Spiro Patents (Class 544/6)
  • Patent number: 6060469
    Abstract: The present invention relates to compounds of formula (I), ##STR1## wherein R.sup.1 represents halogen, hydroxy, C.sub.1-6 alkyl group optionally substituted by one or three fluorine atoms, C.sub.1-6 alkoxy group optionally substituted by one to three fluorine atoms, or C.sub.1-6 alkylthio optionally substituted by one to three fluorine atoms; R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or when R.sup.2 is adjacent to R.sup.1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R.sup.3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; m is 0-3 and n is 0-3, with the proviso that the sum total of m+n is 2 or 3; p is zero or 1; q is 1 or 2; and when m is 1 and n is 1 or 2, the broken line represents an optional double bond; R.sup.4, R.sup.5, R.sup.6, R.sup.9 and R.sup.
    Type: Grant
    Filed: May 18, 1998
    Date of Patent: May 9, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Timothy Harrison, Christopher John Swain, Brian John Williams
  • Patent number: 6013652
    Abstract: Disclosed are spiro-substituted azacycles of formula I are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula I are shown to be neurokinin antagonists.
    Type: Grant
    Filed: December 4, 1997
    Date of Patent: January 11, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Yuan-Ching P. Chiang, Patrick T. Dunn, Hiroo Koyama
  • Patent number: 6011150
    Abstract: There is disclosed an azetidinone compound of the formula [I]: ##STR1## wherein Ring B is a benzene ring which may have substituent(s), R.sup.1 is a hydroxy-substituted lower alkyl group which may have substituent(s), X is oxygen atom and the like, Y is oxygen atom and the like, and Z is a methylene group which may have substituent(s), which is useful as a synthetic intermediate of the 1.beta.-methylcarbapenem-type antibacterial agent.
    Type: Grant
    Filed: May 15, 1995
    Date of Patent: January 4, 2000
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Tameo Iwasaki, Kazuhiko Kondo
  • Patent number: 6002000
    Abstract: Methods are disclosed for determining an analyte in a medium suspected of containing the analyte. One method comprises providing (1) combining a medium suspected of containing the analyte and a novel chemiluminescent compound, (2) combining a means for chemically activating the chemiluminescent compound; and (3) detecting the amount of luminescence generated by the chemiluminescent compound. The amount of luminescence generated is related to the amount of analyte in the medium. The chemiluminescent compound can be chemically activated by hydrogen peroxide. Compositions and kits are also disclosed.
    Type: Grant
    Filed: June 11, 1996
    Date of Patent: December 14, 1999
    Assignee: Dade Behring Marburg GmbH
    Inventors: Sharat Singh, Rajendra Singh, Frank Meneghini, Edwin F. Ullman
  • Patent number: 5994350
    Abstract: The subject of the invention is indolin-2-one derivatives of formula: ##STR1## in which: W represents a --CH.sub.2 -- or --SO.sub.2 -- group;Cy forms, with the carbon to which it is bonded, a non-aromatic, saturated or unsaturated C.sub.3 -C.sub.12 hydrocarbon ring which is optionally condensed or substituted by one or a number of (C.sub.1 -C.sub.7)alkyl groups, it being possible for the said groups to substitute the same carbon atom one or a number of times, or by a C.sub.3 -C.sub.6 spirocycloalkyl;T represents a (C.sub.1 -C.sub.4)alkylene which is optionally interrupted by a (C.sub.3 -C.sub.6)cycloalkylene, the said alkylenes optionally being substituted one or a number of times on the same carbon atom by a (C.sub.1 -C.sub.3)alkyl; or alternatively T represents a direct bond;Z represents in particular an amino group;R.sub.1 and R.sub.2, as well as R.sub.3 and R.sub.4, are either hydrogen or substituents, such as, for example, a halogen, an alkyl, and the like.
