At Least Three Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 548/151)
  • Patent number: 5834499
    Abstract: A 5-HT.sub.3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): ##STR1## wherein the A ring is substituted or unsubstituted and represents a benzene or a heterocyclic ring with one or two heteroatoms;one of L.sub.1 or L.sub.
    Type: Grant
    Filed: August 26, 1996
    Date of Patent: November 10, 1998
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Iwaoka, Hideki Anan, Naoki Imanishi, Kenichi Kazuta, Hiroyuki Koshio, Takeshi Suzuki, Hirotsune Itahana, Hiroyuki Ito, Keiji Miyata, Mitsuaki Ohta
  • Patent number: 5827799
    Abstract: An object of the invention is to provide herbicides which are completely selective to crops such as paddy rice, soybeans and cotton and have an excellent herbicidal activity on weeds.The invention relates to ether compounds of the general formula (I) ##STR1## in which R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the same meanings as defined in the text and herbicides containing said compounds as active components.
    Type: Grant
    Filed: July 19, 1996
    Date of Patent: October 27, 1998
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Kiyoshi Arai, Fumiaki Koizumi, Hiroyuki Suzuki, Takeshi Kakimoto, Sadafumi Koda
  • Patent number: 5766510
    Abstract: A process for producing a liquid crystalline compound represented by the following general formula (A): ##STR1##
    Type: Grant
    Filed: August 22, 1996
    Date of Patent: June 16, 1998
    Assignee: Dai Nippon Printing Co., Ltd.
    Inventors: Junichi Hanna, Masahiro Funahashi, Masanori Akada, Masayuki Ando, Yozo Kosaka
  • Patent number: 5754271
    Abstract: The invention relates to photochromic compounds of general formula: ##STR1## wherein R.sup.a, R.sup.b and R.sup.c is denote hydrogen; alkyl; aryl; OR, SR, COR or COOR, in which R denotes hydrogen, alkyl or aryl, amino of formula NR.sub.1 R.sub.2 in which R.sub.1 and R.sub.2 denote hydrogen, alkyl, cycloalkyl or an aryl; a halogen atom; a mono- or polyhaloalkyl group; or an NO.sub.2, CN or SCN group; n and m denote integers from 1 to 5; p is equal to 1 or 2; and H is a 5-members aromatic heterocycle containing one or more heteroatoms selected from nitrogen, oxygen and sulfur, these heterocyclic nuclei being eventually substituted by one or more alkyl, alkoxy, amino, aryl or aralkyl groups or condensed with a phenyl nucleus, a substituted phenyl nucleus or a 6-members cycloaliphatic nucleus and to their use in ophtalmic optics.
    Type: Grant
    Filed: June 3, 1996
    Date of Patent: May 19, 1998
    Assignee: Essilor International (Compagnie General d'Optique)
    Inventors: Robert Guglielmetti, Jean Luc Pozzo, Andre Samat
  • Patent number: 5705509
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X.sub.1 --(CH.sub.2).sub.x --X.sub.2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X.sub.1 is O or S; X.sub.2 is O, S, NR.sub.5 or NR.sub.6 CO wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl; or one of X.sub.1 and X.sub.2 is O, S or CH.sub.2 and the other is CH.sub.2 ; x is 1, 2 or 3; R.sub.1 and R.sub.2 together are Q--CH.sub.2 --CH.sub.2, Q--CH.dbd.CH, or Q--CH.dbd.N where Q is linked either to the R.sub.1 or the R.sub.2 substitution position and Q is O, S or NR.sub.t wherein R.sub.t is hydrogen or C.sub.1-6 alkyl; R.sub.3 is hydrogen halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino; R.sub.4.sup.1 and R.sub.4.sup.2 are independently hydrogen or C.sub.1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
    Type: Grant
    Filed: July 28, 1995
    Date of Patent: January 6, 1998
    Assignee: SmithKline Beecham plc
    Inventors: Laramie Mary Gaster, Paul Adrian Wyman
  • Patent number: 5686459
    Abstract: Novel dioxopyrrolo-pyrrole derivatives of the formula ##STR1## as well as hydrates or solvates thereof, which inhibit thrombin-induced or Factor Xa-induced platelet aggregation and fibrinogen clotting in blood plasma. The derivatives can be manufactured from the corresponding maleimides which are N-substituted by .alpha.-amino carboxylic acids of the formula HN(R.sup.2)CH(R.sup.4)COOH, or functional derivatives thereof; and ketones or aldehydes of the formula R.sup.5 C(O)R.sup.6.
