmetrically reducing a carbonyl compound, which comprises reducing the carbonyl compound by the use of a reducing agent comprising (i) an optically active tartaric acid or ester thereof and (ii) a metal borohydride, thereby producing an optically active hydroxyl compound. The process can be used for the production of optically active hydroxyesters and alcohols from ketoesters and ketones. These products are useful for the production of medicaments and liquid crystals.
    Type: Grant
    Filed: November 14, 1988
    Date of Patent: July 24, 1990
    Assignee: Ajinomoto Co., Inc.
    Inventors: Masanobu Yatagai, Takashi Ohnuki
  • Patent number: 4931471
    Abstract: Derivatives with amide function obtained by reaction between derivatives of linear, branched or cyclic amines having an amino acid or peptidic structure and paramethoxycinnamic acid or urocanic acid. Application of said compounds as specific solar filter, absorbing about 310 nm and avoiding erythematous phenomena during exposures to the sun and as active principles of dermo-pharmaceutical and cosmetological preparations.
    Type: Grant
    Filed: October 3, 1988
    Date of Patent: June 5, 1990
    Assignee: Universite Louis Pasteur
    Inventors: Louis Jung, Dominique Robert
  • Patent number: 4904815
    Abstract: New phenols are described containing an alkyl substituent containing a functional group; as well as a process for the production of such phenols. The new phenols are useful e.g. as stabilizers in organic or aqueous systems.
    Type: Grant
    Filed: October 13, 1987
    Date of Patent: February 27, 1990
    Assignee: Ciba-Geigy AG
    Inventor: Frederick H. Howell
  • Patent number: 4904661
    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 16, 1987
    Date of Patent: February 27, 1990
    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: 4882329
    Abstract: Calcium antagonists of the formula ##STR1## with R(1), R(2), R(3) and R(4) being, inter alia, H, alkyl, alkoxy, halogen, in some cases phenyl; m being 1-4; n being 0-3; X being CH.sub.2, O, S, CO, CHOH or CR.sub.2, and R(5) being various groups containing nitrogen atoms, are described.They are obtained by reaction of compounds II which are likewise new and which contain in place of R(5) a leaving group Y (Cl, Br, I) with the appropriate (cyclic) amino compound.Another synthesis comprises reaction of the appropriate indolinone derivative IV which has a non-etherified hydroxyl group with a side chain which contains a terminal leaving group Z (Cl, Br, I) in the presence of a base.Furthermore, indolinone derivatives VI with an ether side chain with a terminal epoxide group can be reacted with (cyclic) amines to give compounds I.
    Type: Grant
    Filed: January 30, 1989
    Date of Patent: November 21, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Lerch, Rainer Henning, Joachim Kaiser
  • Patent number: 4880839
    Abstract: An acylanilide of the formula: ##STR1## wherein R.sup.1 or R.sup.2 which may be the same or different, each is an electron-withdrawing substituent, alkylthio or phenylthio or R.sup.1 is hydrogen, alkyl or alkoxy; wherein R.sup.3 is hydrogen or halogen; wherein R.sup.4 is hydrogen or acyl wherein A is branched-chain alkylene; and wherein R.sup.5 is phenyl, substituted phenyl or naphthyl. The compounds possess progestational activity.
    Type: Grant
    Filed: June 16, 1987
    Date of Patent: November 14, 1989
    Assignee: Imperial Chemical Industries PLC
    Inventor: Howard Tucker
  • Patent number: 4876269
    Abstract: Benzo-fused cycloalkane and oxa- and thia-cycloalkane trans-1,2-diamine compounds of the formula: ##STR1## wherein A, B, C, D, n, X, Y, R, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, e.g., trans-3,4-dichloro-N-methyl-N-[2-(pyrrolidin-1-yl)-5-methoxy-1,2,3,4-tetra hydronaphth-1-yl]benzeneacetamide, and the pharmaceutically acceptable salts of N-oxides thereof, are useful as analgesics and/or diuretics.
