Additional Hetero Ring Attached Directly Or Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 540/596)
  • Patent number: 5344934
    Abstract: The present invention provides a process for preparing urethanes and carbonates from an amine or an alcohol, carbon dioxide and a hydrocarbyl halide. The amine or alcohol is reacted with carbon dioxide in a suitable solvent system and in the presence of an amidine or guanidine base, to form the ammonium carbamate or carbonate salt which is then reacted in a polar aprotic solvent with a hydrocarbyl halide. Polymer products can also be prepared utilizing this process or utilizing the resulting urethanes and carbonates under standard polymerization conditions.
    Type: Grant
    Filed: November 16, 1992
    Date of Patent: September 6, 1994
    Assignee: Monsanto Company
    Inventors: William D. McGhee, Dennis P. Riley, John J. Talley, Barry L. Parnas
  • Patent number: 5332741
    Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, andmedicinal products which are useful for treating Central Nervous System disorders.
    Type: Grant
    Filed: May 17, 1993
    Date of Patent: July 26, 1994
    Assignee: Adir et Compagnie
    Inventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
  • Patent number: 5286881
    Abstract: A benzodifuranone compounds of the formula, ##STR1## wherein R.sup.1 and R.sup.2 are each independently a naphthyl group or an unsubstituted or substituted phenyl group, which is useful for dyeing or printing hydrophobic fiber materials, is prepared in high purity and high yield by allowing benzofuran compounds of the formula, ##STR2## wherein R.sup.1 is as defined above, to react with acetonitrile compounds of the formula, ##STR3## wherein R.sup.2 is as defined above, and then carrying out an oxidation reaction to give the benzodifuranone compound.
    Type: Grant
    Filed: September 30, 1992
    Date of Patent: February 15, 1994
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Junichi Sekihachi, Jun Yamamoto, Yutaka Kayane
  • Patent number: 5284857
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
    Type: Grant
    Filed: December 21, 1990
    Date of Patent: February 8, 1994
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 5278174
    Abstract: Sigma binding site agents having the formula ##STR1## which are useful to inhibit sigma binding site-induced activity, pharmaceutical compositions including these agents, and methods of using these agents to inhibit sigma binding site-induced activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented agents.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 11, 1994
    Assignee: Scios Nova, Inc.
    Inventors: Ronald H. Erickson, Kenneth J. Natalie, Jr., Michael J. Pontecorvo, Waclaw J. Rzeszotarski
  • Patent number: 5276168
    Abstract: A new method for the treatment of ischemic conditions and arrhythmia is disclosed. The method uses compounds of the formula ##STR1## wherein A can be --CH.sub.2 --, --O--, --NR.sub.9 --, --S--, --SO--, --SO.sub.2 --; X can be oxygen or sulfur; Y can be --NR.sub.8, --O--, --S--, --CH.sub.2 -- and the R groups are as defined herein. Novel compounds within the definition of formula I are also disclosed.
    Type: Grant
    Filed: June 19, 1992
    Date of Patent: January 4, 1994
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5268471
    Abstract: Process for the preparation of 6-acyl-, 7-acyl- or 6,7-diacyl analogues of forskolin of the general formula ##STR1##
    Type: Grant
    Filed: January 15, 1993
    Date of Patent: December 7, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Noel J. de Souza, Premanand D. Desai, Shrikant V. Savanur, Jurgen Blumbach
  • Patent number: 5268470
    Abstract: A diamine useful as a catalyst for the polymerization of urethane. A method of making the catalyst comprises reacting a spiro quaternary amine with a secondary amine. The spiro quaternary amine is also useful as an antimicrobial agent.
    Type: Grant
    Filed: July 12, 1991
    Date of Patent: December 7, 1993
    Assignee: Buckman Laboratories Internation, Inc.