    Type: Grant
    Filed: February 26, 1996
    Date of Patent: November 11, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Francois Diederich, Ulrike Obst, Sabine Wallbaum, Lutz Weber
  • Patent number: 5633371
    Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.
    Type: Grant
    Filed: September 15, 1995
    Date of Patent: May 27, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mos e Da Prada, Gerhard Z urcher
  • Patent number: 5565482
    Abstract: A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A is --(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --; wherein X is S(O).sub.p or O; wherein m is 0 or 1; wherein n is 0 or 1; wherein p is 0 or 1; wherein B is selected from phenyl and five and six membered heteroaryl; wherein R.sup.1 is selected from lower haloalkyl, cyano, formyl, lower alkoxycarbonyl, lower alkoxy, lower N-alkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R.sup.2 is phenyl substituted at a substitutable position with a radical selected from lower alkylsulfonyl and sulfamyl; and wherein R.sup.
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: October 15, 1996
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Stephen R. Bertenshaw, Matthew J. Graneto, Donald J. Rogier
  • Patent number: 5565479
    Abstract: Condensed thiazole derivatives useful as 5-HT.sub.3 receptor agonists are provided and can be represented by the following formula (I) or a pharmaceutically acceptable salt thereof, a process for the production thereof and a pharmaceutical composition thereof: ##STR1## wherein R, A, L.sub.1, L.sub.2, L, and R.sup.1 -R.sup.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: October 15, 1996
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Iwaoka, Hiroyuki Koshio, Hiroyuki Ito, Keiji Miyata, Mitsuaki Ohta
  • Patent number: 5541323
    Abstract: Anhydride compounds which contain at least one rodlike mesogenic moiety and at least two anhydride groups per molecule, wherein each of said aromatic anhydride groups is linked to the mesogen via an ester linkage are prepared. These anhydride compounds are useful in curing epoxy resins to provide the cured products with one or more improved properties.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: July 30, 1996
    Assignee: The Dow Chemical Company
    Inventors: Robert E. Hefner, Jr., Jimmy D. Earls
  • Patent number: 5512564
    Abstract: The present invention concerns thiazolo- 2,3-a!pyrrole and oxazolo- 1,2-a!pyrrole derivatives of formula I ##STR1## in which HET represents a heterocyclic ring with 3-7 ring atoms which can be substituted by one, two or three residues R.sup.1 which can be the same or different,Y represents an oxygen or sulphur atom, or a SO or SO.sub.2 group,X can be an oxygen or sulphur atom,R denotes an aliphatic residue with 1-9 C-atoms which can be substituted by phenyl or denotes a phenyl ring or a carbocyclic ring with 7-15 C atoms or a heterocyclic ring system each having 5 or 6 ring atoms,in which the aforementioned phenyl rings, carbocyclic rings or heterocyclic ring system can be substituted once or several times, if desired, and R1-R5 denote hydrogen or an aliphatic residue, as well as their tautomers, enantiomers, diastereomers and physiologically tolerated salts.
    Type: Grant
    Filed: March 4, 1994
    Date of Patent: April 30, 1996
    Assignee: Boehringer Mannheim GmbH
    Inventors: Harald Zilch, Herbert Leinert, Alfred Mertens
  • Patent number: 5480874
    Abstract: The invention provides a phosphonic diester derivative of the formula: ##STR1## wherein the variables are as defined in the specification. The derivative of the invention has excellent hypolipidemic and hypoglycemic activities and little side effects and hence is useful as therapeutic and prophylactic agents for hyperlipidemic diseases and diabetes and as a therapeutic agent for cataract.
    Type: Grant
    Filed: January 12, 1995
    Date of Patent: January 2, 1996
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Yasuo Shoji, Yoshihiko Tsuda, Kazuhiko Tsutsumi, Yasuhide Inoue
  • Patent number: 5451594
    Abstract: The invention provides compounds of formula (I) having nematicidal, insecticidal, acaricidal and fungicidal properties, compositions comprising them and processes and intermediates for their preparation: ##STR1## wherein: X is oxygen or sulphur;n is 0, 1 or 2;R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as described in the specification.
