Spiro Patents (Class 544/6)
-
Patent number: 6060469Abstract: 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: GrantFiled: May 18, 1998Date of Patent: May 9, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Raymond Baker, Timothy Harrison, Christopher John Swain, Brian John Williams
-
Patent number: 6013652Abstract: 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: GrantFiled: December 4, 1997Date of Patent: January 11, 2000Assignee: Merck & Co., Inc.Inventors: Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Yuan-Ching P. Chiang, Patrick T. Dunn, Hiroo Koyama
-
Patent number: 6011150Abstract: 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: GrantFiled: May 15, 1995Date of Patent: January 4, 2000Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tameo Iwasaki, Kazuhiko Kondo
-
Patent number: 6002000Abstract: 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: GrantFiled: June 11, 1996Date of Patent: December 14, 1999Assignee: Dade Behring Marburg GmbHInventors: Sharat Singh, Rajendra Singh, Frank Meneghini, Edwin F. Ullman
-
Patent number: 5994350Abstract: 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: GrantFiled: April 17, 1998Date of Patent: November 30, 1999Assignee: Sanofi-SynthelaboInventors: Loic Foulon, Georges Garcia, Claudine Serradeil-Le Gal, Gerard Valette
-
Patent number: 5981523Abstract: 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: GrantFiled: August 14, 1997Date of Patent: November 9, 1999Assignee: Eli Lilly and CompanyInventors: Jill A Panetta, Michael L Phillips
-
Patent number: 5945413Abstract: 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: GrantFiled: September 30, 1996Date of Patent: August 31, 1999Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Govinda Rao Bhisetti, Christopher Todd Baker, Andrew Spaltenstein
-
Patent number: 5929072Abstract: 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: GrantFiled: August 21, 1998Date of Patent: July 27, 1999Assignee: Eli Lilly and Company LimitedInventor: John Fairhurst
-
Patent number: 5922748Abstract: 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: GrantFiled: January 20, 1998Date of Patent: July 13, 1999Assignee: Glaxo Wellcome Inc.Inventors: Robert Charles Glen, David Lawrence Selwood, Graeme Richard Martin, Christopher James Foster
-
Patent number: 5874382Abstract: 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: GrantFiled: January 23, 1998Date of Patent: February 23, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Balreddy Kamireddy, William Mark Murray
-
Patent number: 5783579Abstract: 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: GrantFiled: December 20, 1996Date of Patent: July 21, 1998Assignee: Schering CorporationInventor: Kevin D. McCormick
-
Patent number: 5728693Abstract: Arthropodicidal compounds, compositions and use of compounds having the formula ##STR1##Type: GrantFiled: June 25, 1996Date of Patent: March 17, 1998Assignee: E. I. du Pont de Nemours and CompanyInventor: Thomas Martin Stevenson
-
Patent number: 5726126Abstract: 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: GrantFiled: November 26, 1996Date of Patent: March 10, 1998Assignee: American Cyanamid CompanyInventors: Alvin Donald Crews, Jr., Philip Mark Harrington, Gary Mitchell Karp, Mark Christopher Manfredi, Michael Anthony Guaciaro
-
Patent number: 5696145Abstract: 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: GrantFiled: June 7, 1995Date of Patent: December 9, 1997Assignee: SanofiInventors: Loic Foulon, Georges Garcia, Daniel Mettefeu, Claudine Serradeil-Legal, Gerard Valette
-
Patent number: 5679805Abstract: 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: GrantFiled: June 7, 1995Date of Patent: October 21, 1997Assignee: Vision-Ease Lens, Inc.Inventor: Frank J. Hughes
-
Patent number: 5597819Abstract: 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: GrantFiled: February 13, 1995Date of Patent: January 28, 1997Assignee: Adir Et CompagnieInventors: Jean-Daniel Brion, Anne-Marie Chollet, Luc Demuynck, Lucy De Montarby, Yves Rolland, Jacqueline Bonnet, Pietro Ghezzi, Armel Fradin