    Type: Grant
    Filed: April 17, 1998
    Date of Patent: November 30, 1999
    Assignee: Sanofi-Synthelabo
    Inventors: Loic Foulon, Georges Garcia, Claudine Serradeil-Le Gal, Gerard Valette
  • Patent number: 5981523
    Abstract: This invention provides thiomorpholinone compounds useful for treating multiple sclerosis of formula I wherein:R.sup.1 and R.sup.2 are each independently selected from C.sub.1 -C.sub.8 alkyl; C.sub.2 -C.sub.8 alkenyl; C.sub.2 -C.sub.8 alkynyl; C.sub.1 -C.sub.8 alkyloxy; C.sub.1 -C.sub.8 alkylthio; trifluoromethyl; C.sub.1 -C.sub.4 alkyl substituted with phenyl; phenyl; F; Cl; NO.sub.2 ; phenoxy; C.sub.1 -C.sub.4 alkyl substituted with phenoxy; thiophenyl; C.sub.1 -C.sub.4 alkylthiophenyl; --COOR.sup.7 ; --N(R.sup.7).sub.2 or --N(R.sup.7)SO.sub.2 R.sup.7 where each R.sup.7 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.3 is H or C.sub.1 -C.sub.4 alkyl;R.sup.4 and R.sup.5 are each individually H, or when taken together form a bond;R.sup.6 is H; C.sub.1 -C.sub.8 alkyl; C.sub.2 -C.sub.8 alkenyl; C.sub.2 -C.sub.8 alkynyl; --SO.sub.2 CH.sub.3 ; --(CH.sub.2).sub.n NR.sup.8 R.sup.9 ; --(CH.sub.2).sub.n CO.sub.2 R.sup.8 ; --(CH.sub.2).sub.n OR.sup.8 where n is an integer from 1 to 6, both inclusive, and R.
    Type: Grant
    Filed: August 14, 1997
    Date of Patent: November 9, 1999
    Assignee: Eli Lilly and Company
    Inventors: Jill A Panetta, Michael L Phillips
  • Patent number: 5945413
    Abstract: This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: August 31, 1999
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Govinda Rao Bhisetti, Christopher Todd Baker, Andrew Spaltenstein
  • Patent number: 5929072
    Abstract: A pharmaceutical compound having the formula: ##STR1## in which n is 1 or 2, m is 1 or 2, p is 1 to 6, q is 0 or 1 to 3,R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-4 alkyl,R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted phenyl-C.sub.1-4 alkyl, or R.sup.3 and R.sup.4 together form an alkylene link of formula --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, or R.sup.4 and R.sup.5 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group,R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, carboxy, hydroxy, cyano, halo, trifluoromethyl, nitro or amino,the dotted line represents an optional double bond, andthe fluorine atom is attached at the 6 or 7-position;and salts and esters thereof.
    Type: Grant
    Filed: August 21, 1998
    Date of Patent: July 27, 1999
    Assignee: Eli Lilly and Company Limited
    Inventor: John Fairhurst
  • Patent number: 5922748
    Abstract: Compounds of formula (I) ##STR1## wherein R and R.sup.1 are hydrogen, C.sub.1-4 alkyl or are linked to form a ring,A is a cycloalkyl or alkyl-cycloalkyl group,n is an integer from 0 to 3,W is an optionally substituted 5-or 6-membered heterocyclic ring; or W is an optionally substituted aryl, heteroaryl, aryloxy or thiophenoxy group; orW is a group --SO.sub.2 NR.sup.6 R.sup.7 --NHC(O)R.sup.6 R.sup.7 or --C(O)NHR.sup.6 R.sup.7 ; are useful in treating clinical conditions for which a "5-HT.sub.1 -like" receptor agonist is indicated.
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: July 13, 1999
    Assignee: Glaxo Wellcome Inc.
    Inventors: Robert Charles Glen, David Lawrence Selwood, Graeme Richard Martin, Christopher James Foster
  • Patent number: 5874382
    Abstract: Compounds of Formula I and II, and their agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein X is a direct bond; O; S; NH; N(C.sub.1 -C.sub.3 alkyl); N(C.sub.1 -C.sub.3 haloalkyl); or N(allyl);R.sup.1 is H; F; Cl; or Br;R.sup.2 is H; F; Cl; Br; CF.sub.3 ; nitro; or cyano;R.sup.4 is H; C.sub.1 -C.sub.3 alkyl; or halogen;R.sup.5 is H; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl; halogen; S(O).sub.2 (C.sub.1 -C.sub.6 alkyl); or C(.dbd.O)R.sup.8 ; orR.sup.4 and R.sup.5 are taken together along with the carbon to which they are attached to form a spiro-cyclopropane ring;and R.sup.3, R.sup.8, and J are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formulae I and II and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I or II.
