The Tricyclo Ring System Consists Of Three Six-membered Cyclos (e.g., Xanthene, Etc.) Patents (Class 549/388)
  • Patent number: 6887533
    Abstract: Compounds of the formula (I) where: X1 is H or F G1-G2 is —CH2—CH— or CH?C— R1, R2 are a) H b) the M2-A2-R5 moiety c) for example, a straight-chain or branched alkyl radical having from 1 to 16 carbon atoms R3 and R4 are each, for example, H, the M2-A2-R5 moiety or a straight-chain or branched alkyl or alkyloxy radical having from 1 to 16 carbon atoms A2 is, for example, 1,4-phenylene, with the provisos that a) when R2 is not H, R1 and R3 have to be H, b) when R2 is H, R4 must not have the definitions c) or d), c) R1, R2, R3 and R4 must not at the same time be H.
    Type: Grant
    Filed: March 24, 2004
    Date of Patent: May 3, 2005
    Assignee: Clariant International, Ltd.
    Inventors: Wolfgang Schmidt, Barbara Hornung, Rainer Wingen
  • Publication number: 20040245498
    Abstract: Compounds of the formula (I) 1
    Type: Application
    Filed: March 24, 2004
    Publication date: December 9, 2004
    Inventors: Wolfgang Schmidt, Barbara Hornung, Rainer Wingen
  • Patent number: 6750244
    Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: April 2, 2001
    Date of Patent: June 15, 2004
    Assignee: NPS Pharmaceuticals, Inc.
    Inventors: Alan L. Mueller, Scott T. Moe
  • Patent number: 6730519
    Abstract: A method for the isolation of delta-9-tetrahydrocannibinol (THC) from, Cannabis plant material, wherein delta-9-THC Acid and THC are separately obtained including the steps of extracting the Cannabis plant material, chelating delta-9-THC acid on alumina solid support from cannabis extracts rich in the acid washing of non-acid components of the extract with organic solvents and eluting of the delta-9-THC acid with strong polar solvents.
    Type: Grant
    Filed: December 4, 2001
    Date of Patent: May 4, 2004
    Assignee: The University of Mississippi
    Inventors: Mahmoud A. Elsohly, Samir A. Ross
  • Patent number: 6696569
    Abstract: Novel compounds comprising a C—C double bond substituted at one carbon with two oxygen or sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence by reaction with a peroxidase enzyme and a peroxide. The chemiluminescence thus produced can be used as a detectable signal in assays for peroxidase enzymes and in assays employing enzyme-labeled specific binding pairs.
    Type: Grant
    Filed: April 11, 2001
    Date of Patent: February 24, 2004
    Assignee: Lumigen, Inc.
    Inventors: Hashem Akhavan-Tafti, Zahra Arghavani, Renuka DeSilva
  • Patent number: 6620842
    Abstract: Disclosed are novel chalcone derivatives having the formula (I) The compounds possess antiproliferative activity and are useful for the manufacture of a medicament for the treatment or prevention of neoplasms, particularly those located in the uterus, ovary or breast. The compounds of the invention may also be useful in the manufacture of a medicament for the treatment or prevention of menopausal disorders and osteoporosis.
    Type: Grant
    Filed: February 15, 2002
    Date of Patent: September 16, 2003
    Assignee: Indena SpA
    Inventors: Ezio Bombardelli, Piero Valenti
  • Publication number: 20030158127
    Abstract: The present invention discloses novel sulfenate derivatives and their bioconjugates for phototherapy of tumors and other lesions. The sulfenates of the present invention are designed to absorb low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of free radicals, the reactive intermediate produced upon photofragmentation of the sulfenate moiety, with the tissue of interest.
    Type: Application
    Filed: July 3, 2001
    Publication date: August 21, 2003
    Applicant: MALLINCKRODT INC.
    Inventors: Raghavan Rajagopalan, Gary L. Cantrell, Samuel I. Achilefu, Joseph E. Bugaj, Richard B. Dorshow
  • Patent number: 6608089
    Abstract: Compounds having the formula (I) Z—OCH2—C≡CCH2—NRR1  (I) or a pharmaceutically acceptable salt or solvate thereof wherein Z can represent the formula (1A) or (1B). The compounds possess antiproliferative activity and are useful as modulators of multiple drug resistance in cancer chemotherapy. The compounds may also be useful for the manufacture of a medicament for the treatment or prevention of neoplasms, menopausal disorders and osteoporosis.