    Type: Grant
    Filed: September 10, 1993
    Date of Patent: September 19, 1995
    Assignee: Zeneca Limited
    Inventors: Steven Fitzjohn, Michael P. Robinson, Michael D. Turnbull, Alison M. Smith, Roger Salmon, Robin Taylor
  • Patent number: 5428168
    Abstract: The invention encompasses compounds of general formula I: ##STR1## wherein W represents an imidazo[4,5-c]pyridyl group, optionally substituted with one or more substituents selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halo, CF, and CN; and Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 are variables. These compounds are useful as antagonists of platelet activating factor.
    Type: Grant
    Filed: October 23, 1992
    Date of Patent: June 27, 1995
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Mark Whittaker, Alan H. Davidson, Zoe M. Spavold, Stephen A. Bowles
  • Patent number: 5418248
    Abstract: Compounds of the formula: ##STR1## in which R.sub.1 represents a hydroxy group, a C.sub.1 -C.sub.4 alkoxy group or an amino group of general formula --NR.sub.4 R.sub.5 in which R.sub.4 and R.sub.5 each represent, independently of each other, a hydrogen atom, a straight or branched C.sub.1 -C.sub.4 alkyl group, an allyl group or a methoxyethyl group, or alternatively --NR.sub.4 R.sub.5 represents a heterocycle containing 3 to 6 carbon atoms,Y represents a thienyl group optionally substituted by an alkyl group, andX represents a hydrogen or halogen atom,are useful as anticonvulsants and auxiolytics.
    Type: Grant
    Filed: December 29, 1993
    Date of Patent: May 23, 1995
    Assignee: Synthelabo
    Inventors: Mireille Sevrin, Claude Morel, Michel Mangane, Pascal George
  • Patent number: 5314889
    Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: May 24, 1994
    Assignee: Elf Sanofi
    Inventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
  • Patent number: 5252769
    Abstract: Anthraquinonic colorant represented by the formula (I): ##STR1## wherein Q.sup.1 and Q.sup.2 are each independently substituted or unsubstituted anthraquinonyl groups, Z.sup.1 and Z.sup.2 are bridge groups, A is an aromatic divalent group, and n is 0 or 1. The polarizing film which contains at least one colorant of the present invention in a hydrophobic resin, has excellent durability and moisture resistance.
    Type: Grant
    Filed: June 26, 1992
    Date of Patent: October 12, 1993
    Assignee: Mitsui Toatsu Chemicals, Incorporated
    Inventors: Tsutami Misawa, Hisato Itoh, Tsutomu Nishizawa, Masami Nakano, Hiroyuki Katayama
  • Patent number: 5241076
    Abstract: 2,7-Diazabicyclo[3.3.0] octanes, suitable for 7-position substituents or antibacterially active quinolone carboxylic acids, of the formula ##STR1## in which R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.7 and R.sup.8 may be identical or different and in each case denote H, C.sub.1 -C.sub.5 -alkyl (optionally substituted by halogen, hydroxyl or C.sub.1 -C.sub.3 -alkoxy), C.sub.1 -C.sub.3 -alkoxycarbonyl or C.sub.6 -C.sub.12 -aryl,R.sup.4 additionally denotes halogen,R.sup.2 and R.sup.6 may be identical or different, denote H, C.sub.1 -C.sub.6 -alkyl, benzyl, C.sub.6 -C.sub.12 -aryl, C.sub.1 -C.sub.3 -alkanoyl, benzoyl or C.sub.1 -C.sub.5 -alkoxycarbonyl, orR.sup.2 and R.sup.3 together denote a bridge of the structure (CH.sub.2).sub.n, n=2-4, CH.sub.2 -CHOH-CH.sub.2, CH.sub.2 -S-CH.sub.2 or C(CH.sub.3).sub.2 -S-CH.sub.2, excluding 2,7-diazabicylcol[3.3.0]octane.