    Type: Grant
    Filed: January 23, 1998
    Date of Patent: February 23, 1999
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Balreddy Kamireddy, William Mark Murray
  • Patent number: 5783579
    Abstract: The invention relates to compounds of the formula ##STR1## wherein Z, R.sub.c, y, m, u, Ar.sub.2, n, X, R.sub.c', I and Ar.sub.2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: July 21, 1998
    Assignee: Schering Corporation
    Inventor: Kevin D. McCormick
  • Patent number: 5728693
    Abstract: Arthropodicidal compounds, compositions and use of compounds having the formula ##STR1##
    Type: Grant
    Filed: June 25, 1996
    Date of Patent: March 17, 1998
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Thomas Martin Stevenson
  • Patent number: 5726126
    Abstract: There is provided a 1-(3-heterocyclylphenyl)-s-triazine-2, 4,6-oxo or thiotrione compound having the structural formula I ##STR1## Further provided are a composition and a method comprising that compound for the control of undesirable plant species.
    Type: Grant
    Filed: November 26, 1996
    Date of Patent: March 10, 1998
    Assignee: American Cyanamid Company
    Inventors: Alvin Donald Crews, Jr., Philip Mark Harrington, Gary Mitchell Karp, Mark Christopher Manfredi, Michael Anthony Guaciaro
  • Patent number: 5696145
    Abstract: The present invention relates to 1-benzyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## to their preparation and to the pharmaceutical compositions in which they are present. These derivatives have an affinity for the vasopressin and oxytocin receptors.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 9, 1997
    Assignee: Sanofi
    Inventors: Loic Foulon, Georges Garcia, Daniel Mettefeu, Claudine Serradeil-Legal, Gerard Valette
  • Patent number: 5679805
    Abstract: A naphthopyran compound represented by the formula: ##STR1## wherein A and B are each selected from the following group: a substituted divalent cyclic radical, a substituted divalent aromatic radical, and a substituted divalent fused heterocyclic radical.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 21, 1997
    Assignee: Vision-Ease Lens, Inc.
    Inventor: Frank J. Hughes
  • Patent number: 5597819
    Abstract: New benzothiazine derivatives corresponding to the general formula I: ##STR1## in which: X represents halogen,n represents 0, 1, or 2,B represents the following formula: ##STR2## in which: R.sub.1 & R.sub.2 together with the carbons to which they are attached form a 6-carbon-atom aromatic ring which is optionally substituted by a group X' representing halogen, andY represents the radical --(SO.sub.2).sub.x --Alk--Z, x, Alk, and Z are as defined in the specification;as well as their possible stereoisomers, epimers, N-oxides and pharmaceutically-acceptable acid or base addition salts; and medicinal products containing the same, useful in the treatment of inflammatory disorders requiring an inhibitor of cytokines.
    Type: Grant
    Filed: February 13, 1995
    Date of Patent: January 28, 1997
    Assignee: Adir Et Compagnie
    Inventors: Jean-Daniel Brion, Anne-Marie Chollet, Luc Demuynck, Lucy De Montarby, Yves Rolland, Jacqueline Bonnet, Pietro Ghezzi, Armel Fradin
  • Patent number: 5591848
    Abstract: New intramolecular charge-transfer organic dyes are described. The design of these molecules is based on the phenomenon of spiroconjugation, and it provides a modular approach to the preparation of unique materials with interesting optical properties. In the dyes of the invention, the lowest unoccupied molecular orbital (LUMO) of the acceptor part (based on indandione) is spiroconjugated with the highest unoccupied molecular orbital (HOMO) of the donor part (amines, alcohols and thiols). The interaction between the donor and acceptor is controlled by the energy and symmetry of the frontier orbitals. The novel dyes described herein, with predictable and tunable optical properties, can be used in many optical applications including nonlinear optics (NLO).