    Type: Grant
    Filed: February 15, 2002
    Date of Patent: August 19, 2003
    Assignee: Indena S.p.A.
    Inventors: Ezio Bombardelli, Piero Valenti
  • Patent number: 6472414
    Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X,  are as defined herein.
    Type: Grant
    Filed: May 18, 1999
    Date of Patent: October 29, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
  • Patent number: 6465625
    Abstract: Highly specific biocatalytic reactions have been used to create a population of taxol derivatives.
    Type: Grant
    Filed: June 19, 2000
    Date of Patent: October 15, 2002
    Assignee: Albany Molecular Research, Inc.
    Inventors: Jonathan S. Dordick, Douglas S. Clark, Peter C. Michels, Yuri L. Khmelnitsky
  • Publication number: 20020137225
    Abstract: A compound represented by the following formula (I): 1
    Type: Application
    Filed: May 8, 2002
    Publication date: September 26, 2002
    Applicant: Daiichi Pure Chemicals Co., Ltd.
    Inventors: Tetsuo Nagano, Hirotatsu Kojima
  • Publication number: 20020091150
    Abstract: The present invention is a compound of formula 1
    Type: Application
    Filed: December 10, 2001
    Publication date: July 11, 2002
    Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jurgen Wichmann, Thomas Johannes Woltering
  • Patent number: 6403812
    Abstract: Long wavelength, narrow emission bandwidth fluorecein dyes are provided for detecting spacially overlapping target substances. The dyes comprise 4,7-dichlorofluoresceins, and particularly 2′,4′,5′,7′-tetrachloro-4,7-dicloro-5- (and 6-) carboxyfluoresceins. Methods and kits for using the dyes in DNA analysis are provided.
    Type: Grant
    Filed: May 30, 2000
    Date of Patent: June 11, 2002
    Assignee: The Perkin-Elmer Corporation
    Inventors: Steven M. Menchen, Linda G. Lee, Charles R. Connell, N. Davis Hershey, Vergine Chakerian, Sam L. Woo, Steven Fung
  • Patent number: 6372907
    Abstract: The present invention provides novel, water-soluble, red-emitting fluorescent rhodamine dyes and red-emitting fluorescent energy-transfer dye pairs, as well as labeled conjugates comprising the same and methods for their use. The dyes, energy-transfer dye pairs and labeled conjugates are useful in a variety of aqueous-based applications, particularly in assays involving staining of cells, protein binding, and/or analysis of nucleic acids, such as hybridization assays and nucleic acid sequencing.
    Type: Grant
    Filed: September 14, 2000
    Date of Patent: April 16, 2002
    Assignee: Apptera Corporation
    Inventors: Linda G. Lee, Ronald J. Graham, William E. Werner, Elana Swartzman, Lily Lu
  • Publication number: 20020039795
    Abstract: A method of preparing tetrahydrocannabinol using extraction of plant material with a non-polar solvent followed by vacuum distillation and collection of a constant boiling fraction. Additional distillation steps and chromatographic steps, including HPLC reversed phase HPLC and flash chromatography, may be performed.
    Type: Application
    Filed: October 26, 1998
    Publication date: April 4, 2002
    Applicant: Elsohly Et Al
    Inventors: MAHMOUD A. ELSOHLY, SAMIR A. ROSS
  • Patent number: 6365416
    Abstract: A method of preparing THC using extraction of plant material with a non-polar solvent followed by vacuum distillation and chromatography.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: April 2, 2002
    Assignee: The University of Mississippi
    Inventors: Mahmoud A. Elsohly, Samir A. Ross
  • Patent number: 6355650
    Abstract: The present invention relates to non-psychoactive derivatives of tetrahydro-cannabinol, which exhibit anti-inflammatory, analgesic and leukocyte antiadhesion activities. The invention includes novel derivatives of (3R,4R)-&Dgr;8-tetrahydrocannabinol-11-oic acids [hereinafter referred to as (3R,4R)-&Dgr;8-THC-11-oic acid], as well as pharmaceutical compositions containing the (3R,4R)-&Dgr;8-THC-11-oic acid derivatives. The invention further covers methods of administering the novel derivatives and pharmaceutical compositions as therapeutic agents in the treatment of pain and tissue inflammation. Non-psychoactive derivatives of &Dgr;8-THC-11-oic acid are described which have analgesic and anti-inflammatory properties.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: March 12, 2002
    Assignee: Atlantic Technology Ventures, Inc.