    Type: Grant
    Filed: July 10, 1992
    Date of Patent: August 31, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Thomas Schenke, Uwe Petersen
  • Patent number: 5233017
    Abstract: Benzobisthiazole polymers with thiophene moieties having repeating units of the formula:--Bt--(--Tp--).sub.n --wherein Bt is ##STR1## Tp is ##STR2## and n 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: My Dotrong, Robert C. Evers, Ronald C. Tomlinson, Mark Sinsky
  • Patent number: 5217984
    Abstract: 1-Phenyl substituted-1H,3H-thiazole [3,4-a] benzimidazoles are prepared by reaction of o.phenilendiamine with a substituted benzaldehyde and with 2-mercaptoacetic acid. The new compounds are antiviral products.
    Type: Grant
    Filed: July 25, 1991
    Date of Patent: June 8, 1993
    Inventors: Pietro Monforte, Anna M. Monforte, Maria Zappala, Giovanni Romeo, Silvana Grasso, Alba Chimirri
  • Patent number: 5149819
    Abstract: Squarylium compounds having the following formula (I), ##STR1## and an optical information recording medium comprising a substrate, and a recording layer formed on the substrate, comprising a squarylium compound having formula (II) are disclosed: ##STR2##
    Type: Grant
    Filed: May 1, 1991
    Date of Patent: September 22, 1992
    Assignees: Ricoh Company, Ltd., Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Tsutomu Satoh, Ikuo Shimizu, Yukiyoshi Ito
  • Patent number: 5047554
    Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.
    Type: Grant
    Filed: January 31, 1990
    Date of Patent: September 10, 1991
    Assignee: Pfizer Inc.
    Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
  • Patent number: 4978671
    Abstract: The invention relates to novel thieno-(3',4'-4,5)imidazo(2,1-b)thiazole derivatives of the formula ##STR1## in which R.sub.1 denotes hydrogen, halogen or CF.sub.3 andR.sub.2 denotes hydrogen or C.sub.1 -C.sub.4 alkyl and, in the case in which R.sub.2 denotes hydrogen, their pharmaceutically utilizable salts, a process for the preparation of these compounds and their use for the treatment of cancer or rheumatoid arthritis caused by a defective immune system.
    Type: Grant
    Filed: August 30, 1989
    Date of Patent: December 18, 1990
    Assignee: Chemisch Pharmazeutische Forschungsgesellschaft m.b.H.
    Inventors: Dieter Binder, Franz Rovenszky, Hubert P. Ferber
  • Patent number: 4968708
    Abstract: The present invention relates to novel imidazo-[2,1-b]benzothiazole compounds represented by formula (I) and pharmacological acceptable salts thereof: ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms; R.sub.2 represents a ##STR2## group (wherein X and Y, which may be the same or different, each represents a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms or a substituted or unsubstituted phenyl group), a --CH.sub.2 --O--Z group (wherein Z represents a lower alkyl group having 1 to 4 carbon atoms or a substituted or unsubstituted benzyl group) or a --CH.sub.2 --O--CO--W group (wherein W represents an alkyl group having 1 to 8 carbon atoms, an alkylamino group having 1 to 8 carbon atoms, a substituted or unsubstituted phenyl group or a thienyl group); and R.sub.3 ; R.sub.4 and R.sub.
    Type: Grant
    Filed: June 21, 1989
    Date of Patent: November 6, 1990
    Assignee: Nikken Chemicals Co., Ltd.
    Inventors: Taketsugu Seki, Shigeyuki Tasaka, Ryuichi Hoshino
  • Patent number: 4946955
    Abstract: A method for preparation of polycyclic 1,3-thiazolidines is described. The method comprises reacting a fluoride ion source, in a solvent, with an onium salt synthesized by the reaction of a nitrogenous heteroaromatic compound with a halomethyl trimethylsilylmethyl sulfide, the halomethyl trimethylsilylmethyl sulfide being selected from the group consisting of chloromethyl trimethylsilylmethyl sulfide, bromomethyl trimethylsilylmethyl sulfide, or iodomethyl trimethylsilylmethyl sulfide.