    Type: Grant
    Filed: July 16, 1987
    Date of Patent: October 24, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Penio Pennev, Parthasarathi Rajagopalan, Richard M. Scribner
  • Patent number: 4876084
    Abstract: A novel melanin inhibitor comprising as an active component a p-hydroxycinnamamide derivative of the following general formula (I) ##STR1## in which R.sub.1 represents a hydrogen atom or a 2-hydroxyethyl group, and R.sub.2 represents a hydroxymethyl group or a carboxyl group.The melanin inhibitor may take various forms such as a lotion, an emulsion, a cream, an ointment, a gel and the like, and it is locally applied onto affected parts such as spots and freckles on the skin, and a pigmental deposition after sunburn.
    Type: Grant
    Filed: July 23, 1987
    Date of Patent: October 24, 1989
    Assignee: Kao Corporation
    Inventors: Kimihiko Hori, Koichi Nakamura, Michio Kawai, Itsuro Motegi, Genji Imokawa, Naotake Takaishi
  • Patent number: 4873338
    Abstract: Compounds corresponding to Formula I ##STR1## wherein R.sup.1 denotes an acyl group andX denotes hydrogen, halogen, alkoxy, aroxy, SO.sub.3 H or a heterocyclic group attached through --O-- or --N<are prepared form a compound corresponding to Formula II ##STR2## wherein X has the meaning already indicated and Q denotes the group required for completing a dicarbonimide ringby reduction of the said compound to the amino compound and acylation into a compound corresponding to Formula III ##STR3## wherein X, Q and R.sup.1 have the meanings indicatedfollowed by conversion of the compound corresponding to Formula III into a compound corresponding to Formula I by hydrazinolytic or hydrolytic decomposition of the dicarbonimide ring.
    Type: Grant
    Filed: November 23, 1987
    Date of Patent: October 10, 1989
    Assignee: Agfa-Gevaert Aktiengesellschaft
    Inventors: Heinz Wiesen, Erich Wolff
  • Patent number: 4855323
    Abstract: Leukotriene antagonists, a process for the preparation thereof, and the use thereof for the treatment of diseases ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X have the indicated meanings, a process for the preparation of these compounds, the use thereof as pharmaceuticals, and pharmaceutical products based on these compounds, are described.
    Type: Grant
    Filed: July 22, 1988
    Date of Patent: August 8, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gunther Wess, Wilhelm Bartmann, Gerhard Beck, Hiristo Anagnostopulos
  • Patent number: 4855086
    Abstract: The specification describes and claims methods of controlling acarine pests by application of a compound of Formula (I), methods of controlling arthropod pests by application of a compound of Formula (IA), compounds of Formula (IA) per se, pesticidal compositions comprising a compound of Formula (IA), and processes for preparing a compound of Formula (IA).
    Type: Grant
    Filed: October 11, 1983
    Date of Patent: August 8, 1989
    Assignee: Burroughs Wellcome Co.
    Inventors: Malcolm H. Black, Robert J. Blade
  • Patent number: 4851440
    Abstract: Leukotriene antagonists, processes for the preparation thereof, the use thereof for the treatment of diseases, and precursors.Compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and X have the indicated meanings, processes for the preparation of these compounds, the use thereof as pharmaceuticals, and pharmaceutical products based on these compounds are described. In addition, precursors for the preparation of compounds of the formula I are described.
    Type: Grant
    Filed: July 22, 1988
    Date of Patent: July 25, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Beck, Peter Below, Andreas Bergmann
  • Patent number: 4826873
    Abstract: Compounds of the general formula ##STR1## wherein R.sub.1 represents hydrogen, an acyl group having 1 to 18 carbon atoms or both R.sub.1 together the group ##STR2## R.sub.2 represents hydrogen or a methyl group, have been isolated in small amounts from the leaves of Clausena lansium. The new compounds are to be used for the production of compositions for the use of the treatment of acute and chronical viral hepatitis, liver intoxication, hypoxia or amnesia.