    Inventor: Sumner H. Burstein
  • Patent number: 6340691
    Abstract: Compounds of the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: January 22, 2002
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, Aranapakam M. Venkatesan, Derek C. Cole, James M. Chen, Jamie M. Davis, George T. Grosu
  • Patent number: 6329377
    Abstract: The present invention is directed to novel ketomethylene group-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: December 11, 2001
    Assignee: Cephalon, Inc.
    Inventor: Sankar Chatterjee
  • Publication number: 20010041802
    Abstract: 1
    Type: Application
    Filed: February 28, 2001
    Publication date: November 15, 2001
    Inventors: Philip R. Kym, Benjamin C. Lane, John K. Pratt, Tom Von Geldern, Martin Winn, Jehrod Brenneman, Jyoti R. Patel, David L. Arendsen, Irini Akritopoulou-Zanze, Kimba L. Ashworth, Kresna Hartandi
  • Patent number: 6288234
    Abstract: Disclosed are multibinding compounds which inhibit microsomal triglyceride transferase protein (MTP), a protein which mediates the transfer of lipids during the assembly of lipoproteins and related biomolecules. The multibinding compounds contain from 2 to 10 ligands covalently attached to one or more linkers. The multibinding compounds of this invention are useful for lowering serum lipid, cholesterol and/or triglyceride levels, and for preventing and treating disorders associated with hyperlipemia, hyperlipidemia, hyperlipoproteinemia, hypercholestrolemia, hypertriglyceridemia and the like, such atherosclerosis.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: September 11, 2001
    Assignee: Advanced Medicine, Inc.
    Inventor: John H. Griffin
  • Publication number: 20010012901
    Abstract: The present invention relates to a linker shown by the following formula (I):
    Type: Application
    Filed: March 21, 2001
    Publication date: August 9, 2001
    Applicant: Fujisawa Pharmaceutical Co. Ltd.
    Inventors: Akito Tanaka, Hideo Tsutsumi
  • Patent number: 6245807
    Abstract: We have now discovered that unexpectedly compounds of the following formulae I or 11 can be used to selectively stimulate the death of mammalian prostate cells, including both epithelial cell and prostate cancer cells, and thus are useful in treating prostate diseases: wherein R and R1 are each independently selected from the group consisting of hydrogen, hydroxy, thio (SH), halogen, substituted and unsubstituted alkyl, substituted and unsubstituted alkenyl, substituted and unsubstituted aryl, and substituted and unsubstituted alkoxy, and salts thereof, wherein the dotted double bond between the ring carbons to which R and R1 are bonded represent an optional ring double bond. Preferred compounds of formula I include those in which at least one of the substituents R and R1 is hydrogen and/or at least one of said substituents is allyl. Specifically preferred compounds include &bgr;-lapachone (i.e., R and R1 both being hydrogen), allyl-&bgr;-lapachone, particularly 3-allyl-&bgr;-lapachone (i.e.
    Type: Grant
    Filed: February 24, 1998
    Date of Patent: June 12, 2001
    Assignee: Dana-Farber Cancer Institute
    Inventors: Arthur Pardee, Chiang J. Li
  • Patent number: 6211201
    Abstract: A quaternary ammonium cholinergic agent is complexed with a multivalent anion, or with multiple monovalent anions. The complex may be administered orally to a patient to treat pain, or for some other purpose. Numerous modifications are contemplated, including modifications to the ring structure of the compound, substitution and functionalization of the ring. Other contemplated modifications include the use of different anions, including various monovalent and polyvalent anions, and both organic and inorganic anions. The compounds have utility as cholinergic agents, and especially in the treatment of mysasthenia gravis, chest pain, and carpal tunnel syndrome.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: April 3, 2001
    Assignee: ICN Pharmaceuticals, Inc.