    Type: Grant
    Filed: September 9, 1988
    Date of Patent: August 7, 1990
    Assignee: Toray Silicone Company Limited
    Inventor: Akira Hosomi
  • Patent number: 4895863
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of ##STR2## R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.6 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, halogen, alkoxycarbonyl of 2 to 5 carbon atoms, cyano, ##STR3## R' and R" are individually alkyl of 1 to 5 carbon atoms, R.sub.2 and R.sub.3 together form a member of the group consisting of ##STR4## m is 1, 2 or 3, X.sub.1 and X.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, alkenyl of 2 to 5 carbon atoms, alkoxy of 1 to 5 carbon atoms, aralkoxy, aryloxy, halogen, azido and nitro or taken together form methylenedioxy and their non-toxic, pharmaceutically acceptable acid additon salts capable of treating memory disorders.
    Type: Grant
    Filed: October 18, 1988
    Date of Patent: January 23, 1990
    Assignee: Roussel Uclaf
    Inventors: Charles J. R. Hedgecock, David P. Kay
  • Patent number: 4880824
    Abstract: Heterocyclic compounds of formulae (I) and (II): ##STR1## where R.sup.1 and R.sup.2 are alkyl, R.sup.3 is H or alkyl, m is 2-5 and Het is a hetercycle such as thiazole, benzothiazole, substituted benzothiazole, pyrazine, triazine, thiadiazole, substituted thiadiazole, pyrimidine or substituted pyrimidine. The compounds are calcium channel blockers useful in the treatment of cardiovascular conditions such as hypertension or angina.
    Type: Grant
    Filed: September 21, 1987
    Date of Patent: November 14, 1989
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Maud Urbanski
  • Patent number: 4873237
    Abstract: The invention relates to a method of treatment of ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--(CHR.sup.5).sub.n --CHR.sup.6 -- (Ia)R represents an optionally substituted aryl or heteroaryl radical,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent and said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur;R.sup.5 and R.sup.
    Type: Grant
    Filed: May 22, 1986
    Date of Patent: October 10, 1989
    Assignee: John Wyeth & Brother Limited
    Inventor: Roger Crossley
  • Patent number: 4849327
    Abstract: Benzo-bis-thiazole quaternary salts having attached to at least one quaternary nitrogen atom thereof an alkenyl group carrying a double bond in the .beta.-position and their use as antifogging agents in silver halide light-sensitive materials.
    Type: Grant
    Filed: May 26, 1988
    Date of Patent: July 18, 1989
    Assignee: Minnesota Mining and Manufacturing Company
    Inventor: Ivano Delprato
  • Patent number: 4841009
    Abstract: Described herein are novel substantially linear monomeric compositions which can be polymerized with one or more difunctional monomers to give novel polymeric compositions having liquid crystal properties. This invention is also directed to a process for preparation of the novel substantially linear monomeric compositions.
    Type: Grant
    Filed: July 5, 1985
    Date of Patent: June 20, 1989
    Assignee: Amoco Corporation
    Inventor: Donald R. Kelsey
  • Patent number: 4835167
    Abstract: The present invention provides new tricyclic benzotriazoles of the general formula: ##STR1## wherein Z is a hydrogen atom or an acyl radical, Y is an oxygen or sulphur atom or two hydrogen atoms and X is an oxygen or sulphur atom or a >CR.sub.1 R.sub.2 or >NR.sub.3 group, R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical, R.sub.2 is a hydrogen atom or an alkyl, alkenyl or cyano group or a carbonyl group substituted by a hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino group or R.sub.2, together with R.sub.1, represents a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical and R.sub.3 is a hydrogen atom or an alkyl radical; the tautomers thereof and the physiologically acceptable acid-addition salts thereof with inorganic and organic acids.
    Type: Grant
    Filed: August 3, 1987
    Date of Patent: May 30, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang Von Der Saal, Walter-Gunar Friebe, Alfred Mertens, Bernd Muller-Beckmann, Gisbert Sponer
  • Patent number: 4831032
    Abstract: The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.
    Type: Grant
    Filed: July 3, 1986
    Date of Patent: May 16, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
  • Patent number: 4829077
    Abstract: Compounds of formula ##STR1## (wherein R and R.sub.1 have the meanings reported in the specification) and their preparation are described.The compounds of formula I have anti-allergic, anti-anaphylactic and anti-arthritic activity and are useful in pharmaceutical field.Compositions for pharmaceutical use containing a compound of formula I as active ingredient are described too.