    Type: Grant
    Filed: October 7, 1994
    Date of Patent: January 7, 1997
    Assignee: The Penn State Research Foundation
    Inventor: Przemyslaw B. Maslak
  • Patent number: 5589489
    Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: December 31, 1996
    Assignee: Zeneca Limited
    Inventors: Ashokkumar B. Shenvi, Robert T. Jacobs, Scott C. Miller, Cyrus J. Ohnmacht, Jr., Chris A. Veale
  • Patent number: 5578593
    Abstract: There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: November 3, 1993
    Date of Patent: November 26, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Meng-Hsin Chen, David B. R. Johnston, Ravi P. Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang
  • Patent number: 5559233
    Abstract: The invention relates to processes for preparing N-substituted heterocyclic compounds of formula (I) ##STR1##
    Type: Grant
    Filed: June 30, 1994
    Date of Patent: September 24, 1996
    Assignee: Sanofi
    Inventors: Claude Bernhart, Jean-Claude Breliere, Jacques Clement, Dino Nisato, Pierre Perreault, Claude Muneaux, Yvette Muneaux
  • Patent number: 5550229
    Abstract: Novel process for preparing azetidinone compound of the formula [III]: ##STR1## wherein R.sup.1 is H or lower alkyl, R.sup.2 and R.sup.3 combine together with the adjacent nitrogen to form heterocyclic group, and R.sup.4 is protected or unprotected hydroxy-substituted lower alkyl, which comprises reacting an alkanamide compound of the formula [I]: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a compound of the formula [II]: ##STR3## wherein L.sup.1 is a leaving group and R.sup.4 is the same as defined above, in the presence of a base, said compound [III] being useful as synthetic intermediate for 1-methylcarbapenem derivative having excellent antibacterial activity.
    Type: Grant
    Filed: June 21, 1994
    Date of Patent: August 27, 1996
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Tameo Iwasaki, Kazuhiko Kondo, Hiroshi Ohmizu
  • Patent number: 5545834
    Abstract: Methods are disclosed for determining an analyte in a medium suspected of containing the analyte. One method comprises providing (1) combining a medium suspected of containing the analyte and a novel chemiluminescent compound, (2) combining a means for chemically activating the chemiluminescent compound; and (3) detecting the amount of luminescence generated by the chemiluminescent compound. The amount of luminescence generated is related to the amount of analyte in the medium. The chemiluminescent compound can be chemically activated by hydrogen peroxide. Compositions and kits are also disclosed.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: August 13, 1996
    Assignee: Behringwerke AG
    Inventors: Sharat Singh, Rajendra Singh, Frank Meneghini, Edwin F. Ullman
  • Patent number: 5536716
    Abstract: There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: November 3, 1993
    Date of Patent: July 16, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Meng-Hsin Chen, David B. R. Johnston, Ravi P. Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang
  • Patent number: 5457199
    Abstract: The present invention relates to novel piperidine compounds of the formula (I) ##STR1## in which X.sub.1, X.sub.2, X.sub.3 and n are as defined in the text. The compounds of the invention can be used as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials, in particular synthetic polymers.
    Type: Grant
    Filed: July 11, 1994
    Date of Patent: October 10, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Roberto Scrima, Graziano Zagnoni
  • Patent number: 5447927
    Abstract: Fungicidally active compounds of the formula ##STR1## in which X represents oxygen or sulphur,R represents cycloalkyl, or represents optionally substituted aryl, or represents the radical ##STR2## R.sup.1 and R.sup.2 each independently is hydrogen or an organic radical, or together with the nitrogen atom form a heterocyclic radical,R.sup.3 represents hydrogen, alkyl or optionally substituted aryl, andR.sup.4 represents alkyl or cycloalkyl, or represents optionally substituted aryl,but wherein R.sup.3 and R.sup.4 may not simultaneously represent methyl,and acid addition salts thereof, as well as intermediates therefor.
