The Ring Oxygens Are In The 1,2- Or 1,3-positions Of The Hetero Ring Patents (Class 549/365)
  • Patent number: 7098243
    Abstract: Novel bicyclic carbohydrate compounds are effective for the prophylaxis and treatment of diseases caused by infections of the alphaherpesvirinae HSV-1 and HSV-2. The invention includes the compound wherein X1, X2, and X3 are selected from the group consisting of O, N, and S; wherein Y1 and Y2 are selected from the group consisting of O, N, and S; and wherein Z is selected from the group consisting of F, Cl, and Br, as well as analogs, prodrugs and pharmaceutically acceptable salts thereof, together with pharmaceutical compositions for the prophylaxis and treatment of diseases caused by infections of alphaherpesvirinae.
    Type: Grant
    Filed: September 16, 2003
    Date of Patent: August 29, 2006
    Assignee: Kemin Pharma Europe B.V.B.A.
    Inventors: Benedikt Sas, Johan Van hemel, Jan Vandenkerckhove, Eric Peys, Johan Van Der Eycken, Steven Van Hoof
  • Patent number: 7019003
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Grant
    Filed: March 1, 2002
    Date of Patent: March 28, 2006
    Assignee: Smithkline Beecham Corporation
    Inventors: Jia-Ning Xiang, Siegfried B. Christensen, IV, Jinhwa Lee, Daniel J. Mercer
  • Patent number: 6756375
    Abstract: The invention provides for a non-steroidal compound having the formula wherein Re and ′Re are OH, optionally independently etherified or esterified; Z is —CH2— or —CH2CH2—; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2, R3 and R4 are independently H, halogen, —CF3, —OCF3, (1C-8C)Alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl, halo(1C-8C)alkyl or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-4C)a
    Type: Grant
    Filed: July 24, 2003
    Date of Patent: June 29, 2004
    Assignee: Akzo Nobel N.V.
    Inventors: Gerrit Herman Veeneman, Hubert JanJozef Loozen, Jordi Mestres, Eduard Willem De Zwart
  • Patent number: 6706744
    Abstract: Novel compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.
    Type: Grant
    Filed: November 16, 2001
    Date of Patent: March 16, 2004
    Assignee: Novo Nordisk A/S
    Inventors: Peter Madsen, Jesper Lau, Anthony Ling
  • Patent number: 6583161
    Abstract: The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: December 12, 2000
    Date of Patent: June 24, 2003
    Assignee: Tularik Inc.
    Inventor: Julio C. Medina
  • Patent number: 6410790
    Abstract: 3-amino-3-arylpropan-1-ol compounds of formula I: R1 and R2 independently denoting C1-6 alkyl, or together denoting a (CH2)2-6 ring optionally substituted by phenyl, R3 denoting C3-6 alkyl, C3-6 cycloalkyl, aryl optionally containing heteroatoms and optionally substituted by R6 to R8, or a substituted C1-3 alkylphenyl of formula XII:  R4 and R5 independently denoting C1-6 alkyl, C3-6 cycloalkyl, phenyl, benzyl, or phenethyl, or together forming a (CH2)3-6 or CH2CH2OCH2CH2 ring, R6 to R8 independently denoting H, F, Cl, Br, CHF2, CF3, OH, OCF3, OR14, NR15R16, SR14, phenyl, SO2CH3, SO2CF3, C1-6 alkyl, CN, COOR14, or CONR15R16, or together forming a OCH2O, OCH2CH2O, CH═CHO, CH═C(CH3)O or (CH2)4 ring, R14 denoting C1-6 alkyl, phenyl, benzyl, or phenethyl, R15 and R16 independently denoting H, C1-6 alkyl, phenyl, benzyl or phenethyl, and A denoting optionally substituted aryl optionally containing heteroatoms, or a diastereomer or enantiomer or pharmaceutica
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: June 25, 2002
    Assignee: Gruenenthal GmbH
    Inventors: Bernd Sundermann, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Helmut Buschmann
  • Patent number: 6407100
    Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.
