Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/456)
  • Patent number: 7550461
    Abstract: Disclosed are amide compounds of formula (I): wherein Ar1, Q, Y and R3-R6 of formula (I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: April 10, 2003
    Date of Patent: June 23, 2009
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Kevin Chungeng Qian, Gregory Paul Roth, Christopher Ronald Sarko, Alan David Swinamer, Zhaoming Xiong
  • Patent number: 7452615
    Abstract: Disclosed is a compound of Formula 1 and an organic light emitting device using the same. In Formula 1, R1 to R3 and X1 to X3 are as described in the specification. The compound of Formula 1 acts as a hole injection material, a hole transport material, a light emitting host, or a light emitting dopant in the organic light emitting device depending on the type of substituent.
    Type: Grant
    Filed: September 19, 2005
    Date of Patent: November 18, 2008
    Assignee: LG Chem, Ltd.
    Inventors: Kong Kyeom Kim, Jun Gi Jang
  • Publication number: 20080220285
    Abstract: The present invention relates to the improvement of organic electroluminescent devices, in particular blue-emitting devices, by using compounds of the formula (1) as dopants in the emitting layer.
    Type: Application
    Filed: April 21, 2006
    Publication date: September 11, 2008
    Applicant: Merck Patent GmbH
    Inventors: Horst Vestweber, Holger Heil, Philipp Stoessel, Arne Buesing, Amir Hossain Parham, Rocco Fortte
  • Publication number: 20080177073
    Abstract: The present teachings provide compounds of formulae I and II: where Q, Ra, R1, W, and n are as defined herein. The present teachings also provide methods of preparing compounds of formulae I and II, including methods of preparing compounds of formula II from compounds of formula I. The compounds disclosed herein can be used to prepare semiconductor materials and related composites and electronic devices.
    Type: Application
    Filed: January 7, 2008
    Publication date: July 24, 2008
    Inventors: Antonio Facchetti, Tobin J. Marks, He Yan
  • Patent number: 7345181
    Abstract: The present invention provides a process for preparing benzoprostacycline derivatives of formula (1), i.e. 5,6,7-trinor-4,8-inter-m-phenylene PGI2 derivatives, and vinyl tin compounds of formula (III) as starting materials for the same.
    Type: Grant
    Filed: September 18, 2003
    Date of Patent: March 18, 2008
    Assignee: Yonsung Fine Chemical Co., Ltd.
    Inventors: Yong-Hyun Kim, Yiu-Suk Lee
  • Patent number: 7138411
    Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I? wherein X, A1, A2, A3, A4, R, R?, R1 and R2 are as described in the specification.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: November 21, 2006
    Assignee: G.D. Searle & Co.
    Inventors: Jeffery S Carter, Mark G Obukowicz, Balekudru Devadas, John J Talley, David L Brown, Matthew J Graneto, Stephen R Bertenshaw, Donald J Rogier, Jr., Srinivasan Raj Nagarajan, Cathleen E Hanau, Susan J Hartmann, Cindy L Ludwig, Suzanne Metz, Donald E Korte
  • Patent number: 7138427
    Abstract: The invention discloses the use of sapogenin derivatives in the treatment of cognitive disfunction and similar conditions.
    Type: Grant
    Filed: March 28, 2002
    Date of Patent: November 21, 2006
    Assignee: Phytopharm PLC.
    Inventors: Paul Barraclough, Jim Hanson, Phil Gunning, Daryl Rees, Zongqin Xia, Yaer Hu
  • Patent number: 7122685
    Abstract: An infrared dye, characterized in that the dye comprises a compound that comprises a molecule that can be described by claim 1.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: October 17, 2006
    Assignee: Silverbrook Research Pty Ltd
    Inventors: Lachlan Everett Hall, Kia Silverbrook
  • Patent number: 7018430
    Abstract: The present invention relates to a method of mass-coloring synthetic materials, which comprises using at least one pigment dye of formula (1) wherein R and R1 together form a phenyl or heteroaryl radical and R2 is hydrogen, or R1 and R2 together form a phenyl or heteroaryl radical and R is hydrogen, and the rings A and B may each independently of the other be substituted by C1-C4?alkyl, C1–C4alkoxy, halogen, —COOR3, —CONHR4 and/or by —SR5, wherein R3, R4 and R5 are each independently of the others hydrogen, C1–C4alkyl, C6–C12aryl or heteroaryl, to synthetic materials colored with such pigment dyes, and to novel pigment dyes of formula (3), wherein R6 is hydrogen or bromine
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: March 28, 2006
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Jean-Marie Adam, Jean-Pierre Bacher
  • Patent number: 6930188
    Abstract: A stable solid hydrate of a muscarinic receptor antagonist is useful in the treatment of irritable bowel syndrome, diverticular disease, oesophageal achalasia, chronic obstructive airways disease, over active bladder (including symptoms of incontinence, urge and frequency), urinary incontinence, neurogenic urinary urgency or pollakiuria, treatment of bladder functional disorder, urinary leakage, painful or difficult urination caused by neurogenic bladder, spastic or hypertonic bladder, dysfunctional bladder syndrome, gastrointestinal disorders including gastrointestinal hyperactivity, and relaxing effect on intestinal smooth muscle cells.