    Type: Grant
    Filed: July 25, 1994
    Date of Patent: September 5, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Kramer, Joachim Weissmuller, Dieter Berg, Wilhelm Brandes, Stefan Dutzmann
  • Patent number: 5407943
    Abstract: Quinolone carboxylic acids of the formula ##STR1## wherein R.sup.1, R.sup.2, A and Y are as defined herein, and R.sup.3 is ##STR2## have antibacterial properties.
    Type: Grant
    Filed: November 22, 1993
    Date of Patent: April 18, 1995
    Assignee: Pfizer Inc.
    Inventor: Bingwei V. Yang
  • Patent number: 5376660
    Abstract: Fungicidally active compounds of the formula ##STR1## in which X represents oxygen or sulphur,R represents cycloalkyl, or represents optionally substituted aryl, or represents the radical ##STR2## R.sup.1 and R.sup.2 each independently is hydrogen or an organic radical, or together with the nitrogen atom form a heterocyclic radical,R.sup.3 represents hydrogen, alkyl or optionally substituted aryl, andR.sup.4 represents alkyl or cycloalkyl, or represents optionally substituted aryl,but wherein and R.sup.3 and R.sup.4 may not simultaneously represent methyl,and acid addition salts thereof, as well as intermediates therefore.
    Type: Grant
    Filed: August 3, 1992
    Date of Patent: December 27, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Kramer, Joachim Weissmuller, Dieter Berg, Wilhelm Brandes, Stefan Dutzmann
  • Patent number: 5373009
    Abstract: A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independently, halo, trifluoromethyl, cyano, nitro, alkyl, alkoxy, --CO.sub.2 H, alkylcarbonyl, alkylcarbonyloxy, alkoxycarbonyl, mono- or di-alkylaminocarbonyl, or mono- or di-alkylaminocarbonyloxy;m is 0, 1 or 2 andR.sup.3 is alkyl;n and p are, independently, 0, 1 or 2;X is O, S or CR.sup.4 R.sup.5,where R.sup.4 and R.sup.5 are, independently, H or alkyl or R.sup.4 and R.sup.5 together with the interposed carbon atom form a 3 to 8 membered carbocyclic ring, are anti-cholesterolemic agents.
    Type: Grant
    Filed: February 2, 1994
    Date of Patent: December 13, 1994
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Commons, Donald P. Strike
  • Patent number: 5352788
    Abstract: The invention relates to processes for preparing N-substituted heterocyclic compounds of formula (I) ##STR1## wherein the substituents are as described in the specification, and to intermediates. The compounds are useful for antagonizing angiotensin II.
    Type: Grant
    Filed: June 23, 1993
    Date of Patent: October 4, 1994
    Assignee: Elf Sanofi
    Inventors: Claude Bernhart, Jean-Claude Breliere, Jacques Clement, Dino Nisato, Pierre Perreault, Claude Muneaux, Yvette Muneaux
  • Patent number: 5329006
    Abstract: Chromogenic lactam compounds of the formula ##STR1## in which the ring A is an aromatic or heteroaromatic radical which has 6 ring atoms and may contain a fused aromatic ring, it being possible for both the ring A and the fused ring to be substituted;the ring B is an unsubstituted or substituted benzene ring;Z is ##STR2## R is hydrogen; unsubstituted or substituted C.sub.1 -C.sub.12 alkyl, cycloalkyl having 5 to 10 carbon atoms; unsubstituted or substituted aryl or aralkyl; C.sub.1 -C.sub.12 acyl; N-(lower alkyl)carbamoyl; or N-arylcarbamoyl which is unsubstituted or substituted on the ring;Q is C.sub.1 -C.sub.12 alkylene, aryl-C.sub.1 -C.sub.4 alkylene, 1,2-cycloalkylene, 1,2- or 1,8-arylene or aralkylene; andX.sub.1 and X.sub.2, independently of one another, are each hydrogen; unsubstituted or substituted alkyl having a maximum of 12 carbon atoms; acyl having 1 to 8 carbon atoms; cycloalkyl having 5 to 10 carbon atoms; or unsubstituted or ring-substituted aralkyl or aryl; or (X.sub.1 and X.sub.