    Type: Grant
    Filed: September 1, 1993
    Date of Patent: June 18, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans Peter Isenring, Bettina Weiss
  • Patent number: 6365756
    Abstract: A process for the production of optically enriched (R)- or (S)-albuterol or (R)- or (S)-albuterol salts by the resolution of a novel ketal derivative 2-(N-t-butylamino)-1-(+2,2-dimethyl-1,2-benzodioxin-6-yl) ethanol, with a chiral tartaric acid derivative.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: April 2, 2002
    Assignee: Fine Chemical Corporation Limited
    Inventors: Anne Stevens, Roger Hunter, Luigi Nassimbeni, Mino Caira, Janet Scott, Rainer Clauss, Joanne Gibson, Tarron Grimmbacher
  • Patent number: 6355634
    Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 12, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans Peter Isenring, Bettina Weiss
  • Patent number: 6331627
    Abstract: The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereo-somers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.
    Type: Grant
    Filed: July 5, 2000
    Date of Patent: December 18, 2001
    Assignee: Reddy's Laboratories Ltd.
    Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Rajagopalan Ramanujam, Ranjan Chakrabarti
  • Patent number: 6310080
    Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: December 1, 1999
    Date of Patent: October 30, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
  • Patent number: 6277867
    Abstract: The invention relates to compounds of general formula (I), their optically active isomers and salts wherein Ar=alycylic, aromatic or one or more heteroatom containing heterocyclic moiety, optionally substituted by one or more alkoxy-, methylenedioxy-, alkyl-, halogen-, haloalkyl-,or nitro- group and/or condensed with a benzene ring. Ar—(CR1R2)m—(YR3R4)n—X—(CR5R6)o—(CR7R8)p—C≡C—E  (I) The compounds of general formula (I) according to the invention can be applied as active ingredients of pesticides, preferably arthropodicide compositions, and as synergists of other arthropodicideactive ingredients.
    Type: Grant
    Filed: August 31, 1998
    Date of Patent: August 21, 2001
    Assignee: Chinoin Gyogyszer es Vegyeszeti
    Inventors: Geza Arvai, Ildiko Bakonyvari, Bela Bertok, Laszlo Csiz, Iren Czudor, Zsuzsa R. Kuruczne, Laszlo Pap, Istvan Szekely
  • Patent number: 6274613
    Abstract: The invention relates to novel cyclic imines of the formula (I) in which Ar1 and Ar2 each represent substituted phenyl and n represents 1, to a process for their preparation and to their use as pesticides.
    Type: Grant
    Filed: May 11, 1999
    Date of Patent: August 14, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Andrew Plant, Gerd Kleefeld, Thorsten Pötter, Christoph Erdelen, Norbert Mencke, Andreas Turberg, Ulrike Wachendorff-Neumann
  • Patent number: 5998667
    Abstract: The invention relates to new substituted biphenyloxazolines of the formula (I) ##STR1## in which R.sup.1 represents C.sub.1 -C.sub.6 -halogenoalkylthio andR.sup.2 represents hydrogen, orR.sup.1 and R.sup.2 together with the carbon atoms to which they are bonded form a halogen-substituted 5- or 6-membered heterocyclic ring,X represents hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.
    Type: Grant
    Filed: June 4, 1998
    Date of Patent: December 7, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhard Lantzsch, Albrecht Marhold, Christoph Erdelen
  • Patent number: 5952386
    Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.
    Type: Grant
    Filed: September 24, 1997
    Date of Patent: September 14, 1999
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
  • Patent number: 5869702
    Abstract: Polyol ether derivatives, a method for producing the polyol ether derivatives, and a working fluid composition for a refrigerating machine containing a hydrofluorocarbon and a refrigeration oil containing the polyol ether derivatives as a base oil.