    Type: Grant
    Filed: March 25, 2003
    Date of Patent: August 16, 2005
    Assignee: Novartis International Pharmaceutical, Ltd.
    Inventors: Peter James Dunn, John George Matthews, Trevor Jack Newbury, Garry O'Connor
  • Patent number: 6864225
    Abstract: Compounds of the general formula (I) are described: wherein each of R1, R2, R3, R4, R5 and R6 independently represents a substituent selected from the group consisting of hydrogen, methyl, ethyl, n-propyl, and isopropyl; an wherein x represents either 0 or 1. The compounds are useful as fragrances and as added components in fragrance blends. Methods of improving the harmony, emanation, naturalness an staying power of other fragrance ingredients by the addition of such compounds are also described.
    Type: Grant
    Filed: April 28, 2001
    Date of Patent: March 8, 2005
    Assignee: Kao Corporation
    Inventors: Thomas Markert, Theo Ten Pierik, Werner Faber
  • Patent number: 6794408
    Abstract: The present invention provides novel drechsleranol compounds of formula (I) which are formed by the microorganism Drechslera australlensis, ST 003360, DSM 14093, or a fungus ST 004112, DSM 14524, during fermentation. A process for their preparation, pharmaceutical compositions containing said drechsleranols their use for the treatment and/or prophylaxis of degenerative neuropathies, such as, Alzheimeu's disease, or psychiatric disorders, such as depression, sleep disturbance or seasonal affective disorder, and their use as chelating agents or antioxidants are also disclosed and claimed.
    Type: Grant
    Filed: January 27, 2003
    Date of Patent: September 21, 2004
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Claudia Eder, Michael Kurz, Luigi Toti
  • Patent number: 6716987
    Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)— C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: April 6, 2004
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
  • Patent number: 6703084
    Abstract: A quinone compound represented by formula (1) or (2) below: (wherein X1 to X4 independently represents an oxygen atom, sulfur atom or N—R1; R1 represents a hydrogen atom, alkyl group, aryl group or heterocyclic group; Ar1 to Ar4 independently represents an atomic group necessary for forming an aromatic ring or aromatic rings, where at least one of such aromatic rings formed by Ar1 and Ar2 and at least one of such aromatic rings formed by Ar3 and Ar4 have substituent selected from the group consisting of alkylthio group, arylthio group, heteroarylthio group and —N(R2)(R3) group; and R2 and R3 independently represents a hydrogen atom, alkyl group, aryl group or heterocyclic group, where R2 and R3 may be linked together to form a ring) was disclosed.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: March 9, 2004
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Takashi Katoh
  • Patent number: 6686348
    Abstract: A compound of formula (I): wherein: R1 represents hydrogen, halogen, alkyl or alkoxy, X represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents any one of the groups described in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitor.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: February 3, 2004
    Assignee: Les Laboratoires Servier
    Inventors: Guillaume De Nanteuil, Alain Benoist, Philippe Pastoureau, Massimo Sabatini, John Hickman, Alain Pierre, Gordon Tucker
  • Patent number: 6642217
    Abstract: Methods of treating a fungal or yeast infection and of killing or inhibiting fungi or yeast are disclosed. The methods use derivatives of triterpenes that are abundant in birch bark and other plants. The triterpenes include betulin, allobetulin, and lupeol.