    Type: Grant
    Filed: September 6, 1991
    Date of Patent: July 12, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Baumann, Ian J. Fletcher
  • Patent number: 5296477
    Abstract: Compounds of general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, n, X and A are defined in the description.Medicinal products containing the same are useful as antidepressives or anxiolytics due to their 5-HT1A receptor agonist activity.
    Type: Grant
    Filed: December 1, 1992
    Date of Patent: March 22, 1994
    Assignee: Adir et Compagnie
    Inventors: Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
  • Patent number: 5286723
    Abstract: The present invention relates to spiro compounds of general formula I: ##STR1## wherein the substituents are herein below defined. The present invention relates to antibacterial spiro compounds which are of value as drugs for humans, veterinary drugs or drugs for use in fish culture or as preservatives, and to antibacterial compositions containing one or more of the same compounds as active ingredients.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: February 15, 1994
    Assignee: Daiichi Seiyaku Co., Ltd.
    Inventors: Isao Hayakawa, Shohgo Atarashi, Masazumi Imamura, Youichi Kimura
  • Patent number: 5204474
    Abstract: 2,6-Diarylpiperidin-1-yl substituted 2-butene stabilizers of the formula I or IIT--CH.sub.2 --CH.dbd.CH--CH.sub.2 --T (I)T--CH.sub.2 --CH.dbd.CH--CH.sub.2 --N(E.sub.1)(E.sub.2) (II)where T is a 2,6-diarylpiperidin-1-yl moiety and E.sub.1 and E.sub.2 are independently alkyl, cycloalkyl, aralkyl or aryl, are effective in stabilizing organic materials against the deleterious effects of oxygen, heat and actinic radiation.
    Type: Grant
    Filed: June 3, 1991
    Date of Patent: April 20, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Glen T. Cunkle, Joseph E. Babiarz
  • Patent number: 5177216
    Abstract: The present invention provides a new diastereomer ester compound which is useful as an intermediate in the making of an optically active 3,4-dihydro-3,4-epoxy-2H-1-benzopyran compound.
    Type: Grant
    Filed: May 13, 1991
    Date of Patent: January 5, 1993
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventor: Tsutomu Yamanaka
  • Patent number: 5149823
    Abstract: A novel class of sulfonamoyl-substituted 1,6-diaza[4.4]spirodilactams, having a sulfonamoyl substituent on the hydrocarbyl group attached to each spiro ring nitrogen atom, is useful for the preparation of polymers, including polyamides and as latent curing agents for epoxy resins.
    Type: Grant
    Filed: August 9, 1990
    Date of Patent: September 22, 1992
    Assignee: Shell Oil Company
    Inventor: Pen-Chung Wang
  • Patent number: 5109006
    Abstract: This invention relates to novel derivatives of 1,7'-[imidazo-[1,2-a]pyridine]5'-(6'H)ones, to the method for their preparation and to their use as anti-hypertensive, anxiety, anti-depressant and anti-migraine agents, and to their use as appetite regulators useful for the treatment of anorexia and obesity.
    Type: Grant
    Filed: August 22, 1991
    Date of Patent: April 28, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Marcel Hibert
  • Patent number: 5104872
    Abstract: Compound of the general formula (I), which is useful as an agricultural and horticultural fungicide, an agricultural and horticultural fungicidal composition containing said compound, use of said composition for controlling plant disease, and process for the production of said compound: ##STR1## wherein ##STR2## shows a case in which R.sup.3 and R.sup.4 together form a cyclic substituent, and R.sup.1 and R.sup.4 are substituents disclosed in the specification.
    Type: Grant
    Filed: August 15, 1990
    Date of Patent: April 14, 1992
    Assignee: Nihon Hohyaku Co., Ltd.