    Inventors: Wallace E. Puckett, Mark L. Zollinger
  • Patent number: 5262549
    Abstract: 4-[3-(benz[b]pyran-4-ylidene)prop-1-enyl]benz[b]pyrylium, 4-[5-(4H-benz[b]pyran-4-ylidene)penta-1,3-dienyl]benz[b]pyrylium and 4-[7-(4H-benz[b]pyran-4-ylidene)hepta-1,3,5-trienyl]benz[b]pyrylium dyes, wherein at least one of the benzpyrylium nuclei carries at its 2-position a substituent in which a non-aromatic carbon atom is bonded directly to the benzpyrylium nucleus, subject to the proviso that if the or each 2-substituent contains an aromatic nucleus, this aromatic nucleus is not conjugated with the benzpyrylium nucleus, are useful as visible and near infra-red absorbers, having high extinction coefficients and a reduced tendency to develop absorptions at shorter wavelengths when dispersed in polymeric media.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: November 16, 1993
    Assignee: Polaroid Corporation
    Inventors: Stephen J. Telfer, Socorro M. Ramos, Michael J. Zuraw
  • Patent number: 5256657
    Abstract: Compounds having the structural formula ##STR1## wherein X is HONH or HO and especially wherein the carbon atom bearing CH.sub.2 R.sup.1 has the R-configuration, the carbon atom bearing CH.sub.2 R.sup.2 has the S-configuration, R.sup.1 is isopropyl, R.sup.2 is 3-indolyl, m is 2, n is 0, p is 2 and R.sup.3 and R.sup.4 taken alone are each methyl or R.sup.3 and R.sup.4 taken together with N are morpholino and pharmaceutically acceptable acid addition salts or solvates or acid addition salts-solvates thereof, which are matrix-metalloprotease inhibitors useful in treatment of disease in which matrix-metalloprotease promoted connective tissue remodelling is a causative factor, for example, rheumatoid arthritis and cancer, and a method of preparation and method of use thereof and methods of preparation of intermediates therefor are disclosed.
    Type: Grant
    Filed: August 19, 1991
    Date of Patent: October 26, 1993
    Assignee: Sterling Winthrop, Inc.
    Inventors: Jasbir Singh, Barry A. Morgan, James A. Gainor, Thomas D. Gordon, Robert C. Wahl
  • Patent number: 5252598
    Abstract: The present invention relates to labdane-derivatives of the formula ##STR1## a process for their preparation and the use of these substances as medicaments, preferably as medicaments having a positive ionotropic effect, an effect of lowering intraocular pressure and lowing blood pressure.
    Type: Grant
    Filed: May 4, 1992
    Date of Patent: October 12, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Yatendra Khandelwal, Greta Moraes, Bansi Lal, Vijay A. Aroskar, Alihussein N. Dohadwalla, Richard H. Rupp
  • Patent number: 5250682
    Abstract: Process for the manufacture of 6.beta.
    Type: Grant
    Filed: July 22, 1991
    Date of Patent: October 5, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Yatendra Khandelwal, Bansi Lal, Jurgen Blumbach
  • Patent number: 5244893
    Abstract: New compounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.6 have the meanings given in the description, their preparation and use in plant protection, the protection of materials and in the field of human and veterinary medicine.Formula (I) gives a definition of the compounds which can be prepared by analogous processes, for example from suitable benzothiophene derivatives by oxidation.
    Type: Grant
    Filed: April 29, 1992
    Date of Patent: September 14, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Ludwig Elbe, Dieter Berg, Heinz-Wilhelm Dehne, Stefan Dutzmann, Georg-Wilhelm Ludwig, Manfred Plempel
  • Patent number: 5245030
    Abstract: An IR-ray absorptive compound represented by the formula (1) or (2): ##STR1## and an optical recording medium having a substrate and an organic dye thin film, comprising the formulae (1) and/or (2).
    Type: Grant
    Filed: January 31, 1992
    Date of Patent: September 14, 1993
    Assignee: Canon Kabushiki Kaisha
    Inventors: Tetsuro Fukui, Yoshihiro Oguchi, Hiroyuki Sugata, Kyo Miura
  • Patent number: 5223498
    Abstract: Compounds of formula I ##STR1## and their salts in which n=0 or 1, R.sub.1 and R.sub.2 are each aliphatic or cycloalkyl or NR.sub.1 R.sub.2 is an optionally substituted heterocyclic ring, R.sub.3 is alkyl, cycloalkyl or optionally substituted amino, R.sub.5 is an aliphatic group, R.sub.6 is H, an optionally substituted aliphatic group or a cycloalkyl group, or R.sub.3 and R.sub.5 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached form a heterocyclic ring optionally substituted by alkyl and R.sub.7 is optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkoxycarbonyl, trifluoromethyl or cyano have utility as hypoglycemic agents.