    Type: Grant
    Filed: June 4, 1997
    Date of Patent: February 9, 1999
    Assignee: Kao Corporation
    Inventors: Shoji Nakagawa, Hiroki Sawada, Hiroyasu Togashi, Toshiya Hagihara
  • Patent number: 5773463
    Abstract: This invention describes the use of aminoindane and amino-tetrahydronaphthalene derivatives of general formula (I) ##STR1## in which Ar, X, R.sub.1, R.sub.2 and n are defined in claim 1, for the manufacture of a medicament for the treatment of disorders in which a calcium channel antagonist is indicated. Novel compounds falling within formula (I) are also claimed.
    Type: Grant
    Filed: January 22, 1996
    Date of Patent: June 30, 1998
    Assignee: SmithKline Beecham p.l.c.
    Inventors: John David Harling, Barry Sidney Orlek
  • Patent number: 5612381
    Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 18, 1997
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
  • Patent number: 5578252
    Abstract: Described are novel reversible photochromic 3H-naphtho[2,1-b]pyran compounds, examples of which are substituted with an oxy-bearing substituent at the number 8 carbon atom and with either an alkyl group at the number 7 carbon atom or with a carbonyl bearing substituent at the number 9 carbon atom and certain substituents at the 3-position of the pyran ring, e.g., 3,3-spirofluoren-9-ylidene 8-methoxy-9-carbomethoxy-3H-naphtho[2,1-b]pyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: November 29, 1995
    Date of Patent: November 26, 1996
    Assignee: Transitions Optical, Inc.
    Inventors: Barry Van Gemert, Anil Kumar
  • Patent number: 5569640
    Abstract: Cyclic acetals of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 and R.sup.2 are hydrogen, unsubstituted or substituted alkyl or phenyl; additionally R.sup.1 and R.sup.2 together are an unsubstituted or substituted C.sub.2 -C.sub.6 -alkylene chain;Y is oxygen or sulfur;A has the meaning as given in claim 1;a process for preparing the acetals I and their use for the production of crop protection compositions are described.
    Type: Grant
    Filed: November 1, 1994
    Date of Patent: October 29, 1996
    Inventors: Joachim Rheinheimer, Uwe J. Vogelbacher, Ernst Baumann, Hartmann Konig, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 5569669
    Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.2', R.sub.2", R.sub.2'", R.sub.3 and n are as defined in the description, an optical isomer, and an addition salt thereof with a pharmaceutically-acceptable acid or base,and medicinal product containing the same useful for treating a mammal afflicted with a disorder associated to 5-HT.sub.1A or 5-HT.sub.2C receptors.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: October 29, 1996
    Assignee: Adir et Compagnie
    Inventors: G erald Guillaumet, Marie-Claude Viaud, Pierre Renard, G erard Adam, Daniel-Henri Caignard, B eatrice Guardiola-Lemaitre, Marie-Claire Rettori
  • Patent number: 5514588
    Abstract: The present invention provides for enhanced bioremediation of hydrocarbon contaminated soils and waters by treating soil or water with a composition comprising a phosphorous source, a diluent and a compound or mixtures thereof represented by the structural formula: ##STR1## wherein R is a linear or branched alkane having about 8 to about 22 carbons, a linear or branched alkene having about 4 to about 22 carbon atoms; T.sub.1, T.sub.2, T.sub.3 are independently ethylene, trimethylene, or CH.sub.2 CH.sub.2 (NHCH.sub.2 CH.sub.2).sub.x, where x is an integer from 1 to 10; Q is HNO.sub.3 or H.sub.3 PO.sub.4 ; and, n is an integer from 0 to 10.
    Type: Grant
    Filed: December 13, 1994
    Date of Patent: May 7, 1996
    Assignee: Exxon Research and Engineering Company
    Inventors: Ramesh Varadaraj, Cornelius H. Brons, Jan Bock, Stanley J. Brois
  • Patent number: 5475132
    Abstract: R.sub.3, R.sub.4 and R.sub.5, each represents a hydrogen or halogen atom (at least one of R.sub.3, R.sub.4 and R.sub.5 being other than hydrogen or halogen); optionally substituted amino; optionally halogenated or hydroxylated alkyl, alkoxy, alkylalkoxy or alkylthio; or R.sub.3 and R.sub.4 (in the 3- and 4-positions) can together form a single divalent radical with 3 or 4 members containing 1 or 2 non-adjacent oxygen atoms; are useful as agricultural fungicides.