-
Patent number: 5591848Abstract: 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: GrantFiled: October 7, 1994Date of Patent: January 7, 1997Assignee: The Penn State Research FoundationInventor: Przemyslaw B. Maslak
-
Patent number: 5589489Abstract: 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: GrantFiled: December 12, 1994Date of Patent: December 31, 1996Assignee: Zeneca LimitedInventors: Ashokkumar B. Shenvi, Robert T. Jacobs, Scott C. Miller, Cyrus J. Ohnmacht, Jr., Chris A. Veale
-
Patent number: 5578593Abstract: 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: GrantFiled: November 3, 1993Date of Patent: November 26, 1996Assignee: Merck & Co., Inc.Inventors: Meng-Hsin Chen, David B. R. Johnston, Ravi P. Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang
-
Patent number: 5559233Abstract: The invention relates to processes for preparing N-substituted heterocyclic compounds of formula (I) ##STR1##Type: GrantFiled: June 30, 1994Date of Patent: September 24, 1996Assignee: SanofiInventors: Claude Bernhart, Jean-Claude Breliere, Jacques Clement, Dino Nisato, Pierre Perreault, Claude Muneaux, Yvette Muneaux
-
Patent number: 5550229Abstract: 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: GrantFiled: June 21, 1994Date of Patent: August 27, 1996Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tameo Iwasaki, Kazuhiko Kondo, Hiroshi Ohmizu
-
Patent number: 5545834Abstract: 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: GrantFiled: January 17, 1995Date of Patent: August 13, 1996Assignee: Behringwerke AGInventors: Sharat Singh, Rajendra Singh, Frank Meneghini, Edwin F. Ullman
-
Patent number: 5536716Abstract: 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: GrantFiled: November 3, 1993Date of Patent: July 16, 1996Assignee: Merck & Co., Inc.Inventors: Meng-Hsin Chen, David B. R. Johnston, Ravi P. Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang
-
Patent number: 5457199Abstract: 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: GrantFiled: July 11, 1994Date of Patent: October 10, 1995Assignee: Ciba-Geigy CorporationInventors: Roberto Scrima, Graziano Zagnoni
-
Patent number: 5447927Abstract: 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: GrantFiled: July 25, 1994Date of Patent: September 5, 1995Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Joachim Weissmuller, Dieter Berg, Wilhelm Brandes, Stefan Dutzmann
-
Patent number: 5407943Abstract: 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: GrantFiled: November 22, 1993Date of Patent: April 18, 1995Assignee: Pfizer Inc.Inventor: Bingwei V. Yang
-
Patent number: 5376660Abstract: 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: GrantFiled: August 3, 1992Date of Patent: December 27, 1994Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Joachim Weissmuller, Dieter Berg, Wilhelm Brandes, Stefan Dutzmann
-
Patent number: 5373009Abstract: 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: GrantFiled: February 2, 1994Date of Patent: December 13, 1994Assignee: American Home Products CorporationInventors: Thomas J. Commons, Donald P. Strike
-
Patent number: 5352788Abstract: 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: GrantFiled: June 23, 1993Date of Patent: October 4, 1994Assignee: Elf SanofiInventors: Claude Bernhart, Jean-Claude Breliere, Jacques Clement, Dino Nisato, Pierre Perreault, Claude Muneaux, Yvette Muneaux
-
Patent number: 5329006Abstract: 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: GrantFiled: September 6, 1991Date of Patent: July 12, 1994Assignee: Ciba-Geigy CorporationInventors: Hans Baumann, Ian J. Fletcher
-
Patent number: 5296477Abstract: 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: GrantFiled: December 1, 1992Date of Patent: March 22, 1994Assignee: Adir et CompagnieInventors: Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
-
Patent number: 5286723Abstract: 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: GrantFiled: June 22, 1992Date of Patent: February 15, 1994Assignee: Daiichi Seiyaku Co., Ltd.Inventors: Isao Hayakawa, Shohgo Atarashi, Masazumi Imamura, Youichi Kimura