    Type: Grant
    Filed: December 28, 1989
    Date of Patent: June 29, 1993
    Assignee: The Boots Company plc
    Inventor: Balasubramanian Gopalan
  • Patent number: 5212170
    Abstract: The compounds ##STR1## in which Z is ##STR2## where R.sup.4 is --H or alkyl; q is one of the integers 0, 1 or 2; Y is H.sub.2 or O; or Z, taken with R.sup.1 forms ##STR3## R.sup.1 is hydrogen or alkyl or combined with Z as described above; R.sup.2 and R.sup.3 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, carbamoyl or sulfonamido or R.sup.2 and R.sup.3, taken together are methylenedioxy, ethylenedioxy or propylenedioxy; m is one of the integers 1, 2 or 3; n is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are antipsychotic, antidepressant and anxiolytic agents useful in relieving the symptoms of these disease states.
    Type: Grant
    Filed: May 13, 1992
    Date of Patent: May 18, 1993
    Assignee: American Home Products Corporation
    Inventor: Gary P. Stack
  • Patent number: 5208339
    Abstract: A nitrogen-containing perfluoroalkanoyl peroxide is provided which is represented by the formula: ##STR1## wherein Rf.sub.1 and Rf.sub.2 independently stand for an alkyl group of 1 to 5 carbon atoms, provided that Rf.sub.1 and Rf.sub.2 are joined to each other in one of the three patterns of union, 1) direct union, 2) union through the medium of an oxygen atom or 3) union through the medium of a nitrogen atom to form one of the three rings, i.e. five-membered ring, six-membered ring or seven-membered ring.
    Type: Grant
    Filed: September 8, 1992
    Date of Patent: May 4, 1993
    Assignees: Agency of Industrial Science & Technology, Ministry of International Trade & Industry
    Inventors: Haruhiko Fukaya, Takashi Abe, Eiji Hayashi, Yoshio Hayakawa
  • Patent number: 5192799
    Abstract: Amine represented by the following formula (1), or their acid addition salts or their quaternary ammonium salts. ##STR1## The amines of formula (1) or their pharmaceutically acceptable acid addition salts or quaternary ammonium salts are useful for the treatment and prevention of heart diseases of animals, particularly arrhythima, myocardial infarction, angina pectoris and heart failure and psychoneurological diseases.
    Type: Grant
    Filed: June 5, 1992
    Date of Patent: March 9, 1993
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Ikuo Tomino, Masaharu Ishiguro, Takumi Kitahara, Keiichi Yokoyama, Noriaki Kihara, Joji Kamiya, Kanji Yoshihara, Masaaki Ishii, Akira Mizuchi, Kazutoshi Horikomi, Akira Awaya, Takuo Nakano
  • Patent number: 5180736
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 19, 1993
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5179205
    Abstract: Heterocyclic (poly)peroxycarboxylic acids having a N-amidic heteroatom, which have the formula:R--(CH.sub.2) .sub.m --R' (I)wherein: R and R', alike or different from each other, represent hydrogen atoms or a group: ##STR1## with the proviso that at least one of R and R' shall be different from H, and wherein the other symbols have the following meaning:R" represents a hydrogen atom or any other substituent non-reactive in the presence of the active oxygen of the peroxycarboxylic group and/or under the preparation conditions;m represents a number between 1 to 12;n represents a number selected from 0, 1 and 2;p represents a number between 1 and 3;their process of preparation and their use as bleaching agents.
    Type: Grant
    Filed: April 18, 1991
    Date of Patent: January 12, 1993
    Assignee: Ausimont S.r.l.
    Inventors: Carlo Venturello, Claudio Cavalotti
  • Patent number: 5143922
    Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic acitvity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: November 20, 1990
    Date of Patent: September 1, 1992
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
  • Patent number: 5142048
    Abstract: The invention relates to novel intermediate compounds for preparation of novel amino acid derivatives having renin inhibiting activity.