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: December 12, 1995
    Assignee: Rhone-Poulenc Agrochimie
    Inventors: Regis Pepin, Christian Schmitz, Guy-Bernard Lacroix, Philippe Dellis, Christine Veyrat
  • Patent number: 5472984
    Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.
    Type: Grant
    Filed: December 29, 1993
    Date of Patent: December 5, 1995
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
  • Patent number: 5440051
    Abstract: Aryl ethers are chlorinated in the .alpha.-position by a process in which they are metered into a reaction vessel at the same time as chlorine, the reaction being carried out at temperatures in the range from 60.degree. to 150.degree. C.
    Type: Grant
    Filed: March 22, 1994
    Date of Patent: August 8, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Albrecht Marhold, Klaus Jelich
  • Patent number: 5420333
    Abstract: An anti-hyperlipemic agent which has a potent activity of reducing LDL and VLDL cholesterols, which are thought to be a risk factor for arteriosclerosis among total blood cholesterols, and which is excellent in the antioxidant activity on LDL, is provided. Additionally, a compound and a pharmaceutically acceptable salt thereof are disclosed, which is represented by Formula (I): ##STR1## [wherein R.sup.1 is a power alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl or aralkyl group which is optionally substituted; R.sup.2 is a group represented by the formula: --COOR' (wherein R' is a lower alkyl or aralkyl which is optionally substituted), lower alkyl or halogenated lower alkyl; or R.sup.1 and R.sup.2, together with adjacent carbonyl group, form a cyclohexanone ring represented by the formula: ##STR2## R.sup.3 is a phenyl group optionally being substituted, and, ring A is a benzene nucleus which is optionally substituted, or a heterocyclic ring containing S or O optionally being substituted].
    Type: Grant
    Filed: June 17, 1993
    Date of Patent: May 30, 1995
    Assignee: Shionogi & Co., Ltd.
    Inventors: Sachio Mori, Shozo Takechi, Shiro Kida, Takuji Mizui, Teruhisa Ichihashi
  • Patent number: 5420273
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.6 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.
    Type: Grant
    Filed: December 23, 1993
    Date of Patent: May 30, 1995
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
  • Patent number: 5360815
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: June 23, 1993
    Date of Patent: November 1, 1994
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Rejean Fortin, Yves Girard, Erich Grimm, John Hutchinson, John Scheigetz
  • Patent number: 5356924
    Abstract: Compounds of the general formula: ##STR1## wherein R.sub.1 and R.sub.2 each independently represents a halogen atom or an alkyl, alkoxy, haloalkyl, haloalkoxy, alkoxycarbonyl, alkenoxy, cyano or nitro group; R.sub.3 and R.sub.4 each independently represents a hydrogen atom or an alkyl group; R.sub.5 represents a hydrogen atom, or an alkyl, alkoxy or alkoxycarbonylalkyl group; X and Y each independently represents an oxygen or sulphur atom or a group N--R, in which R is a hydrogen atom or an alkyl group; n is 0-3; r is 0 or 1; m is 0-4; and A or B represents a group of the general formula: ##STR2## wherein R.sub.6 represents a hydrogen or halogen atom, or an alkyl group; and R.sub.7 represents a halogen atom or an alkyl group; the other of A and B being a hydrogen atom or as for R.sub.1 or R.sub.2, have useful pesticidal activity.
    Type: Grant
    Filed: February 22, 1993
    Date of Patent: October 18, 1994
    Assignee: Shell Research Limited
    Inventors: Martin Anderson, Antony G. Brinnand, Roger E. Woodall
  • Patent number: 5312831
    Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.