    Inventors: Kenji Tsubata, Nobuyuki Niino, Katsutoshi Endo, Yoshinobu Yamamoto, Hideo Kanno
  • Patent number: 5084454
    Abstract: The present invention relates to compounds having the following formula (I) ##STR1## wherein X represents --O-- or --S--;each of R and R.sub.1, independently, is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino, nitro or trihalo-C.sub.1 -C.sub.6 alkyl;each of R.sub.2 and R.sub.3, independently, is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or phenyl-C.sub.1 -C.sub.6 alkyl; or R.sub.2 and R.sub.3, taken together with the nitrogen atom to which they are linked, form an unsubstituted or substituted, 6-membered, saturated, heteromonocyclic ring optionally containing a further heteroatom chosen from oxygen, sulphur and nitrogen;each of R.sub.4 and R.sub.5, independently, is hydrogen, halogen, nitro, amino or trihalo-C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof. The compounds of the invention are useful in therapy as major tranquilizers e.g., in the management of psychotic disorders.
    Type: Grant
    Filed: October 11, 1989
    Date of Patent: January 28, 1992
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Mario Varasi, Piero Melloni, Maria A. Cervini, Alberto Bonsignori, Roberto Commisso
  • Patent number: 5059689
    Abstract: Compounds which contain at least one group of the formula I ##STR1## in which X is a group which completes the ring to form a piperidine ring, are effective stabilizers for organic materials against damage by light, oxygen and heat.
    Type: Grant
    Filed: January 30, 1989
    Date of Patent: October 22, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Jean Rody, Gerhard Rytz, Mario Slongo
  • Patent number: 5051417
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, ##STR1## in which, R.sub.1 is hydrogen or lower alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.4 and R.sub.4 ' together form a group .dbd.N--Ra, or .dbd.CRaRb, where Ra is hydrogen, lower alkyl, aryl, aryloxy, lower alkylcarbonyl, arylcarbonyl, aryloxycarbonyl, lower alkoxy, lower alkoxy carbonyl, lower alkoxy carbonyl alkoxy, lower thioalkoxy, hydroxy, nitrile, heterocyclyl, or --NRcRd, where Rc is hydrogen, lower alkyl, cycloalkyl, aryl, aralkyl, lower alkylcarbonyl, arylcarbonyl, aminocarbonyl, aminothiocarbonyl, aminoiminocarbonyl, lower alkoxycarbonyl, lower alkoxythiocarbonyl, aryloxycarbonyl, thiocarbonyl, nitrile, carboxyl, heterocyclyl or heterocyclylcarbonyl, and Rd is hydrogen or lower alkyl; Rb is hydrogen, lower alkyl, aryl, lower alkylcarbonyl, lower alkoxycarbonyl, nitrile or nitro;or R.sub.4 is --NH--Ra, in which Ra is as defined above, and R.sub.4 ' is hydrogen or lower alkyl;each of R.sub.3 and R.sub.
    Type: Grant
    Filed: July 13, 1989
    Date of Patent: September 24, 1991
    Assignee: Les Laboratoires Beecham S.A.
    Inventors: Guy Nadler, Michel Martin, Richard Zimmermann
  • 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: 5013827
    Abstract: Triggerable dioxetanes with a fluorescent molecule containing group bonded or tethered in the dioxetane so as to produce fluorescence from the group are described. The compounds are useful in immunoassays and in probes using enzymes or other chemicals for triggering the dioxetanes to produce light from the fluorescent molecule in the group as a signal.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: May 7, 1991
    Assignee: Board of Governors of Wayne State University
    Inventor: Arthur P. Schaap
  • Patent number: 5000777
    Abstract: 1,5-substituted imidazole derivatives of formula I ##STR1## the stereochemically isomeric forms thereof, and the salts thereof, have useful herbicidal properties. The substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2, X.sup.3, A, L and m have the meanings defined herein.