    Type: Grant
    Filed: January 8, 1990
    Date of Patent: August 25, 1992
    Assignee: Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Keiji Hemmi, Masahiro Neya, Hiroshi Marusawa, Keisuke Imai, Natsuko Kayakiri, Masashi Hashimoto
  • Patent number: 5126366
    Abstract: The compounds: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido, or sulfonamido, or R.sup.1 and R.sup.2 together form methylenedioxy, ethylenedioxy, or propylenedioxy; R.sup.3 is hydrogen or alkyl; n is one of the integers 2, 3 or 4; R.sup.4 and R.sup.5 are, independently, hydrogen, alkyl, cycloalkyl, alkanoyl, aroyl, alkylsulfonyl or arylsulfonyl, or R.sup.4 and R.sup.5 together form a 3-7 membered polymethylene ring; or a pharmaceutically acceptable salt thereof, are antipsychotic, antidepressant and anxiolytic agents useful in the treatment of multi-CNS disease states.
    Type: Grant
    Filed: June 21, 1991
    Date of Patent: June 30, 1992
    Assignee: American Home Products Corporation
    Inventors: Gary P. Stack, Magid A. Abou-Gharbia, Terrance H. Andree, Noreen T. Scherer
  • Patent number: 5120843
    Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).
    Type: Grant
    Filed: October 23, 1989
    Date of Patent: June 9, 1992
    Assignee: Upjohn
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
  • Patent number: 5116863
    Abstract: Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma and also employed in the treatment of inflammation.
    Type: Grant
    Filed: March 2, 1987
    Date of Patent: May 26, 1992
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Toshiaki Kumazawa, Shizuo Otaki, Hiroyuki Obase, Kenji Ohmori, Hidee Ishii, Haruhiko Manabe, Tadafumi Tamura, Katsuichi Shuto
  • Patent number: 5116835
    Abstract: Enzyme-inhibiting urea derivatives of dipeptides, a process for the preparation thereof, agents containing these, and the use thereof.The present invention relates to compounds of the formula I ##STR1## in which A and B denote, indpendently of one another, an amino acid,X as desired can be absent or represents --O--, --S--, --CF.sub.2 --, --CO-- or --CHR.sup.8,p and q denote, independently of one another, 0, 1, 2, 3 or 4, andR.sup.1 to R.sup.4 are defined in the description, as well as the salts thereof.The invention furthermore relates to a process for the preparation of the compounds of the formula I and to the use thereof as medicines.
    Type: Grant
    Filed: December 7, 1989
    Date of Patent: May 26, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Ruger, Hansjorg Urbach, Dieter Ruppert, Bernward Scholkens
  • Patent number: 5100911
    Abstract: Thienyloxyalkylamine derivatives of the general formula: ##STR1## wherein --O--CH.sub.2 --CH.sub.2 --NR.sub.2 R.sub.3 is in position 4 or 5 of the thiophene ring;R.sub.1 is hydrogen, halogen, CF.sub.3, alkyl or alkoxy;R.sub.2 and R.sub.3 are the same or different and are each alkyl, cycloalkyl, alkenyl or alkynyl each having up to 8 C atoms, or NR.sub.2 R.sub.3 is a 5 to 7-membered saturated heterocyclic ring optionally containing a further hetero atom which is oxygen or nitrogen optionally substituted by an alkyl group having 1 to 3 C atoms; andn is an integer of 1 to 5; as well as their acid addition salts, are suitable for treatment of heart rhythm disturbances.
    Type: Grant
    Filed: May 15, 1990
    Date of Patent: March 31, 1992
    Assignee: Ebewe Arzneimittel Gesellschaft m.b.H.
    Inventors: Dieter Binder, Gerhard Greier, Franz Rovenszky, Friedrich Hillebrand
  • Patent number: 5097027
    Abstract: Heterocyclic compounds of the formula ##STR1## are used as pigments for surface coatings and for coloring and pigmenting high molecular weight organic material.