    Type: Grant
    Filed: May 12, 1993
    Date of Patent: May 17, 1994
    Assignee: American Cyanamid Company
    Inventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
  • Patent number: 5292748
    Abstract: A process for the production of substituted vinylbenzenes of the general formula: ##STR1## wherein R is a lower alkyl group having 1 to 4 C atoms, R.sub.1 is hydrogen or an acetyl group and R.sub.2 is hydrogen, a lower alkyl group having 1 to 4 C atoms or a benzyl group. A trialkylhydroquinone is cyclized with an aldehyde to an acetal and the latter is pyrolized to the end product. The substituted vinylbenzenes are valuable intermediate products in the synthesis of antioxidants.
    Type: Grant
    Filed: April 8, 1993
    Date of Patent: March 8, 1994
    Assignee: Lonza, Ltd.
    Inventors: Aleksander Warm, David Laffan
  • Patent number: 5274176
    Abstract: A process for the production of substituted vinylbenzenes of the general formula: ##STR1## wherein R is a lower alkyl group having 1 to 4 C atoms, R.sub.1 is hydrogen or an acetyl group and R.sub.2 is hydrogen, a lower alkyl group having 1 to 4 C atoms or a benzyl group. A trialkylhydroquinone is cyclized with an aldehyde to an acetal and the latter is pyrolized to the endproduct. The substituted vinylbenzenes are valuable intermediate products in the synthesis of antioxidants.
    Type: Grant
    Filed: October 21, 1992
    Date of Patent: December 28, 1993
    Assignee: Lonza Ltd.
    Inventors: Aleksander Warm, David Laffan
  • Patent number: 5272144
    Abstract: Aryloxy- and heteroaryloxy-alkylene derivatives of amines of formula ##STR1## wherein each of A and B is a group of formula (i) to (iii): ##STR2## wherein Y is --O--, --S-- or --NR-- in which R is hydrogen or C.sub.1 -C.sub.6 alkyl; each of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 is independently:a) hydrogen, halogen, hydroxy, cyano or nitro;b) C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by halogen,c) C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio;d) C.sub.1 -C.sub.6 alkyl-sulfonyl;e) a substituted amine group --NR.sub.7 R.sub.8 ;f) a --COR.sub.12 group; org) two adjacent groups of R.sub.3, R.sub.4, R.sub.5 and R.sub.6, taken together, form a C.sub.1 -C.sub.4 alkylenedioxy group;each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 alkenyl or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl; or R.sub.1 and R.sub.
    Type: Grant
    Filed: June 13, 1991
    Date of Patent: December 21, 1993
    Assignee: Farmitalia Carlo Erba s.r.l.
    Inventors: Piero Melloni, Philippe Dostert, Arturo D. Torre, Alberto Bonsignori
  • Patent number: 5214053
    Abstract: Thiourea derivatives represented by the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl group, or R.sub.1 and R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.x --CHR.sub.3 --(CH.sub.2).sub.y -- in which R.sub.3 represents hydrogen or a lower alkyl group and x and y represent an integer of 0 to 2, respectively, A represents the formula --CH.dbd.CH-- or --CH.dbd.N--, 1 is 1 or 2, m represents an integer of 0 to 2 and n represents an integer of 1 to 5.The thiourea derivatives possess an antiulcer activity and an antimicrobial activity against Helicobacter pyroli and are useful as an antiulcer agent and an antimicrobial agent against Helicobacter pyroli.
    Type: Grant
    Filed: September 2, 1992
    Date of Patent: May 25, 1993
    Assignee: Terumo Kabushiki Kaisha
    Inventors: Keiichi Nakazawa, Masashi Isozaki, Shingo Koyama
  • Patent number: 5212173
    Abstract: Pharmacologically active compounds corresponding to the formula I ##STR1## in which n represents 2-5,m represents 2-6,R.sup.1 denotes hydrogen or lower alkyl,R.sup.2 represents an OR.sup.4 group in which R.sup.4 denotes lower alkyl or a phenyl or phenyl-lower alkyl group which is optionally substituted in the phenyl ring, orR.sup.2 represents a ##STR2## group in which R.sup.5 and R.sup.6 independently of one another each denote hydrogen, lower alkyl or a phenyl or phenyl-lower alkyl group which is optionally substituted in the phenyl ring, orR.sup.5 and R.sup.6, together with the nitrogen atom to which they are bonded, represent a saturated 5- or 6-membered heterocycle,R.sup.3 represents a saturated monocyclic or bicyclic hydrocarbon group which is derived from terpenes and has 10 or 11 carbon atoms, andZ represents oxygen or, if R.sup.3 is a dihydronopyl group, Z may also represent sulfur,and salts thereof.