    Inventors: Colin Granger, Robert Orr, Kandasamy Ramasamy
  • Patent number: 6191278
    Abstract: The present invention provides novel, water-soluble, red-emitting fluorescent rhodamine dyes and red-emitting fluorescent energy-transfer dye pairs, as well as labeled conjugates comprising the same and methods for their use. The dyes, energy-transfer dye pairs and labeled conjugates are useful in a variety of aqueous-based applications, particularly in assays involving staining of cells, protein binding, and/or analysis of nucleic acids, such as hybridization assays and nucleic acid sequencing.
    Type: Grant
    Filed: November 3, 1999
    Date of Patent: February 20, 2001
    Assignee: PE Corporation
    Inventors: Linda G. Lee, Ronald J. Graham, William E. Werner, Elana Swartzman, Lily Lu
  • Patent number: 6172058
    Abstract: A pharmaceutical compound of the formula in which R1 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-10 alkyl, C3-10 cycloalkyl-C2-10 alkenyl, C3-10 cycloalky-C2-10 alkynyl, optionally substituted phenyl-C1-10 alkyl, optionally substituted phenyl-C2-10 alkenyl, optionally substituted phenyl-C2-10 alkynyl, optionally substituted naphthyl, optionally substituted naphthyl-C1-10 alkyl, C1-10 alkoxy-C1-10 alkyl, C3-10 cycloalkoxy-C1-10 alkyl, optionally substituted heterocyclyl, optionally substituted heterocyclyl-C1-10 alkyl, optionally substituted phenyl fused to C5-10 cycloalkyl, optionally substituted tricyclic, optionally substituted tricyclic-C1-10 alkyl, or [optionally substituted phenyl(CH2)n]2-C1-10 alkyl, where n is 0 or 1 to 4, and R2 is hydrogen or one of the values for R1; or a salt or ester thereof.
    Type: Grant
    Filed: April 3, 1998
    Date of Patent: January 9, 2001
    Assignee: Lilly, SA
    Inventors: Concepci{acute over (o)}n Pedregal Tercero, Ivan Collado Cano, Angel Maz{acute over (o)}n Ruiz
  • Patent number: 6166226
    Abstract: A method for preparing an aryl ether compound is provided in which an alcohol is reacted with an aromatic compound in the presence of a base, and a transition metal catalyst selected from the group consisting of platinum and nickel to form an aryl ether. The aromatic compound comprises an activated substituent, X, said activated substituent being a moiety such that its conjugate acid HX has a pKa of less than 5.0. The catalyst is preferably a soluble palladium complex in the presence of supporting ligands.
    Type: Grant
    Filed: December 8, 1998
    Date of Patent: December 26, 2000
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, John P. Wolfe, Michael Palucki
  • Patent number: 6136961
    Abstract: Highly specific biocatalytic reactions have been used to create a population of derivatives from a single starting compound. Examples demonstrate synthesis of derivatives of taxol, taxol-2'-adipate, taxol-2'-vinyl adipate, 2,3-(methylenedioxy) benzaldehyde, (.+-.)-(2-endo, 3-exo)-bicyclo (2.2.2)octo-5-ene-2,3-dimethanol, adenosine and erythromycin.
    Type: Grant
    Filed: June 29, 1998
    Date of Patent: October 24, 2000
    Assignee: EnzyMed, Inc.
    Inventors: Jonathan S. Dordick, Douglas S. Clark, Peter C. Michels, Yuri L. Khmelnitsky
  • Patent number: 6127415
    Abstract: The present invention relates to specific adamantyl or adamantyl group derivative containing retinoid compounds induce apoptosis of cancer cells. These adamantyl retinoid derivatives are useful for the treatment of many cancers and solid tumors, especially androgen-independent prostate cancer, skin cancer, pancreatic carcinomas, colon cancer, melanoma, ovarian cancer, liver cancer, small cell lung carcinoma, non-small cell lung carcinoma, cervical carcinoma, brain cancer, bladder cancer, breast cancer, neuroblastoma/glioblastoma, and leukemia. Also, the invention relates to novel adamantyl or adamantyl group derivative compounds which are useful as active agents for the treatment or prevention of keratinization disorders and other dermatological conditions, and other diseases.
    Type: Grant
    Filed: April 14, 1999
    Date of Patent: October 3, 2000
    Assignee: Galderma Research & Development, S.N.C.
    Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
  • Patent number: 6124484
    Abstract: The present invention provides a method for the preparation of triarylmethyl protecting group reagents. The reagents are prepared from reaction effluent from the cleavage step of oligonucleotide synthetic regimes.
    Type: Grant
    Filed: July 17, 1998
    Date of Patent: September 26, 2000
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Yogesh S. Sanghvi, Zhiqiang Guo
  • Patent number: 6054448
    Abstract: Compounds of the formula ##STR1## in which R.sup.1 is Y or Y--C.sub.1-6 alkyl, where Y is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or optionally substituted phenyl-C.sub.1-6 alkyl,and R.sup.2, R.sup.3, R.sup.4, X and Z are as defined in the specification, possess affinity for metabotropic glutamate receptors and are useful in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: October 17, 1997
    Date of Patent: April 25, 2000
    Assignee: Eli Lilly and Company Limited
    Inventors: Barry Peter Clark, John Richard Harris
  • Patent number: 5977077
    Abstract: Therapeutic compositions for the treatment of infectious diseases are disclosed. These compositions comprise xanthones and xanthone derivatives, such as 2,3,4,5,6-pentahydroxyxanthone. Also disclosed are methods for the treatment of infectious diseases using such compounds.
    Type: Grant
    Filed: March 20, 1996
    Date of Patent: November 2, 1999
    Assignee: Interlab Corporation
    Inventors: Rolf Walter Winter, Michael Kevin Riscoe, David J. Hinrichs
  • Patent number: 5965605
    Abstract: Disclosed are chemical agents with unexpected activity to inhibit the interactions between human immunoglobulin E (IgE) and its receptor (Fc.epsilon.RI) which interactions are known to be involved in triggering allergic responses. The agents may be used to module the allergic response in the treatment of various clinical conditions, including rhinitis, asthma, urticaria, atopic dermatitis, and anaphylacric shock. The agents can be formulated for oral, topical or parenteral administration.
    Type: Grant
    Filed: December 29, 1997
    Date of Patent: October 12, 1999
    Assignee: Heska Corporation
    Inventors: Y.-S. Edmond Cheng, Yuan Liu, John Chu, Jean-Pierre Kinet, Marie-Helene Jouvin, Yukio Sudo, Xiuqi Qian
  • Patent number: 5932726
    Abstract: The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1- benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
    Type: Grant
    Filed: April 11, 1997
    Date of Patent: August 3, 1999
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Michael Ernest Pierce, Anusuya Choudhury, Rodney Lawrence Parsons, Jr., Lilian Alicia Radesca
  • Patent number: 5919846
    Abstract: A novel colorant compound is provided which is the addition product of an organic chromophore having at least one reactive hydroxyl or amine substituent, a polyisocyanate, and a carboxylic acid, sulfonic acid, or salt of either thereof. The polyisocyanate, added in a molar excess relative to the number of such reactive substituents, reacts with the reactive hydroxyl or amine groups to provide terminal isocyanate groups. Subsequently, the carboxylic acid or salt thereof, also added in an amount excessive in relation to the number of terminal isocyanate groups, reacts therewith to from urethane moieties on the colorant. Such a compound provides excellent ink compositions upon dilution and are very soluble within all the standard ink diluents. Furthermore, such colorants provide good jettability, waterfastness, washfastness, and the like, within ink-jet applications on various types of printing substrates.
    Type: Grant
    Filed: February 19, 1998
    Date of Patent: July 6, 1999
    Assignee: Milliken Research Corporation
    Inventors: Raj Batlaw, John W. Miley
  • Patent number: 5877030
    Abstract: Methods for forming combinatorial libraries and the libraries produced thereby are provided. According to a preferred aspect of the invention, a plurality of core molecules are reacted with a plurality of different tool molecules to form a library of molecules having non-naturally occurring molecular diversity. The libraries are useful for identifying lead compounds which modulate the functional activity of a biological molecule. Protease inhibitors that have been isolated from the libraries also are disclosed.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: March 2, 1999
    Inventors: Julius Rebek, Jr., Thomas Carell, Edward A. Wintner
  • Patent number: 5847166
    Abstract: A method for preparing an aryl ether compound is provided in which an alcohol is reacted with an aromatic compound in the presence of a base, and a transition metal catalyst selected from the group consisting of platinum and nickel to form an aryl ether. The aromatic compound comprises an activated substituent, X, said activated substituent being a moiety such that its conjugate acid HX has a pKa of less than 5.0. The catalyst is preferably a soluble palladium complex in the presence of supporting ligands.