    Type: Grant
    Filed: October 1, 2001
    Date of Patent: November 4, 2003
    Assignee: Naturtek, LLC
    Inventors: Pavel A. Krasutsky, Robert M. Carlson, Raj Karim
  • Publication number: 20030171427
    Abstract: The present invention provides novel drechsleranol compounds of formula (I) which are formed by the microorganism Drechslera australiensis, ST 003360, DSM 14093, or a fungus ST 004112, DSM 14524, during fermentation. A process for their preparation, pharmaceutical compositions containing said drechsleranols, their use for the treatment and/or prophylaxis of degenerative neuropathies, such as, Alzheimer's disease, or psychiatric disorders, such as depression, sleep disturbances or seasonally related affective disorders, and their use as chelating agents or antioxidants are also disclosed and claimed.
    Type: Application
    Filed: January 27, 2003
    Publication date: September 11, 2003
    Inventors: Claudia Eder, Michael Kurz, Luigi Toti
  • Patent number: 6579328
    Abstract: Sterically hindered N-substituted aryloxyamines are prepared by the transition-metal-catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitroxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.
    Type: Grant
    Filed: April 2, 2001
    Date of Patent: June 17, 2003
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Stephen D. Pastor, Sai Ping Shum
  • Patent number: 6548537
    Abstract: Compounds useful in immunosuppressive, anti-inflammatory and anticancer treatment are described. The compounds are triptolide analogs with improved water solubility and generally lower toxicity than the parent compound.
    Type: Grant
    Filed: March 2, 2001
    Date of Patent: April 15, 2003
    Assignee: Pharmagenesis, Inc.
    Inventors: Dongcheng Dai, Hongwei Yuan, John H. Musser
  • Patent number: 6547841
    Abstract: Sterically hindered N-substituted alkoxyamines are prepared by the transition-metal-catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitroxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.
    Type: Grant
    Filed: April 2, 2001
    Date of Patent: April 15, 2003
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Stephen D. Pastor, Sai Ping Shum
  • Patent number: 6514996
    Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents C
    Type: Grant
    Filed: November 19, 1997
    Date of Patent: February 4, 2003
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
  • Patent number: 6444709
    Abstract: The invention relates to novel heteroethynylenic compounds having the general formula (I): as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.
    Type: Grant
    Filed: February 7, 2000
    Date of Patent: September 3, 2002
    Assignee: Galderma Research & Development S.N.C.
    Inventors: Philippe Diaz, Jean-Michel Bernardon
  • Patent number: 6410754
    Abstract: Novel spiropyran compounds, particularly with photochromic properties, are disclosed, as well as photochromic compositions and ophthalmic articles containing said compounds. The photochromes have been designed so as to have a high colorability, a high sensitivity to activating radiation breaking the pyran ring, to be entirely or practically free from coloration in a non activated non exposed state, to have an intense coloration following activation and a high coverage of the visible spectrum in combination with at least one other photochrome, and to have high rates of coloration/decoloration. The spiropyrans are easily produced and photochemically stable, and are, e.g., of formula (i), wherein L=(a); (b).
    Type: Grant
    Filed: November 14, 1997
    Date of Patent: June 25, 2002
    Assignee: Flamel Technologies
    Inventors: Gérard Soula, You-Ping Chan
  • Patent number: 6399779
    Abstract: The invention provides a process for covalently coupling organic compounds which comprises reacting an aromatic ring compound having a halogen substituent or other substituent which undergoes substitution with a diboronic acid ester at a coupling position with a diboron derivative in the presence of a Group VIII metal catalyst and a suitable base.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: June 4, 2002
    Assignee: Commonwealth Scientific and Industrial Research Organisation
    Inventors: Sebastian Mario Marcuccio, Mary Rodopoulos, Helmut Weigold
  • Publication number: 20020049341
    Abstract: Novel spiropyran compounds, particularly with photochromic properties, are disclosed, as well as photochromic compositions and ophthalmic articles (e.g. lenses) containing said compounds. The photochromes have been designed so as to have a high colorability, a high sensitivity to activating radiation breaking the pyran ring, to be entirely or practically free from coloration in a non activated (non exposed) state, to have an intense coloration following activation and a high coverage of the visible spectrum in combination with at least one other photochrome, and to have high rates of coloration/decoloration. The spiropyrans are easily produced and photochemically stable, and are, e.g., of formula (i), wherein L=(a);(b).