    Type: Grant
    Filed: December 19, 1991
    Date of Patent: May 18, 1993
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Herman Kraehling, Samuel David, Insa Hell, Ulf Preuschoff, Ivan Ban, Marie-Odile Christen
  • Patent number: 5212171
    Abstract: Compounds of the general formula: ##STR1## ps wherein R.sub.1 and R.sub.2 each independently represents a halogen atom or an alkyl, alkoxy, haloalkyl, haloalkoxy, alkoxycarbonyl, alkenoxy, cyano or nitro group; R.sub.3 and R.sub.4 each independently represents a hydrogen atom or an alkyl group; R.sub.5 represents a hydrogen atom, or an alkyl, alkoxy or alkoxycarbonylalkyl group; X and Y each independently represents an oxygen or sulphur atom or a group N-R, in which R is a hydrogen atom or an alkyl group; n is 0-3; r is 0 or 1; m is 0-4; and A or B represents a group of the general formula: wherein R.sub.6 represents a hydrogen or halogen atom, or an alkyl group; and R represents a halogen atom or an alkyl group; the other of A and B being a hydrogen atom or as for R.sub.1 or R.sub.2, have useful pesticidal activity.
    Type: Grant
    Filed: July 9, 1991
    Date of Patent: May 18, 1993
    Assignee: Shell Research limited
    Inventors: Martin Anderson, Antony G. Brinnand, Roger E. Woodall
  • Patent number: 5202351
    Abstract: A novel 1-phenylalkyl-3-phenylurea derivative represented by the following formula (I): ##STR1## wherein R.sup.1 and R.sup.5 represent independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.5 alkoxyl or halo; R.sup.2 represents hydrogen or C.sub.1 -C.sub.15 alkyl; R.sup.3 represents C.sub.1 -C.sub.15 alkyl or R.sup.3 represents together with R.sup.2 C.sub.2 -C.sub.9 alkylene; R.sup.4 and R.sup.5 represent independently C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxyl or halo; X represents oxygen or sulfur; Y represents --O--(CH.sub.2).sub.l --O-- wherein l is an integer of 1 to 3 or --(CH.sub.2).sub.p -- wherein p is an integer of 3 to 5; m is 0 or an integer of 1 to 5; and n is 0 or an integer of 1 to 3, is provided. The 1-phenylalkyl-3-phenylurea derivative (I) have the action of reducing cholesterol in blood by ACAT inhibition, and therefore, useful for treating hyperlipemia and atherosclerosis.
    Type: Grant
    Filed: January 22, 1991
    Date of Patent: April 13, 1993
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Tetsuo Sekiya, Shinya Inoue, Chiaki Hyodo, Hiromi Okushima, Kohei Umezu, Kazuo Suzuki
  • Patent number: 5147463
    Abstract: This invention provides novel cyclic acetals useful as delayed release flavorants and odorants having the general formula: ##STR1## These compounds possess no detectable flavor or odor themselves at normal temperatures and atmospheric conditions but release an aldehyde flavorant upon heating at higher temperatures. The novel cyclic acetals of the present invention may be used as flavorants in tobacco compositions or tobacco substitutes, as sustained flavorants and odorants to mask or enhance the flavors and odors of burning tobacco products, as flavor additives to microwaveable foods, and in the preparation of chewing gums.