    Type: Grant
    Filed: November 21, 1989
    Date of Patent: March 19, 1991
    Assignees: Ciba-Geigy Corporation, Janssen Pharmaceutica
    Inventors: Henry Szczepanski, Lourens Wals
  • Patent number: 4985421
    Abstract: Fungicidal substituted dioxolanylethylamine of the formula ##STR1## in which R represents alkyl, or represents in each case optionally substituted cycloalkylalkyl, aralkyl, cycloalkyl or aryl, andR.sup.1 and R.sup.2 independently of one another each represents hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, dialkoxyalkyl, hydroxyalkyl, hydroxyalkoxyalkyl, alkoxycarbonylalkyl, dioxolanylalkyl, dioxanylalkyl or oxolanylalkyl, or represents in each case optionally substituted cycloalkylalkyl, cycloalkyl, aralkyl, aralkenyl or aryl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical, which can optionally contain further hetero atoms,and acid addition salts thereof.Intermediates wherein the amino group is an electron-withdrawing leaving group are also new.
    Type: Grant
    Filed: August 17, 1989
    Date of Patent: January 15, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Kramer, Joachim Weissmuller, Dieter Berg, Wilhelm Brandes, Stefan Dutzmann
  • Patent number: 4973593
    Abstract: Compounds of the formulae: ##STR1## are useful as anti-hypertensives.
    Type: Grant
    Filed: August 4, 1987
    Date of Patent: November 27, 1990
    Assignee: Research Corporation Technologies, Inc.
    Inventor: Abram N. Brubaker
  • Patent number: 4968810
    Abstract: Arylcyclobutenealkyl ether of hydroxyaryl-substituted 1,6-diaza [4.4] spirodilactams having a hydroxyaryl substituent on each spiro ring nitrogen atom are self-curing upon application of heat to produce cured products of relatively high glass transition temperature having good physical properties.
    Type: Grant
    Filed: March 17, 1989
    Date of Patent: November 6, 1990
    Assignee: Shell Oil Company
    Inventor: Pen C. Wang
  • Patent number: 4968812
    Abstract: A novel class of bis(spirolactonelactam) compounds is produced by reaction of a primary diamine in the presence of a stoichiometric excess of a spirodilactam precursor selected from ketodiacid compounds and 1,6-dioxo [4.4] spirodilactones.
    Type: Grant
    Filed: June 23, 1989
    Date of Patent: November 6, 1990
    Assignee: Shell Oil Company
    Inventors: Pen-Chung Wang, William J. Asbell
  • Patent number: 4968811
    Abstract: Novel 1,6-diaza[4.4]spirodilactams having a hydroxyaryl substituent on each spiro ring nitrogen atom and at least one alkenyl group located on an aromatic ring carbon atom which is ortho to the hydroxy of the hydroxyaryl substituents are produced by Claisen Rearrangement of an alkenyl ether of the hydroxyaryl-substituted spirodilactam having one fewer ortho-alkenyl substituent.
    Type: Grant
    Filed: May 24, 1989
    Date of Patent: November 6, 1990
    Assignee: Shell Oil Company
    Inventor: Pen C. Wang
  • Patent number: 4963538
    Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by structural formulae (I) or (II): ##STR1## wherein position 5 of the polyhydronaphthyl ring is singly or doubly bonded to oxygen or incorporated into a C.sub.3-7 carbocyclic ring.
    Type: Grant
    Filed: March 13, 1989
    Date of Patent: October 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman
  • Patent number: 4952707
    Abstract: Chemiluminescent 1,2-dioxetane compounds are disclosed in which the molecule is stabilized at the 3-position on the dioxetane ring against decomposition prior to the molecule's coming in contact with a labile group-removing substance (e.g., an enzyme that will cleave the labile group to cause the molecule to decompose to form at least one light-emitting fluorophore) and substituted at the 4-position on the dioxetane ring with a fused polycyclic ring-containing fluorophore moiety bearing a labile ring substituent whose point of attachment to the fused polycyclic ring, in relation to this ring's point(s) of attachment to the dioxetane ring, is such that the total number of ring atoms separating these points of attachment, including the ring atoms at the points of attachment, is an odd whole number. These odd pattern substituted compounds decompose to emit light of greater intensity and of a different wavelength than that emitted by the corresponding even pattern substituted isomers.
    Type: Grant
    Filed: June 30, 1988
    Date of Patent: August 28, 1990