    Type: Grant
    Filed: January 15, 1987
    Date of Patent: May 2, 1989
    Assignees: Chinese Academy of Medical Sciences, Bayer Aktiengesellschaft
    Inventors: Ming-he Yang, Yan-rong Chen, Geng-tao Liu, Liang Huang
  • Patent number: 4827016
    Abstract: Dermal inflammations which are induced and propagated by leukotrienes are treated by topically applying to the inflamed dermis the following compound: ##STR1## wherein R.sup.3 is H or a thiol; n is 1 to 12; p is 0 to 12; X is a substituted carbonyl, such as an ester or a carboxylic acid; and Y is an aliphatic or branched hydrocarbon, aromatic ring, carbonyl or substituted amide.
    Type: Grant
    Filed: July 20, 1987
    Date of Patent: May 2, 1989
    Inventor: Lee R. Morgan
  • Patent number: 4826815
    Abstract: The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; Or.sub.10 wherein R.sub.10 is hydrogen or loweralkyl; NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are independently selected from hydrogen and loweralkyl; or R.sub.13 --CO--B wherein B is NH, O, CH.sub.2, HNCH.sub.2 and R.sub.13 is loweralkyl, alkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, aminoalkyl, N-protected aminoalkyl, hydroxylated dialkylamino, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic, carboxyalkyl, or lower alkyl carboxyalkyl esters; W is N or CH: U,V may be the following combinations H,OH; OH,H; H,H; or when taken together as O represents a carbonyl with the provisos that if U,V.dbd.H,OH, then W=CH, and if U,V.dbd.O then W.dbd.N; R.sub.1 , R.sub.3 and R.sub.5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R.sub.2, R.sub.4, R.sub.7, R.sub.8 and R.sub.
    Type: Grant
    Filed: January 9, 1987
    Date of Patent: May 2, 1989
    Assignee: Abbott Laboratories
    Inventors: Jay R. Luly, Joseph Dellaria, Anthony K. L. Fung, Dale J. Kempf, Jacob J. Plattner, Saul H. Rosenberg, Hing L. Sham
  • Patent number: 4820858
    Abstract: The invention relates to a process for the preparation of 2-(hydroxyalkyl)acrylic compounds having the formula ##STR1## wherein X represents a --CN group, a --COOR.sub.3 group, a --COR.sub.4 group or a --CONR.sub.4 R.sub.5 group wherein R.sub.3 is an alkyl group containing 1-4 C atoms and R.sub.4 and R.sub.5 independently represent an H atom or R.sub.3, andwherein R.sub.1 and R.sub.2 independently represent an H atom or an alkyl group with 1-4 C atoms or an (hetero) aryl group, or R.sub.1 and R.sub.2 together represent a cyclic compound with 5-12 C atomsby contacting an acrylic compound H.sub.2 C.dbd.CH--X with a carbonyl compound of the formula ##STR2## wherein X, R.sub.1 and R.sub.2 denote the same as in the above, this being effected in the liquid phase in the presence of a tertiary amine, characterized in that the reaction is carried out at a pressure in excess of 500 bar in excess of 500 bar, advantageously 1,500-18,000 bar.
    Type: Grant
    Filed: March 18, 1988
    Date of Patent: April 11, 1989
    Assignee: Stamicarbon B.V.
    Inventors: Neil S. Isaacs, Jonathan Hill
  • Patent number: 4816486
    Abstract: Novel amide derivatives are disclosed. As examples of said amide derivatives are mentioned N-cyclohexyl-N-methyl-(2-(3-(3-methoxy-4-hydroxyphenyl)-2-(propenoylamino) -3, 5-dibromobenzyl)amine and N-cyclohexyl-N-methyl-(2-(5-(3-methoxy-4-hydroxyphenyl)-2,4-pentadienoylam ino )-3,5-dibromobenzyl)amine. These amide derivatives have a 5-lipoxygenase inhibitory activity and are useful as an antiallergic agent.