    Type: Grant
    Filed: October 5, 1990
    Date of Patent: March 17, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventor: Hans Hochstetter
  • Patent number: 5093331
    Abstract: The present invention relates to polyoxygenated labdane-derivatives of the formula ##STR1## a process for their preparation and the use of these substances as medicaments, preferably as medicaments having a positive inotropic effect, an effect of lowering intraocular pressure and lowering blood pressure.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: March 3, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Bansi Lal, Ashok K. Gangopadbya, Alihussein N. Dohadwalla, Ramanujam Rajgopalan, Richard H. Rupp
  • Patent number: 5091526
    Abstract: Biologically active, enantiomerically substantially pure intermediates of trans-hexahydro-benzo[d]naphtho[2,1-b]azepines are prepared.The present invention involves a process for preparing compounds of the general formula 3: ##STR1## wherein: R* is ##STR2## Each R.sup.1 is independently H or alkyl; Q is methylene, --O-- or --S--;m and n are independently variable and may each have a value of 0, 1 or 2, with the provisos that the sum of m and n is not greater than 3, that m may not equal zero when Q is --O-- or --S--, and that when Q is --CH.sub.2 --, m and n cannot both be zero;X is hydrogen, halo, alkyl, alkylthio, alkylsulfinyl, alkylsufonyl, hydroxy, alkoxy or trifluoromethyl;Y is hydrogen, hydroxy, alkoxy, --OC(O)NR.sup.2 R.sup.3, --OC(O)--R.sup.9, --N(R.sup.1).sub.2, --NHC(O)R.sup.1 or --OP(O)(OH)OR.sup.1,R.sup.2 and R.sup.3 are the same or different and each is hydrogen (provided that both are not hydrogen), alkyl, aralkyl, cycloalkyl, aryl, hydroxyalkyl, or alkoxyalkyl;in addition, when one of R.sup.
    Type: Grant
    Filed: January 8, 1991
    Date of Patent: February 25, 1992
    Assignee: Schering Corporation
    Inventors: Joel G. Berger, John W. Clader
  • Patent number: 5075301
    Abstract: A furan derivative and a pharmaceutically acceptable salt thereof having gastrointestinal enterokinetic activity which is expected to be used in a broad spectrum of diseases associated with gastrointestinal dyskinesia.
    Type: Grant
    Filed: August 14, 1990
    Date of Patent: December 24, 1991
    Assignee: Kyowa Hakko Kogyo, Co., Ltd.
    Inventors: Setsuya Sasho, Shunji Ichikawa, Hiromasa Kato, Hiroyuki Obase, Katsuichi Shuto, Yoshimasa Oiji
  • Patent number: 5071853
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: December 10, 1991
    Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
  • Patent number: 5071844
    Abstract: The invention provides compounds of the formula: ##STR1## wherein k is 1, 2 or 3;m is 1, 2 or 3;n is 1, 2 or 3;p is 0, 1 or 2;X is O, S or a direct link, with the proviso that when X is O or S, n is 2 or 3;R.sup.1 is H or C.sub.1-C.sub.4 alkyl; andR.sup.2 is an optionally substituted phenyl or heteroaryl group; andpharmaceutically acceptable salts thereof.These compounds are useful for the treatment of motility disorders, particularly those of the gut such as irritable bowel syndrome.
    Type: Grant
    Filed: May 23, 1990
    Date of Patent: December 10, 1991
    Assignee: Pfizer Inc.
    Inventors: David Alker, Robert J. Bass, Peter E. Cross
  • Patent number: 5071848
    Abstract: Isothiazolo-quinoline derivatives are described which are cytotoxic for various tumor cell lines and are useful in the treatment of neoplastic diseases.
    Type: Grant
    Filed: October 23, 1989
    Date of Patent: December 10, 1991
    Assignee: Abbott Laboratories
    Inventors: Daniel Tim-Wo Chu, Jacob J. Plattner, Linus L. Shen, Larry L. Klein
  • Patent number: 5071858
    Abstract: Disclosed are 3,4-dihydro-2H-1-benzothiopyran-3-yl-methyl- and ethylamines useful as antipsychotics, processes for the preparation of said compounds, pharmaceutical compositions containing same, and a method of treating psychotic disorders by administering said compounds.
    Type: Grant
    Filed: October 12, 1990
    Date of Patent: December 10, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Alan J. Hutchison
  • Patent number: 5068231
    Abstract: A method of treating animals to obtain muscle relaxation and/or to relieve anxiety is disclosed utilizing novel and known 3-aryloxy and 3-arylthioazetidinecarbonxamides having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo substituted pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, aryl, allyl groups, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloakylloweralkyl, arylloweralkyl and diloweralkylaminoalkyl, and R.sup.1 and R.sup.2 when taken together with the adjacent nitrogen atom may form a heterocyclic amine radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof and pharmaceutical salts thereof and hydrates thereof when they are possible.