    Type: Grant
    Filed: March 23, 1988
    Date of Patent: May 9, 1989
    Assignee: Zambon Group S.p.A.
    Inventors: Dario Chiarino, Gian C. Grancini, Viviana Frigeni, Angelo Carenzi
  • Patent number: 4814329
    Abstract: The invention relates to novel, sulfur-containing 5-substituted benzimidazole derivatives of formula I ##STR1## and acid-addition salts thereof antihyperlipoproteinemic action, a process for preparing the same, pharmaceutical formulations comprising the novel compound as active ingredient and a method for inhibiting atherosclerosis, trombus formation and treating hyperlipoproteinemic diseases.
    Type: Grant
    Filed: March 17, 1986
    Date of Patent: March 21, 1989
    Assignee: Richter Gedeon Vegyeszeti Gyar R.T.
    Inventors: Kalmen Harsanyi, Andrea Maderspach, Andres Javor, Gyorgy Hajos, Gyorgy Fekete, Laslo Szporny, Peter Tetenyi, Katalin Csomor, Egon Karpati, Bela Hegedus, Marta Kapolnas nee Pap, Marta Szollosy, Anna Kallay nee Sohonyai
  • Patent number: 4812574
    Abstract: The invention concerns a process for preparing a thiazolo[3,2-a]benzimidazole of formula I ##STR1## in which formula n is 1 or 2, and R.sub.1 is hydrogen, lower alkyl, lower alkoxy, trifluoromethyl or halo, or a salt thereof which comprises dehydrating a compound of formula II, ##STR2## or a salt thereof wherein n and R, are as defined above, and COOR is an acid or ester function in the presence of an acid selected from sulphuric, sulphonic and phosphoric acid or mixtures thereof and if desired or required an inert solvent provided that if water is present then the amount of water is less than about 15% by volume of the acid, the reaction being carried out with heating if necessary.
    Type: Grant
    Filed: December 23, 1987
    Date of Patent: March 14, 1989
    Assignees: John Wyeth & Brother Ltd., American Home Products Corporation
    Inventors: Robin G. Shepherd, Sie-Yearl Chai, Maynard E. Lichty, Arnold S. Milowsky
  • Patent number: 4788292
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, independently of one another, represent hydrogen, hydroxy or halogen or are alkyl, alkoxy, alkanoyloxy, or alkanoylamino groups which are unsubstituted or substituted by alkoxy, hydroxyl, halogen, aryl, cycloalkyl, azacycloalkyl, cyano or by polyalkyleneoxy, or two or more of adjacent R.sub.1 -R.sub.4 together form one or more fused rings of 5-8 members each; R is alkylene of up to 16 carbon atoms which is unsubstituted or substituted by hydroxy, lower alkoxy, or halo and which may be interrupted by oxygen, sulfur, carboxamido, sulfonamido, aminosulfonyl, aminocarbonyl, carbonyloxy, sulfinyl, or sulfonyl; and R.sub.f is perfluoroalkyl or perfluoroalkoxyalkyl of 4 to 16 carbon atoms; or mixtures thereof. Such compounds are useful as oil soluble corrosion inhibitors.
    Type: Grant
    Filed: July 31, 1986
    Date of Patent: November 29, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Kirtland P. Clark, Athanasios Karydas
  • Patent number: 4732984
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --O--, --NH--, ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.7 is 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl, 3-pyridazinyl or phenyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, trifluoromethyl, cyano, nitro or halo, with the proviso that when R.sup.1 and R.sup.2 taken together represent ##STR3## then R.sup.7 is other than 2-pyridinyl, 2-pyrimidinyl or substituted pyrimidin-2-yl;Z is --(CH.sub.2).sub.
    Type: Grant
    Filed: August 5, 1986
    Date of Patent: March 22, 1988
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Guy A. Schiehser, Scott J. Childress
  • Patent number: 4730003
    Abstract: The present invention provides compounds of the general formula: ##STR1## wherein the various substituents are defined hereinbelow. The compounds are used for the treatment and/or prophylaxis of heart and circulatory diseases.
    Type: Grant
    Filed: September 4, 1986
    Date of Patent: March 8, 1988
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann
  • Patent number: 4725605
    Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.