    Type: Grant
    Filed: September 29, 1986
    Date of Patent: March 28, 1989
    Assignee: Terumo Corporation
    Inventors: Makoto Takai, Noriie Itoh, Shin Hattori, Hirokazu Hasegawa, Toshio Wakabayashi
  • Patent number: 4801735
    Abstract: Compounds are described of the following formula ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-12 alkyl or C.sub.2-12 alkenyl, at least one of R.sup.1 and R.sup.2 being C.sub.1-12 alkyl or C.sub.2-12 alkenyl; X.sup.1 and X.sup.2 are each hydrogen or a protecting group; and Y is(a) --(CH.dbd.CH).sub.n Z in which n is 1, 2 or 3 and Z is --CHO, --CH.sub.2 OH, --COR.sup.3, --(CH.sub.2).sub.m --COR.sup.3 or --(CH.sub.2).sub.p CH.dbd.CH(CH.sub.2).sub.q --COR.sup.3 in which m is an integer of 1 to 12, p is an integer of 1 to 4, q is an integer of 1 to 10 and R.sup.3 is (i) --OH or (ii) --NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl or optionally substituted phenyl, or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form a morpholino, pyrrolidinyl or piperidino ring,(b) --CH.dbd.NR.sup.6 in which R.sup.6 is (i) --OH, (ii) C.sub.1-12 alkyl optionally substituted by --OH, --COOH or --NR.sup.7 R.sup.8 where R.sup.7 and R.sup.
    Type: Grant
    Filed: November 25, 1985
    Date of Patent: January 31, 1989
    Assignee: Lilly Industries Limited
    Inventors: Mark A. W. Finch, John R. Harris
  • 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: 4791133
    Abstract: This invention relates to leukotriene B.sub.4 antagonists having the structure ##STR1## and the pharmaceutically acceptable addition salts thereof; wherein R.sup.1 is lower alkyl having 1-10 carbon atoms; or lower alkenyl or alkynyl having 2-10 carbon atoms; or lower alkadienyl having 3-10 carbon atoms; or lower alkadiynyl or alkenynyl having 4-10 carbon atoms;wherein R.sup.2 and R.sup.3 are the same or different and represent hydrogen or lower alkyl having 1-6 carbon atoms;wherein X is CH.dbd.CH, S, or O;wherein Y is CH.dbd.CH or C.tbd.C;wherein Z is OR.sup.4 or NR.sup.5 R.sup.6, and wherein R.sup.4 represent H, lower alkyl having 1-6 carbon atoms, or a pharmaceutically acceptable cation, and wherein R.sup.5 and R.sup.6 act independently and represent H or lower alkyl having 1-6 carbon atoms, or R.sup.5 and R.sup.
    Type: Grant
    Filed: June 26, 1987
    Date of Patent: December 13, 1988
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
  • Patent number: 4785107
    Abstract: The novel phenol derivatives of the general formula (I) ##STR1## where R is hydrogen, straight-chain or branched C.sub.1 -C.sub.8 -alkyl or cycloalkyl, A is a bridge member and B is a radical of the formula ##STR2## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and T.sup.1 independently of one another are each hydrogen, C.sub.1 -C.sub.8 -alkyl, halogen, CN, COOT.sup.2 or CONHT.sup.2, with the proviso that one or more of the radicals R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and T.sup.1 are halogen, CN, COOT.sup.2 and CONHT.sup.2 and T.sup.2 is C.sub.1 -C.sub.8 -alkyl, are useful for stabilizing organic material, in particular polyolefins, to degradation by oxidation.