    Type: Grant
    Filed: October 22, 1986
    Date of Patent: November 26, 1991
    Assignee: A. H. Robins Company Incorporated
    Inventors: Chandler R. Taylor, Jr., Albert D. Cale. Jr., David N. Johnson, Harold F. Stauffer. Jr.
  • Patent number: 5061311
    Abstract: Novel herbicides and plant growth regulants of the formula ##STR1## in which R.sup.1 represents hydrogen alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, halogenoalkinyl, alkoxyalkyl, alkoxy, cycloalkylalkyl or cycloalkyl, or represents in each case optionally substituted aralkyl or aryl,R.sup.2 represents a radical ##STR2## or represents a radical --S(O).sub.n --R.sup.7, R.sup.3 and R.sup.
    Type: Grant
    Filed: March 16, 1988
    Date of Patent: October 29, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Kurt Findeisen, Markus Lindig, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen, Harry Strang
  • Patent number: 5061813
    Abstract: Novel compounds are disclosed having the formula ##STR1## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are as defined herein. These compounds are useful, for example, as cardiovascular agents and especially as anti-ischemic agents.
    Type: Grant
    Filed: April 2, 1990
    Date of Patent: October 29, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 5059620
    Abstract: The present invention relates to new compounds of the formula ##STR1## wherein X is ##STR2## wherein R.sub.1 is hydrogen, lower alkyl, phenyl, benzyl, cinnamoyl, thiophene, furan, pyrrole, imidazole, pyrazole oxazole or thiazole; W is hydrogen or hydroxy; (Y).sub.A is positioned ortho to W and is an aminoloweralkyl having the formula --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 are the same or different and may be lower alkyl or R.sub.2 and R.sub.3 may together with N form a pyrrolidine, piperidine or azepine ring, and A is 2; n and m are independently from 0 to 5; and R is straight or branched C.sub.1 -C.sub.10 alkyl, straight or branched C.sub.3 -C.sub.10 cycloalkyl, straight or branched C.sub.2 -C.sub.4 alkenyl or straight or branched C.sub.2 -C.sub.4 alkynyl, or a pharmaceutically acceptable salt thereof.These compounds are useful in the treatment of various cardiac arrhythmias.
    Type: Grant
    Filed: April 7, 1988
    Date of Patent: October 22, 1991
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: David M. Stout, William L. Matier, Lawrence A. Black
  • Patent number: 5047406
    Abstract: Substituted cyclohexanols and cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
    Type: Grant
    Filed: May 2, 1990
    Date of Patent: September 10, 1991
    Assignee: Warner-Lambert Co.
    Inventors: Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
  • Patent number: 5047549
    Abstract: Derivatives of pravastatin are provided which are useful in inhibiting cholesterol biosynthesis and in preparing radiolabeled compounds useful in the radioimmunoassay (RIA) of pravastatin and derivatives thereof. The pravastatin derivatives have the structure ##STR1## wherein R is hydroxy, lower alkylamine, arylamine, arylalkylamine or heterocyclic alkylamine such as histamine, tyramine, O-benzyltyramine, methyl tyrosinate as well as iodinated derivatives thereof.
    Type: Grant
    Filed: April 17, 1989
    Date of Patent: September 10, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard A. DiPietro, Jan-I Tu, Noor Z. Turabi
  • Patent number: 5043459
    Abstract: This invention relates to novel saccharoascorbic acid derivatives and their production. The derivatives are represented by the general formula set forth below, for example, an amido, a thioester or carboxylic ester of saccharoascorbic acid, and their salts.The compounds of the present invention are useful for food additives as antioxidants, an intermediate for the production of dichiral compounds and medicines having antithrombotic activity. ##STR1## wherein Z represents ##STR2## --SR.sub.6 or --OR.sub.7, R.sub.4 and R.sub.5 independently represent hydrogen or a hydrocarbon group of 1 to 24 carbon atoms, or R.sub.4 and R.sub.5 may together form --CH.sub.2 --.sub.n in which n is an integer of 4 to 7, R.sub.6 represents a hydrocarbon group of 1 to 24 carbon atoms, R.sub.7 represents hydrogen or a hydrocarbon group of 1 to 24 carbon atoms, R.sub.1, R.sub.2 and R.sub.3 independently represent hydrogen, an acyl group of 1 to 18 carbon atoms or a hydrocarbon group of 1 to 24 carbon atoms, and .about.