    Type: Application
    Filed: November 14, 1997
    Publication date: April 25, 2002
    Inventors: GERARD SOULA, YOU-PING CHAN
  • Patent number: 6369101
    Abstract: A therapeutic method is provided for treating a mammal afflicted with a herpesvirus infection, comprising administering an effective amount of a compound of formula I: wherein R1-R11, have any of the values disclosed in the specification; or a pharmaceutically acceptable salt thereof. The invention also provides novel compounds of formula I, and pharmaceutical compositions comprising compounds of formula I.
    Type: Grant
    Filed: February 26, 1999
    Date of Patent: April 9, 2002
    Assignee: Regents of the University of Minnesota
    Inventor: Robert M. Carlson
  • Publication number: 20020032339
    Abstract: The invention provides a process for covalently coupling organic compounds which comprises reacting an aromatic ring compound having a halogen or halogen-like substituent at a coupling position with a diboron derivative in the presence of a Group VIII metal catalyst and a suitabIe base. The invention also provides useful arylboron intermediates.
    Type: Application
    Filed: December 18, 1998
    Publication date: March 14, 2002
    Inventors: SEBASTIAN MARIO MARCUCCIO, MARY RODOPOULOS, HELMUT WEINGOLD
  • Patent number: 6297363
    Abstract: The present invention relates to a novel class of glycoside indoles. More specifically, the present invention relates to a novel class of glycoside indoles isolated from Calanthe discolor Lindl. and derivatives thereof.
    Type: Grant
    Filed: February 25, 1998
    Date of Patent: October 2, 2001
    Assignee: Nomura Co., Ltd.
    Inventors: Michinori Kubo, Masayuki Yoshikawa, Hideaki Matsuda, Hisashi Matsuda, Toshiyuki Murakami, Hiromi Shimada, Tetsuo Sakurama, Manabu Nomura
  • Patent number: 6284789
    Abstract: The present invention is directed to tetrahydronaphthalene derivatives of &agr;-conindendrin, &bgr;-conindendrin, sikkimotoxin, and podophyllotoxin having at least one methyleneoxy bridge wherein the oxygen atom extends to the benzhydrylic carbon atom.
    Type: Grant
    Filed: September 2, 1999
    Date of Patent: September 4, 2001
    Assignee: The Research Foundation of State University of New York
    Inventors: Robert T. LaLonde, Frank D. Ramdayal, Mianji Zhang
  • Patent number: 6150539
    Abstract: Compounds useful in immunosuppressive and anti-inflammatory treatment are described. The compounds are hydrolyzable triptolide analogs with improved water solubility and generally lower toxicity than the parent compound.
    Type: Grant
    Filed: September 2, 1999
    Date of Patent: November 21, 2000
    Assignee: Pharmagenesis, Inc.
    Inventor: John H. Musser
  • Patent number: 6046233
    Abstract: The present invention relates to an agent for treating cor pulmonale containing as an active ingredient a prostaglandin I.sub.2 derivative represented by the following formula, or a pharmacologically acceptable salt thereof. The agent exhibits excellent effects in oral or parenteral administration.
    Type: Grant
    Filed: January 3, 1997
    Date of Patent: April 4, 2000
    Assignee: Toray Industries, Inc.
    Inventors: Reiji Kasukawa, Masayuki Miyata, Yuji Ueno, Hiroshi Koike, Hajimu Kurumatani, Shintaro Nishio
  • Patent number: 6034256
    Abstract: A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I' ##STR1## wherein X, A.sup.1, A.sup.2, A.sup.3, A.sup.4, R, R", R.sup.1 and R.sup.2 are as described in the specification.
    Type: Grant
    Filed: April 17, 1998
    Date of Patent: March 7, 2000
    Assignee: G.D. Searle & Co.
    Inventors: Jeffery S Carter, Mark G Obukowicz, Balekudru Devadas, John J Talley, David L Brown, Matthew J Graneto, Stephen R Bertenshaw, Donald J Rogier, Jr., Srinivasan R Nagarajan, Cathleen E Hanau, Susan J Hartmann, Cindy L Ludwig, Suzanne Metz
  • Patent number: 6028101
    Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring that is furan;A is selected from --C(X)-amine, --C(O)--SR.sub.3, --NH--C(X)R.sub.4, and --C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W is selected from --C(R.sub.3).sub.p H.sub.(2-p) --, --N(R.sub.3).sub.m H.sub.(1-m) --, --S(O).sub.p --, and --O--;X is O or S;n is 2;m is 0 or 1;p is 0, 1, or 2;R, R.sub.2, R.sub.3, R.sub.4 and R.sub.7 are herein defined;or an agronomic salt thereof.