    Type: Grant
    Filed: August 18, 1989
    Date of Patent: September 15, 1992
    Assignee: BASF K&F Corporation
    Inventors: Robert G. Eilerman, Philip A. Christenson, John M. Yurecko, Jr., Frank Mild, Peter E. Kucharski
  • Patent number: 5137578
    Abstract: This invention provides smoking compositions which contain a novel flavorant-release additive.Under cigarette smoking conditions, a combustible filler and/or paper wrapper additive such as 4'-formyl-2'-methoxyphenyl 4,6-O-cinnamylidene-.beta.-D-glucopyranoside pyrolyzes into cinnamaldehyde and vanillin flavorants as volatile components of the cigarette smoke.
    Type: Grant
    Filed: February 26, 1991
    Date of Patent: August 11, 1992
    Assignees: Philip Morris Incorporated, Philip Morris Products Inc.
    Inventor: Wootung G. Chan
  • Patent number: 4968717
    Abstract: Compounds of the formula ##STR1## where R.sup.1 to R.sup.7, m, n and p have the meanings stated in the description, and certain derivatives which are p-substituted in the left-hand phenyl ring, are useful for the treatment of disorders.
    Type: Grant
    Filed: May 12, 1989
    Date of Patent: November 6, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Liliane Unger, Manfred Raschack, Verena Baldinger, Ferdinand Dengel, Oskar Ehrmann, Hans J. Treiber, Werner Seitz
  • Patent number: 4956474
    Abstract: The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus.
    Type: Grant
    Filed: June 20, 1989
    Date of Patent: September 11, 1990
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventors: Haruo Ohnishi, Hiroshi Kosuzume, Masahiro Mizota, Yasuo Suzuki, Ei Mochida
  • Patent number: 4943591
    Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein X represents a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain andY represents a bond, or a C.sub.1-4 alkylene, C.sub.2-4 alkenylene or C.sub.2-4 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 8;Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-3 alkyl, nitro, --(CH.sub.2).sub.q R [where R is hydroxy, C.sub.1-3 alkoxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represent a hydrogen atom, or a C.sub.1-4 alkyl group, or --NR.sup.3 R.sup.4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O-- or --S-- or a group --NH-- or --N(CH.sub.3)--), --NR.sup.5 COR.sup.6 (where R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.6 represents a hydrogen atom or a C.sub.
    Type: Grant
    Filed: October 14, 1986
    Date of Patent: July 24, 1990
    Assignee: Glaxo Group Limited
    Inventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell
  • Patent number: 4940806
    Abstract: Novel substituted 2-(1H-1,2,4-triazolyl)-1-phenylethan-1-one ketals of the general formula ##STR1## wherein one of the two phenyl substituents is in 2-position and the other is in 4-position, and wherein R.sub.a is halogen, methyl or C.sub.1 -C.sub.3 haloalkoxy, and U and V are each independently of the other C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted by halogen or C.sub.1 -C.sub.6 alkoxy, or together are an alkylene bridge selected from ##STR2## wherein R.sub.1 to R.sub.5 are as defined herein, and the acid addition salts and metal complex salts, have microbicidal properties and are especially suitable for controling phytopathogenic microorganisms. They can be used in the form of plant protective or seed dressing agents for preventing or controlling plant pathogens.
    Type: Grant
    Filed: June 21, 1989
    Date of Patent: July 10, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Adolf Hubele
  • Patent number: 4908386
    Abstract: The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain;Y represents a bond or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
    Type: Grant
    Filed: December 20, 1988
    Date of Patent: March 13, 1990
    Assignee: Glaxo Group Limited
    Inventors: Harry Finch, Lawrence H. C. Lunts, Alan Naylor, Ian F. Skidmore, Ian B. Campbell, David Middlemiss, Charles Willbe
  • Patent number: 4880775
    Abstract: The present invention relates to novel poly-alkylated benzodioxin compounds possessing a musk-like aroma which are useful as fragrance materials. The compounds of the invention have the formula: ##STR1## where R.sup.1 to R.sup.4 are hydrogen or lower alkyl (C.sub.1 to C.sub.5), provided that the compound has no more than 18 carbon atoms. The invention provides for synthesis of a novel phenolic intermediate and synthesis of the compounds of the invention. The invention also provides fragrance compositions which utilize the compounds of the invention to modify, enhance, or impart a musk-like aroma to perfume compositions, colognes and perfumed articles.