    Type: Grant
    Filed: June 12, 1986
    Date of Patent: November 15, 1988
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Helwig, Peter Neumann, Herbert Bender, Alexander Aumueller, Hubert Trauth
  • Patent number: 4760161
    Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit lipoxygenase, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
    Type: Grant
    Filed: April 25, 1983
    Date of Patent: July 26, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Timothy F. Gallagher
  • Patent number: 4741848
    Abstract: A method of preparing boron-containing compositions is described which comprises reacting at least one hydroxy-substituted ester, amide or imide with a boron compound. Such boron-containing compositions are useful in lubricating oils and provide the lubricating oils with anti-wear and/or friction-reducing properties. The boron-containing compositions also are useful in fuel compositions.
    Type: Grant
    Filed: March 13, 1986
    Date of Patent: May 3, 1988
    Assignee: The Lubrizol Corporation
    Inventors: Frederick W. Koch, Joseph W. Pialet, Daniel E. Barrer, Calvin W. Schroeck
  • Patent number: 4733002
    Abstract: A lipoxygenase inhibitor comprising as active ingredient a substituted styrene derivative having a radical of the general formula ##STR1## wherein X denotes a hydroxyl group or a lower alkoxy group and q is an integer of 2 or 3, and containing carbon atoms in total of at least 8.
    Type: Grant
    Filed: May 23, 1985
    Date of Patent: March 22, 1988
    Assignee: Green Cross Corporation
    Inventors: Kazumasa Yokoyama, Chikara Fukaya, Masanori Sugiura, Youichiro Naito, Youichiro Nishida, Tadakazu Suyama
  • Patent number: 4685962
    Abstract: A compound of the formula ##STR1## wherein Y represents a halogen atom, a lower alkyl group, a lower alkoxy group or a trifluoromethyl group and R represents a lower alkyl group. This compound can be produced by reacting a compound of the formula ##STR2## or a reactive derivative thereof with an aniline derivative of the formula ##STR3## and is useful as a herbicide.
    Type: Grant
    Filed: December 17, 1984
    Date of Patent: August 11, 1987
    Assignee: Yashima Chemical Industrial Co., Ltd.
    Inventors: Tetsuo Takematsu, Akinori Suzuki, Kazuya Toda, Masuo Goto
  • Patent number: 4661505
    Abstract: This invention provides novel alkane derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
    Type: Grant
    Filed: November 3, 1982
    Date of Patent: April 28, 1987
    Assignee: Eli Lilly and Company
    Inventors: Winston S. Marshall, John P. Verge
  • Patent number: 4661601
    Abstract: New compounds having the formula 1 ##STR1## wherein W is hydrogen, halogen, n-alkyl, --NHCOR.sup.1, --COR.sup.1, or phenoxyacetylamino optionally substituted by one or two C.sub.1-12 straight- or branched chain alkyl, X is a substituent in the coupling position and is selected from hydrogen, chlorine, bromine, --SR.sup.11 or a nitrogen-containing heterocyclic residue attached at a ring nitrogen atom, and Y is a group having the formula 2 ##STR2## wherein Q is selected from the residues: --COOR.sup.4 or --CONR.sup.4 R.sup.5, --OM, --NR.sup.7 R.sup.8, --PO(OR.sup.9)[O].sub.x R.sup.10 with X=0 or 1, --SO.sub.2 OH, --SO.sub.2 NR.sup.4 R.sup.5 or CN. The groups R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, M, k and n are defined hereinafter.These compounds are used as black color couplers in photographic materials.