    Type: Grant
    Filed: August 7, 1997
    Date of Patent: February 22, 2000
    Assignee: Monsanto Company
    Inventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
  • Patent number: 5972997
    Abstract: The present invention relates to UCT1072 compounds represented by formula (I): wherein R.sup.1 and R.sup.2 together represent --CH(OH)CH.sub.2 O-- or --CH.sub.2 CH.sub.2 CH(OH)CH.sub.2 --.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: October 26, 1999
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Tamio Mizukami, Akira Asai, Katsuhiko Ando, Shingo Kakita, Akira Mihara, Katsunori Kita, Yasuhiro Suzuki, Tadashi Ashizawa
  • Patent number: 5965718
    Abstract: Sarcodictyin A and B, eleutherobin, and bioactive analogs thereof synthesized using solid phase and solution phase chemistries. The synthetic method employs an attachment of common precursors, e.g., compounds 1880 or 200, on a solid support for generating conjugates 230 and 240, followed by standard chemical manipulations. A combinatorial library of sarcodictyins and eletherobin analogs was constructed with modified C-8 ester, C-15 ester and C-4 ketal functionalities and was screened for activity with respect to tubulin polymerization and cytotoxic activity against tumor cells, including Taxol-resistant lines. Compounds 600, 610, 630, 660-700, 730, 760, 850, and 920 were identified to be of equal or superior biological activities as compared to their corresponding natural product.
    Type: Grant
    Filed: September 1, 1998
    Date of Patent: October 12, 1999
    Assignee: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, Floris VanDelft, Seijiro Hosokawa, Sanghee Kim, Tianhu Li, Takashi Ohshima, Jeff Pfefferkorn, Dionisios Vourloumis, Jin-You Xu, Nicolas Winssinger
  • Patent number: 5952371
    Abstract: The compounds of Formula I ##STR1## are useful as iumnunosuppressive agents.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: September 14, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht
  • Patent number: 5874594
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: February 23, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht
  • Patent number: 5728849
    Abstract: New taxoids of general formula (I): ##STR1## wherein Z represents a hydrogen atom or a radical of general formula: ##STR2## in which R.sub.1 represents an optionally substituted benzoyl radical, a thenoyl or furoyl radical or a radical R.sub.2 --O--CO-- in which R.sub.2 represents an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl or phenyl radical, optionally substituted, or a heterocyclic radical,R.sub.3 represents an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl, naphthyl or aromatic heterocyclic radical,either R.sub.4 represents a hydrogen atom,R.sub.6 and R.sub.7 together form a ketone function, andR and R.sub.5 together form a bond,or R.sub.4 represents a hydrogen atom or ahydroxyl radical or an alkoxy, alkenyloxy or alkynyloxy radical, optionally substituted, an alkanoyloxy, aryloxy, alkenoyloxy, alkynoyloxy, cycloalkanoyloxy, alkoxyacetyl, alkylthioacetyl, alkyloxycarbonyloxy, cycloalkyloxy, cycloalkenyloxy, carbamoyloxy, alkylcarbamoyloxy or dialkylcarbamoyloxy radical,R.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: March 17, 1998
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Herve Bouchard, Alain Commer.cedilla.on
  • Patent number: 5663379
    Abstract: Compounds of the formula ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in claim 1 can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: September 2, 1997
    Assignee: Ciba-Geigy Corporation
    Inventor: Friedrich Karrer
  • Patent number: 5635107
    Abstract: Fluorine-containing five-membered ring compounds of the formula IR.sup.1 -(A.sup.1 -Z.sup.1).sub.m -A.sup.2 -Z.sup.2 -W Iin whichW is ##STR1## is a cyclohexane, cyclohexene or phenyl,Y.sup.1 is O or S,Y.sup.2 is (a) O, S, C.dbd.O or fluoroalkyl,Y.sup.3 is (a) N, CH or CF,Q is C.dbd.O, CHF, CF.sub.2, CHR.sup.2 or CFR.sup.2Q' is CF or CR.sup.2,R.sup.2 is C.sub.1-15 -alkyl, optionally at least mono-substituted by F,X is H, F or Cl,R.sup.1 H or hydrocarbyl,A.sup.1 and A.sup.2 are a carbocyclic, aromatic or heterocyclic radicalZ.sup.1 and Z.sup.2 are --CO--O, --O--CO--, --CH.sub.2 O--, --O--CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.ident.C-- or a single bond, andm is 0, 1 or 2, and liquid-crystalline media containing same.