    Type: Grant
    Filed: February 1, 1987
    Date of Patent: November 14, 1989
    Assignee: BASF K&F Corporation
    Inventors: Philip A. Christenson, Brian Drake, Paul J. Riker
  • Patent number: 4880572
    Abstract: Novel unnatural ceramide related compounds, for instance, (2S, 3S)-2-tetracosanamido-octadecane-1,3-diol are herein provided, which are useful as intermediates in preparing ceramide moieties employed in the preparation of glycolipids and gangliosides known as tumor markers or molecular markers and which are prepared by, for instance, subjecting a chiral compound represented by the following formula: ##STR1## to deacetal treatment.
    Type: Grant
    Filed: May 26, 1988
    Date of Patent: November 14, 1989
    Assignee: MECT Corporation
    Inventors: Shuji Fujita, Shoji Yoshimura, Masayoshi Ito, Yoshiyasu Shitori, Tomoya Ogawa
  • Patent number: 4808762
    Abstract: Compounds of the formula ##STR1## in which Ar is substituted or unsubstituted phenyl, naphthyl, or thienyl; Z is oxygen, sulfur, or methylene; and Ar' is 2-methyl[1,1'-biphenyl]-3-yl, 3-phenoxyphenyl, 4-fluoro-3-phenoxyphenyl, or 6-phenoxy-2-pyridyl exhibit pyrethroid-like insecticidal and acaricidal activity and are relatively harmless to aquatic fauna.
    Type: Grant
    Filed: September 9, 1987
    Date of Patent: February 28, 1989
    Assignee: FMC Corporation
    Inventors: Gary A. Meier, Scott M. Sieburth, Thomas G. Cullen, John F. Engel
  • Patent number: 4794188
    Abstract: Compounds of the formula:Ar.sub.1 -X-Ar-Z-(R).sub.n'and salts thereof, whereinAr.sub.1 is a nitrogen, sulfur or oxygen heterocyclic ring;Ar is a phenyl ring or a nitrogen, oxygen or sulfur heterocyclic ring;Ar and Ar.sub.1 may be fully substituted or less than fully substituted with H, CH.sub.3, lower alkyl, aryl, aralkyl, halo, hydroxy, lower alkoxy, CF.sub.
    Type: Grant
    Filed: December 19, 1985
    Date of Patent: December 27, 1988
    Assignee: USV Pharmaceutical Corporation
    Inventors: John H. Musser, Utpal R. Chakraborty
  • Patent number: 4792606
    Abstract: A process for the preparation of a dimeric aromatic acyl cyanide of the formula ##STR1## in which Ar is optionally substituted phenyl, naphthyl or hetaryl,comprising reaction an acyl halide of the formulaAr--CO--Halin whichHal is fluorine, chlorine or bromine, with an alkali metal cyanide in a two-phase system comprising water and a water-immiscible or only sparingly water-miscible aliphatic ketone, and in the presence of a phase-transfer catalyst. The products are known intermediates for pesticides.
    Type: Grant
    Filed: July 16, 1987
    Date of Patent: December 20, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhard Lantzsch, Hermann-Dieter Krall
  • Patent number: 4734217
    Abstract: Liquid crystalline 2,6-disubstituted trans-1,3-dioxadecalins of the general formula ##STR1## are well suited as components of low double refraction for mixtures which are utilized in opto-electronic components.
    Type: Grant
    Filed: September 26, 1985
    Date of Patent: March 29, 1988
    Assignee: VEB Werk fuer Fernsehelektronik im VEB Kombinat Mikroelektronik
    Inventors: Dietrich Demus, Horst Zaschke, Carsten Tschierske, Maike Hettrich