    Type: Grant
    Filed: April 3, 1985
    Date of Patent: April 28, 1987
    Assignee: Ciba-Geigy AG
    Inventor: Frederick H. Howell
  • Patent number: 4647413
    Abstract: Perfluoropolyether oligomers or block polymers, having a backbone with one or a plurality of perfluoropolyether segments each consisting essentially of (1) at least one perfluoroisopropyleneoxy unit, (2) a bis(perfluoromethyleneoxy-terminated) unit, and (3) a perfluoroethylidene unit terminating each segment, the backbone of the perfluoropolyether being terminated with COF and/or a functional or nonfunctional derivative thereof, said perfluoropolyethers being made by reacting a perfluoroaliphatic diacid fluoride with hexafluoropropylene epoxide to produce an acid fluoride-terminated perfluoropolyether adduct or oligomer which then can be photopolymerized to yield an acid fluoride-terminated perfluoropolyether block polymer. These oligomers and block polymers are useful as high temperature lubricants, hydraulic fluids, gaskets, adhesives and coatings as well as co-reactants wtih urethane in forming propellant binders.
    Type: Grant
    Filed: January 20, 1984
    Date of Patent: March 3, 1987
    Assignee: Minnesota Mining and Manufacturing Company
    Inventor: Patricia M. Savu
  • Patent number: 4647389
    Abstract: A lubricating oil composition containing a product prepared by reacting a natural oil with a (C.sub.2 -C.sub.10) hydroxy acid and a polyamine whereby the lubricating oil is improved in anti-friction and other properties.
    Type: Grant
    Filed: August 19, 1985
    Date of Patent: March 3, 1987
    Assignee: Texaco Inc.
    Inventors: Thomas J. Karol, Harold S. Magaha, Raymond C. Schlicht
  • Patent number: 4645852
    Abstract: In an improved process of converting a 1,2-epoxy-2-phenylbutane or a 1,2-epoxy-2-phenylpentane to a 2-hydroxy-2-phenylbutylsulfonate, sulfamate, or halide, or the corresponding 2-hydroxy-2-phenylpentyl compound, respectively, by the reaction at about 40.degree. to 120.degree. C. in the presence of an organic solvent of the requisite epoxybutane or epoxypentane with a proton source and a nucleophile. The proton source can be a free strong acid such as a sulfonic, sulfamic acid, or hydrohalide acid, or the proton source can be derived from an equilibrium system comprising a free strong acid and weak base in equilibrium with the respective deprotonated strong acid and protonated weak base. The process is carried out in one step with reduction or avoidance of aldehyde formation by rearrangement of the epoxyalkane.
    Type: Grant
    Filed: September 16, 1985
    Date of Patent: February 24, 1987
    Assignee: The Dow Chemical Company
    Inventors: Lennon H. McKendry, Richard C. Krauss
  • Patent number: 4626597
    Abstract: 16-Fluoro-16,17-didehydro prostanoids, processes for their preparation, compositions containing them and methods of using them are disclosed. The compounds and compositions have pharmaceutical utility including, for example, luteolytic activity.
    Type: Grant
    Filed: August 22, 1984
    Date of Patent: December 2, 1986
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Franco Faustini, Roberto d'Alessio, Achille Panzeri, Enrico di Salle
  • Patent number: 4623729
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
    Type: Grant
    Filed: July 22, 1982
    Date of Patent: November 18, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Sesha I. Natarajan, Eric M. Gordon
  • Patent number: 4616082
    Abstract: New hydroquinone ether compounds of formula I are described: ##STR1## wherein p is 1 or 2 and Q is 0 or 1, provided that p+q is 1 or 2, R is a residue of formula II ##STR2## and R.sub.o, R.sub.oo, R.sub.1, R.sub.2, R.sub.3, Q, n and k are as defined in the specification,The new compounds are useful e.g. as stabilizers in photographic material.
    Type: Grant
    Filed: June 7, 1985
    Date of Patent: October 7, 1986
    Assignee: Ciba-Geigy AG
    Inventor: Frederick H. Howell
  • Patent number: 4610819
    Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed.
    Type: Grant
    Filed: September 19, 1984
    Date of Patent: September 9, 1986
    Assignee: A. H. Robins Company, Inc.
    Inventors: Young S. Lo, Albert D. Cale, Jr.