    Type: Grant
    Filed: January 8, 1993
    Date of Patent: June 3, 1997
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Ekkehard Bartmann, Georg Weber
  • Patent number: 5585505
    Abstract: The invention is directed to a hatching agent for hatching the species and patho types of nematodes causing potation sickness, which nematodes comprise Globodera pallida, from the cysts thereof, with a molecular weight of 498, a component C.sub.27 H.sub.30 O.sub.9 and the structure of formula (a) and the derivatives, esters and salts thereof.
    Type: Grant
    Filed: June 1, 1994
    Date of Patent: December 17, 1996
    Assignee: B.V. Chemische Pharmaceutische Industrie "Luxan"
    Inventors: Johan G. Mulder, Pieter Diepenhorst, Pieter Plieger, Ingrid E. M. Br uggemann-Rotgans
  • Patent number: 5290553
    Abstract: A method of preparing substantially purified alkaloids from seeds, stems, uit-rind and bark of a plant selected from Picralima nitida, Gongronema latifolia, Dorstenia multiradiata, Cola attiensis, Rothmania withfieldii and Desmodium gangeticum, for use in the treatment of protozoal diseases, comprising:pulverizing said plant;a first solvent, drying the extracted material and re-extracting the dried material with a different solvent;extracting a fresh sample of said plant with boiling water;filtering and concentrating the boiling water solvent extracts under reduced pressure;concentrating the dried extract to a gum and re-extracting said gum with an aqueous acidic HCl solution;filtering the acidic extract and making it alkaline to a pH of about 9 with a concentration NaOH solution;extracting the alkaline solution with dichloromethane;concentrating organic layers of the extracted alkaline solution to dryness under reduced pressure to obtain an alkaloid fraction; andseparating the alkaloid fraction by liquid chr
    Type: Grant
    Filed: July 22, 1991
    Date of Patent: March 1, 1994
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: Maurice M. Iwu, Daniel L. Klayman, Joan E. Jackson, John D. Tally, Steven L. Andersen
  • Patent number: 5284870
    Abstract: The present invention relates to an aldose reductase inhibitor represented by the formula: ##STR1## wherein R.sub.1 is (CH.sub.2).sub.2 COOH and R.sub.2 is phenyl or p-hydroxyphenyl, or R.sub.1 and R.sub.2 are combined together to form a group of the formula: ##STR2## which was isolated from the fermentation products of Chaetomella circinoseta RF-3192.
    Type: Grant
    Filed: February 9, 1993
    Date of Patent: February 8, 1994
    Assignee: Shionogi Seiyaku Kabushiki Kaisha
    Inventors: Tadashi Yoshida, Toshiyuki Kato, Yoshimi Kawamura, Koichi Matsumoto, Hiroshi Itazaki
  • Patent number: 5122361
    Abstract: Novel CNS dopamine D-2 receptors, such as the compound 5-iodo-7-N-[(1-ethyl-2-pyrrolidinyl)methyl]carboxamide-2,3-dihydrobenzofur an, are disclosed. These compounds are useful as imaging agents for D-2 receptors in the human brain and exhibit good brain retention and in vivo stability.
    Type: Grant
    Filed: April 17, 1989
    Date of Patent: June 16, 1992
    Assignee: Trustees of the University of Pennsylvania
    Inventors: Hank F. Kung, Raymond Murphy
  • Patent number: 5112977
    Abstract: Substituted naphthacenediones of the formula I ##STR1## in which R.sup.1 to R.sup.8 are H and at least one of R.sup.1 to R.sup.8, for example R.sup.2 and R.sup.3 or R.sup.2 and R.sup.6, are, for example, C.sub.1 -C.sub.20 alkoxy, C.sub.1 -C.sub.20 alkenoxy, C.sub.1 -C.sub.20 -alkylsulfinyl, --CN, --CF.sub.3, --NO.sub.2, --Si(CH.sub.3).sub.3 or --COO(C.sub.1 -C.sub.12 alkyl), are suitable, when incorporated into polymers having hydroxyalkyl groups, for currentless deposition of metals onto the polymer surface. They are in some cases suitable as photoinitiators.