    Type: Grant
    Filed: January 31, 1990
    Date of Patent: August 27, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Koichi Matsumura, Yoshihiro Sugihara, Yoshiaki Shimizu, Kouichi Iida, Toshiro Yamashita
  • Patent number: 5041545
    Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: August 20, 1991
    Assignee: Atochem North America, Inc.
    Inventor: Terry N. Myers
  • Patent number: 5028711
    Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: July 2, 1991
    Assignee: Beiersdorf Aktiengesellschaft
    Inventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
  • Patent number: 4999350
    Abstract: The present invention relates to (RS)-2-(2,3-dihydro-5-hydroxy-4,6,7-trimethylbenzofuranyl) acetic acids and 2-(2,3-dihydro-5-acyloxy-4,6,7-trimethylbenzofuranyl) acetic acids and esters thereof, the process for producing them and their relevant therapeutical use as mucoregulators and antiischemic agents.
    Type: Grant
    Filed: April 13, 1989
    Date of Patent: March 12, 1991
    Assignee: Biomedica Foscama Industria Chimico-Farmaceutica S.p.A.
    Inventors: Mario Brufani, Stefano Ceccarelli, Patrizia Giannetti, Agnese Paesano, Romolo Scuri, Sergio Zanarella
  • Patent number: 4996318
    Abstract: The amino-9,10-secosteroids ##STR1## of the present invention contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain and are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc.
    Type: Grant
    Filed: September 19, 1989
    Date of Patent: February 26, 1991
    Assignee: The Upjohn Company
    Inventors: Martin Gall, Robert I. Higuchi
  • Patent number: 4994463
    Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: December 8, 1988
    Date of Patent: February 19, 1991
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
  • Patent number: 4994486
    Abstract: Novel compounds of Formula (I): ##STR1## or pharmaceutically acceptable salts, esters and amides thereof, wherein A is O, C, CH or CH.sub.2, n is 0 or 1, and the dotted line is a single bond when A is O or CH.sub.2 and a double bond when A is CH or when n=0, A is C andR.sub.6 and A taken together form a nitrogen-containing heterocycle;R is hydrogen, lower alkyl or a readily cleavable group;R.sub.1 is selected from hydrogen, halogen, lower alkyl, haloalkyl and lower alkoxy;R.sub.2 is selected from hydrogen, halogen, lower alkyl and haloalkyl or, taken together with R.sub.8, forms a fused ring;R.sub.3 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl or arylalkyl or, taken together with R.sub.4, forms a spirocycloalkyl or, taken together with R.sub.5, forms a fused cycloalkyl;R.sub.4 is hydrogen or alkyl or, taken together with R.sub.3, forms a spirocycloalkyl;R.sub.5 is hydrogen or alkyl or, taken together with R.sub.3, forms a fused cycloalkyl;R.sub.
    Type: Grant
    Filed: December 22, 1989
    Date of Patent: February 19, 1991
    Assignee: Abbott Laboratories
    Inventors: Robert W. Schoenleber, John W. Kebabian, Michael P. DeNinno, Michael R. Michaelides, Sheela A. Thomas
  • Patent number: RE33906
    Abstract: A compound of formula (I): ##STR1## or a salt or solvate thereof in which R. CO is an acyl group containing a substituted or unsubstituted carbocyclic or heterocyclic aromatic ring, R.sub.1 and R.sub.2 are independently C.sub.1-6 alkyl or together form a C.sub.3-6 polymethylene or alkylene group, and p is 1, 2, 3 or 4, is useful for treating pain.
    Type: Grant
    Filed: August 3, 1990
    Date of Patent: April 28, 1992
    Assignee: Dr.Lo.Zambeletti S.p.A.
    Inventors: Vittorio Vecchietti, Massimo Signorini, Antonio Giordani