    Type: Grant
    Filed: October 10, 1996
    Date of Patent: December 8, 1998
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, John P. Wolfe, Michael Palucki
  • Patent number: 5827877
    Abstract: The present invention is directed to novel ketomethylene group-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.
    Type: Grant
    Filed: May 7, 1996
    Date of Patent: October 27, 1998
    Assignee: Cephalon, Inc.
    Inventor: Sankar Chatterjee
  • Patent number: 5811389
    Abstract: There are described compounds of the formula ##STR1## Wherein the variables have been defined herein. The compounds are useful as research tools in the determination of biologically active peptides sequences and also potentially suitable as medicaments, some of them being useful in the prevention or control of the formation of blood platelet thrombi, and some compounds are useful as intermediates.
    Type: Grant
    Filed: June 24, 1996
    Date of Patent: September 22, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Wilhelm Bannwarth, Fernand Gerber, Alfred Grieder, Andreas Knierzinger, Klaus Muller, Daniel Obrecht, Arnold Trzeciak
  • Patent number: 5770378
    Abstract: Tricyclic retinoids having activity for retinoic acid receptors and/or retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such tricyclic retinoid compounds and methods for their therapeutic use.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 23, 1998
    Assignee: Ligand Pharmaceuticals, Inc.
    Inventors: Chan Kou Hwang, Steven K. White, Youssef L. Bennani, Stacie S. Canan Koch, Beth Ann Badea, Jonathan J. Hebert, Alex M. Nadzan
  • Patent number: 5770382
    Abstract: Tricyclic retinoids having activity for retinoic acid receptors and/or retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such tricyclic retinoid compounds and methods for their therapeutic use.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 23, 1998
    Assignee: Ligand Pharmaceuticals, Inc.
    Inventors: Chan Kou Hwang, Steven K. White, Beth Ann Badea, Alex M. Nadzan
  • Patent number: 5770383
    Abstract: Tricyclic retinoids having activity for retinoic acid receptors and/or retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such tricyclic retinoid compounds and methods for their therapeutic use.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 23, 1998
    Assignee: Ligand Pharmaceuticals, Inc.
    Inventors: Chan Kou Hwang, Steven K. White, Youssef L. Bennani, Stacie S. Canan Koch, Beth Ann Badea, Jonathan J. Hebert, Luc J. Farmer, Alex M. Nadzan
  • Patent number: 5760246
    Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2;R.sup.x is H, alkyl, aryl or halogen;A is(1) a bond;(2) --O--; or(3) ##STR2## B is: ##STR3## and wherein L.sup.2, L.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.3', R.sup.3a, R.sup.3b, R.sup.4, R.sup.4', R.sup.5, X, ##STR4## are as defined herein.
    Type: Grant
    Filed: December 17, 1996
    Date of Patent: June 2, 1998
    Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
  • Patent number: 5686586
    Abstract: A polycyclic aromatic compound having the formula ##STR1## and its salts have useful therapeutic and cosmetic action particularly in psoriasis.In the formula, X represents --CH.dbd.CH--, O or S,R.sub.1 represents hydrogen, branched alkyl having 3-15 carbon atoms, alkoxy having 1-6 carbon atoms or 1-adamantyl, R.sub.2 represents hydroxy, hydrogen, linear or branched alkyl having 1-15 carbon atoms or alkoxy having 1-6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are not simultaneously hydrogen, or R.sub.1 and R.sub.2 together with the adjacent carbon atoms of the naphthalene ring form a 5 or 6 chain ring optionally substituted by at least one lower alkyl radical, or interrupted by an oxygen atom,R.sub.3 represents --CH.sub.2 OH or --COR.sub.4, or --CH.sub.3 when R.sub.1 and R.sub.2 taken together form a 5 or 6 chain ring,R.sub.4 represents --OR.sub.5 or ##STR2## R.sub.