    Type: Grant
    Filed: May 24, 1989
    Date of Patent: May 12, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Fischer, Marcus Baumann, Jurgen Finter, Vratislav Kvita, Carl W. Mayer, Wolfgang Wernet
  • Patent number: 5047554
    Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.
    Type: Grant
    Filed: January 31, 1990
    Date of Patent: September 10, 1991
    Assignee: Pfizer Inc.
    Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
  • Patent number: 4990529
    Abstract: 2-Pyrazoline derivatives of the formula (A): ##STR1## where R.sup.1 is a pyridyl, a pyrazyl or an alkoxyl group; and R.sup.2 is a hydrogen atom, an alkyl, a pyridyl, a furyl, phenyl or a substituted phenyl group, and to a process for producing the same. Therapeutic agents for treating cerebrovascular diseases containing, as the active ingredient, a 2-pyrazoline derivative represented by the formula (G): ##STR2## where R.sup.3 is a hydrogen atom, an alkyl, acetyl, an alkoxycarbonyl, an amino, benzoyl, a substituted benzoyl, a pyridylcarbonyl, a furylcabonyl, a thienylcarbonyl, a pyrazylocarbonyl, an N-substituted carbamoyl, an N-substituted thiocarbamoyl, or carboxyl group; and R.sup.4 is a hydrogen atom, an alkyl, a pyridyl, a thienyl, a furyl, cyclohexyl, phenyl or a substituted phenyl group or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: February 5, 1991
    Assignee: Mitsui Toatsu Chemicals
    Inventors: Hiroyuki Yamashita, Makoto Odate, Hajime Iizuka, Hiroshi Kawazura, Yoshio Shiga, Hiroshi Namekawa
  • Patent number: 4960791
    Abstract: Derivatives of salannin, including 2',3',20,21,22,23-hexahydro salannin and 20,21,22,23-tetrahydro salannin derivatives, having up to 40-fold greater insect antifeedant activity than native salannin.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: October 2, 1990
    Assignee: NPI
    Inventors: James A. Klocke, Ronald B. Yamasaki
  • Patent number: 4935532
    Abstract: All possible isomeric forms of a compound of the formula ##STR1## wherein A has a structure selected from the group consisting of ##STR2## wherein Y.sub.1 and Y.sub.2 are individually selected from the group consisting of hydrogen, fluorine, chlorine, bromine and alkyl of 1 to 6 carbon atoms, or Y.sub.1 and Y.sub.2 together with the carbon to which they are attached form a carbon homocycle of 3 to 7 carbon atoms and Z is selected from the group consisting of hydrogen, chlorine, bromine and iodine, Y is selected from the group consisting of hydrogen, alkyl of 1 to 18 carbon atoms unsubstituted or substituted with at least one halogen, the .beta., .alpha. bond together with Y can be part of A and and R is selected from the group consisting of non-heterocyclic primary, secondary or teritiary alcohol moiety having at least one asymetric carbon or the remainder of a substituted alcohol with a chirality due to the dissymetric spatial configuration of the entire molecule.
    Type: Grant
    Filed: May 25, 1988
    Date of Patent: June 19, 1990
    Assignee: Roussel Uclaf
    Inventors: Jean Tessler, Jean-Pierre Demoute
  • Patent number: 4788305
    Abstract: Compounds of the formula ##STR1## wherein A is a hydrocarbon chain containing 1 to 16 groups, the said chain containing at least one heteroatom, at least one unsaturation, the assembly of the group constituting the chain may be a mono- or polycyclic system including a spiro or endosystem and the assembly of chain A and the carbon atoms attached thereto can contain at least one chiral atom or the hemiacetal moiety thereto which can present a chirality due to the dissymetric spatial configuration of the molecule and Y is selected from the group consisting of hydrogen, alkyl of 1 to 18 carbon atoms optionally substituted, --CY.sub.3 ' and the .beta.,.gamma. bond together with Y can be part of A and Y' is bromine or chlorine.
    Type: Grant
    Filed: July 17, 1987
    Date of Patent: November 29, 1988
    Assignee: Roussel Uclaf
    Inventors: Jean Tessier, Jean-Pierre Demoute