    Type: Grant
    Filed: May 22, 1986
    Date of Patent: February 16, 1988
    Assignee: John Wyeth & Brother Limited
    Inventors: Roger Crossley, Peter J. Meade
  • Patent number: 4695571
    Abstract: Tricyclic oxindole carboxamides, prepared by (a) reaction of an isocyanate with the basic ring system or (b) ammonolysis of a corresponding alkyl ester, are non-steroidal antiinflammatory agents useful in the treatment of rheumatoid arthritis.
    Type: Grant
    Filed: April 2, 1986
    Date of Patent: September 22, 1987
    Assignee: Pfizer Inc.
    Inventor: Lawrence S. Melvin
  • Patent number: 4665206
    Abstract: The invention relates to compounds of the general formula I ##STR1## wherein R.sub.1 represents one up to and including four, the same or different substituents selected from alkyl(1-6 C), alkoxy(1-6 C), hydroxy, halogen, NO.sub.2 CF.sub.3 or the group --NR.sub.5 R.sub.6, whereby two substituents taken together may also represent a methylene-dioxy group,X represents nitrogen or the group ##STR2## n has the value 0, 1 or 2, R.sub.3 represents one of the moieties: ##STR3## the latter meaning of R.sub.3 (amide) only under the condition that for X is nitrogen the meaning of R.sub.1 is limited to substituents selected from hydroxy, alkoxy(1-6 C) and methylenedioxy, and R.sub.4, R.sub.5 and R.sub.6 represent hydrogen or alkyl(1-6 C), and pharmaceutically acceptable salts thereof, suitable in the treatment of heart failure.
    Type: Grant
    Filed: March 7, 1985
    Date of Patent: May 12, 1987
    Assignee: Akzo N.V.
    Inventors: James Redpath, Robert T. Logan, David B. McFadzen, Robert G. Roy
  • Patent number: 4563476
    Abstract: Substituted 5-hydroxy-2,3-dihydrobenzofuran and analogs such as the substituted 6-hydroxy-2,3-dihydrobenzopyrans were prepared from an appropriately substituted (5-hydroxy-2,3-dihydrobenzofuran-6-yl) formaldehyde or analog thereof with an aryl amine followed by reduction. These compounds were found to be potent topical anti-inflammatory agents.
    Type: Grant
    Filed: November 21, 1983
    Date of Patent: January 7, 1986
    Assignee: Merck & Co., Inc.
    Inventors: Michael N. Chang, Milton L. Hammond, Norman P. Jensen, Robert A. Zambias
  • Patent number: 4509971
    Abstract: Novel substituted carboxylic acid amide compound of the formula ##STR1## wherein n is an integer from 1 to 4each R is independently selected from hydrogen, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkylamino, dialkylamino, nitro, cyano and alkoxycarbonyl; and two R radicals taken together can represent methylenedioxy, dichloromethylenedioxy or difluoromethylenedioxy,R.sup.1 is hydrogen or alkyl,R.sup.2 and R.sup.3 are individually selected from hydrogen or a radical selected from alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, aryl and nitrogen-containing heterocycles, each of which radicals may be substituted and each of which radicals may, together with the nitrogen atom to which they are attached, form an optionally substituted, optionally partially unsaturated and optionally benzofused monocyclic or bicyclic radical, which may contain one or more further hetero-atoms, and X is oxygen or sulfur.
    Type: Grant
    Filed: August 19, 1983
    Date of Patent: April 9, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz Forster, Wolfgang Hofer, Volker Mues, Ludwig Eue, Robert R. Schmidt
  • Patent number: 4464384
    Abstract: Novel 2-phenylimidazo[2,1-b]benzothiazole compounds shown by general formula I ##STR1## and the salts thereof, a process of producing the compounds, and pharmaceutical compositions containing the compounds.The compounds of this invention act on immune response, in particular, suppress a delayed type hypersensitivity reaction, and are useful as antiallergic agents, antirheumatics, therapeutic agents for autoimmune diseases, and suppressants of rejection at tissue transplantation and skin graft.