-
Patent number: 5204474Abstract: 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: GrantFiled: June 3, 1991Date of Patent: April 20, 1993Assignee: Ciba-Geigy CorporationInventors: Glen T. Cunkle, Joseph E. Babiarz
-
Patent number: 5177216Abstract: 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: GrantFiled: May 13, 1991Date of Patent: January 5, 1993Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventor: Tsutomu Yamanaka
-
Patent number: 5149823Abstract: 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: GrantFiled: August 9, 1990Date of Patent: September 22, 1992Assignee: Shell Oil CompanyInventor: Pen-Chung Wang
-
Patent number: 5109006Abstract: 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: GrantFiled: August 22, 1991Date of Patent: April 28, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Marcel Hibert
-
Patent number: 5104872Abstract: 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: GrantFiled: August 15, 1990Date of Patent: April 14, 1992Assignee: Nihon Hohyaku Co., Ltd.Inventors: Kenji Tsubata, Nobuyuki Niino, Katsutoshi Endo, Yoshinobu Yamamoto, Hideo Kanno
-
Patent number: 5084454Abstract: 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: GrantFiled: October 11, 1989Date of Patent: January 28, 1992Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Mario Varasi, Piero Melloni, Maria A. Cervini, Alberto Bonsignori, Roberto Commisso
-
Patent number: 5059689Abstract: 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: GrantFiled: January 30, 1989Date of Patent: October 22, 1991Assignee: Ciba-Geigy CorporationInventors: Jean Rody, Gerhard Rytz, Mario Slongo
-
Patent number: 5051417Abstract: 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: GrantFiled: July 13, 1989Date of Patent: September 24, 1991Assignee: Les Laboratoires Beecham S.A.Inventors: Guy Nadler, Michel Martin, Richard Zimmermann
-
Patent number: 5028711Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.Type: GrantFiled: July 6, 1989Date of Patent: July 2, 1991Assignee: Beiersdorf AktiengesellschaftInventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
-
Patent number: 5013827Abstract: 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: GrantFiled: November 13, 1989Date of Patent: May 7, 1991Assignee: Board of Governors of Wayne State UniversityInventor: Arthur P. Schaap
-
Patent number: 5000777Abstract: 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: GrantFiled: November 21, 1989Date of Patent: March 19, 1991Assignees: Ciba-Geigy Corporation, Janssen PharmaceuticaInventors: Henry Szczepanski, Lourens Wals
-
Patent number: 4985421Abstract: 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: GrantFiled: August 17, 1989Date of Patent: January 15, 1991Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Joachim Weissmuller, Dieter Berg, Wilhelm Brandes, Stefan Dutzmann
-
Patent number: 4973593Abstract: Compounds of the formulae: ##STR1## are useful as anti-hypertensives.Type: GrantFiled: August 4, 1987Date of Patent: November 27, 1990Assignee: Research Corporation Technologies, Inc.Inventor: Abram N. Brubaker
-
Patent number: 4968810Abstract: 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: GrantFiled: March 17, 1989Date of Patent: November 6, 1990Assignee: Shell Oil CompanyInventor: Pen C. Wang
-
Patent number: 4968812Abstract: 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: GrantFiled: June 23, 1989Date of Patent: November 6, 1990Assignee: Shell Oil CompanyInventors: Pen-Chung Wang, William J. Asbell
-
Patent number: 4968811Abstract: 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: GrantFiled: May 24, 1989Date of Patent: November 6, 1990Assignee: Shell Oil CompanyInventor: Pen C. Wang
-
Patent number: 4963538Abstract: 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: GrantFiled: March 13, 1989Date of Patent: October 16, 1990Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman
-
Patent number: 4952707Abstract: 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: GrantFiled: June 30, 1988Date of Patent: August 28, 1990