    Type: Grant
    Filed: October 4, 1996
    Date of Patent: November 11, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventors: Braham Shroot, Jacques Eustache, Oliver Watts, Jean-Michel Bernardon, Philippe Nedoncelle
  • Patent number: 5654442
    Abstract: Long wavelength, narrow emission bandwidth fluorecein dyes are provided for detecting spacially overlapping target substances. The dyes comprise 4,7-dichlorofluoresceins, and particularly 2',4',5',7'-tetrachloro-4,7-dichloro-5- (and 6-) carboxyfluoresceins. Methods and kits for using the dyes in DNA analysis are provided.
    Type: Grant
    Filed: March 8, 1995
    Date of Patent: August 5, 1997
    Assignee: The Perkin-Elmer Corporation
    Inventors: Steven M. Menchen, Linda G. Lee, Charles R. Connell, N. Davis Hershey, Vergine Chakerian, Sam L. Woo, Steven Fung
  • Patent number: 5633357
    Abstract: A method of producing a carboxylic acid glucuronide by reacting a carboxylic acid precursor with a blocked sugar epoxide precursor is disclosed. Also disclosed are: deuterated 11-nor-.DELTA..sup.8 - or .DELTA..sup.9 -THC carboxylic acid glucuronide having a deuterated hydrocarbon chain; 5'-deuterated 11-nor-.DELTA..sup.8 - or .DELTA..sup.9 -THC-carboxylic acid or 5'-deuterated .DELTA..sup.8 - or .DELTA..sup.9 -THC glucuronide. The compositions are useful as GC-MS standards; in methods for preparing antibodies reactive with a THC glucuronide; and, in GC-MS diagnostic methods for THC metabolites.
    Type: Grant
    Filed: March 4, 1994
    Date of Patent: May 27, 1997
    Assignee: Synthetic Technology Corporation
    Inventors: Marcus A. Tius, Mark R. Hagadone
  • Patent number: 5614550
    Abstract: Compounds of formula (I) are provided: ##STR1## wherein: R.sup.1 represents an alkyl group; or a group of formula (II), (III), (IV) or (V): ##STR2## and wherein the groups R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen or various organic groups; and pharmaceutically acceptable salts thereof; as well as methods for the preparation of such compounds and their use in the treatment and prophylaxis of hypercholesteremia and arteriosclerosis.
    Type: Grant
    Filed: February 27, 1996
    Date of Patent: March 25, 1997
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Koza Oda, Sadao Ishihara, Fujio Saito, Hiroyuki Koike, Teiichiro Koga, Eiichi Kitazawa, Hiroshi Kogen, Ichiro Hayakawa
  • Patent number: 5567829
    Abstract: Organic values are salvaged from scrap polycarbonate by heating in the presence of an acid catalyst and a C.sub.1-4 alkyl phenol such as m- or p-cresol. Among the compounds which can be salvaged are polyalkylated xanthenes, phenol and diaryl carbonate.
    Type: Grant
    Filed: April 17, 1995
    Date of Patent: October 22, 1996
    Assignee: General Electric Company
    Inventors: Andrew J. Caruso, Julia L. Lee
  • Patent number: 5563169
    Abstract: ConstitutionTricyclic heterocyclyl compounds having a general formula (I): ##STR1## wherein: R.sup.1 and R.sup.2 each represents H, a lower alkyl or lower alkoxy group, a halogen atom or halogeno-lower alkyl; R.sup.3 represents H or a lower alkyl group; R.sup.4 represents a substituted phenyl or naphthyl group; R.sub.5 represents H or a lower alkyl group; A represents a lower alkylene group; B represents an --O-- or --S-- group; and n is 0-1.EffectThe compounds have an excellent activity in the inhibition of acyl-CoA: cholesterol acyltransferase (ACAT) and are useful for the treatment and prophylaxis of atherosclerosis.
    Type: Grant
    Filed: July 6, 1994
    Date of Patent: October 8, 1996
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Teiichiro Koga, Kazuo Hasegawa
  • Patent number: 5554770
    Abstract: Polyalkylated xanthenes are prepared by effecting reaction between an alkylated phenol such as m-cresol and an oxygenated organic material such as acetone in the presence of an acid catalyst such as methanesulfonic acid.
    Type: Grant
    Filed: April 17, 1995
    Date of Patent: September 10, 1996
    Assignee: General Electric Company
    Inventors: Andrew J. Caruso, Julia L. Lee, Joseph A. King, Jr.