    Type: Grant
    Filed: December 14, 1982
    Date of Patent: August 7, 1984
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Murase, Toshiyasu Mase, Hideki Arima, Kunihiro Niigata, Kenichi Tomioka, Shinichiro Kobayashi
  • Patent number: 4463179
    Abstract: Novel thioesters effective as acylating agents for amines or hydrazines, especially effective as active esters in synthesis of cephalosporin compounds are disclosed. The novel thioester of the present invention can be prepared by reacting a thiol or a derivative thereof with an acetic acid derivative or a reactive derivative thereof. By reacting the thioester of the present invention with a 7-aminocephalosporin derivative or a salt thereof, cephalosporin derivatives or pharmacologically acceptable salts thereof which are excellent antibiotic substances having a high antimicrobial activity can be obtained in high yield very safely.
    Type: Grant
    Filed: September 2, 1981
    Date of Patent: July 31, 1984
    Assignee: Asahi Kasei Kogyo Kabushiki Kaisha
    Inventors: Masahiro Murakami, Masateru Kobayashi, Kimiyo Yamamoto, Chisei Shibuya
  • Patent number: 4344946
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.1 ', which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 2 carbon atoms;R.sub.2 and R.sub.2 ', which may be identical to or different from each other, are each hydrogen or ##STR2## but other than both hydrogen at the same time, where A is alkylene of 1 to 2 carbon atoms,R.sub.5 is hydrogen, lower alkyl, lower alkylamino-lower alkyl, lower alkoxy-lower alkyl, hydroxycarbonyl-lower alkyl, cycloalkyl of 5 to 8 carbon atoms, lower alkyl-cycloalkyl of 5 to 8 carbon atoms, phenyl or morpholino;R.sub.6 is hydrogen, lower alkyl, lower alkylamino-lower alkyl or lower alkoxy-lower alkyl; orR.sub.5 and R.sub.
    Type: Grant
    Filed: August 28, 1980
    Date of Patent: August 17, 1982
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Ernest Cullen, Genus Possanza, Patrick B. Stewart
  • Patent number: 4340738
    Abstract: This invention relates to a novel series of 2,3-dihydroimidazo[2,1-b]benzothiazoles which display monoamine oxidase inhibiting activities.
    Type: Grant
    Filed: January 9, 1981
    Date of Patent: July 20, 1982
    Assignee: Janssen Pharmaceutica, N.V.
    Inventor: Victor Sipido
  • Patent number: 4275065
    Abstract: Novel 2-substituted-3-hydroxythiazolo[2,3-b]benzo-(and azabenzo)thiazolium salts, the mesoionic didehydro derivatives thereof and related compounds are disclosed, as well as the use thereof as modulators of the immune response.
    Type: Grant
    Filed: March 31, 1980
    Date of Patent: June 23, 1981
    Assignee: American Home Products Corporation
    Inventors: Peter H. L. Wei, Francis J. Gregory
  • Patent number: 4262004
    Abstract: This invention relates to a novel series of 2,3-dihydro-imidazo[2,1-b]benzothiazoles which display monoamine oxidase inhibiting activities.
    Type: Grant
    Filed: June 21, 1979
    Date of Patent: April 14, 1981
    Assignee: Janssen Pharmaceutica, N.V.
    Inventor: Victor Sipido
  • Patent number: 4259474
    Abstract: The sulfur-containing polyoxyalkylenes having the formula: ##STR1## wherein E is --SW or a halogen atom; W is hydrogen, phenyl, alkyl of 1 to 4 carbon atoms, an alkali metal or ammonium ion, or a heterocyclic radical containing from 2 to 4 hetero atoms in a 5-or 6-membered ring which may be monocyclic or may be fused to an aromatic ring; A, C and D represent lower alkylene of 2 to 4 carbon atoms; B is alkylene of 2 to 8 carbon atoms; y and z are each integers having a value of 0 to 50; x is an integer having a value of from 2 to 50; and n is an integer having a value of from 1 to 30; and intermixtures of said polyoxyalkylenes.The above compounds display a wide variety of uses; however, all are active metal working lubricants.
    Type: Grant
    Filed: September 25, 1979
    Date of Patent: March 31, 1981
    Assignee: GAF Corporation
    Inventors: Paritosh M. Chakrabarti, Lindley S. Wood, David J. Tracy