The Tricyclo Ring System Consists Of Three Six-membered Cyclos (e.g., Xanthene, Etc.) Patents (Class 549/388)
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Patent number: 7094910Abstract: An infrared dye, characterised in that the dye comprises two bridged diarylpolymethine type dyes or derivatives thereof connected together at either the 3, 4, 5 or 6 position by a central moiety such that the two dyes are located on each side of the central moiety, wherein the infrared dye absorbs strongly in the near infrared region of the spectrum but poorly in the visible region of the spectrum.Type: GrantFiled: August 10, 2001Date of Patent: August 22, 2006Assignee: Silverbrook Research Pty LtdInventors: Lachlan Everett Hall, Kia Silverbrook
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Patent number: 7087765Abstract: 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: GrantFiled: March 9, 2004Date of Patent: August 8, 2006Assignee: NPS Pharmaceuticals, Inc.Inventors: Alan L. Mueller, Scott T. Moe
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Patent number: 6939977Abstract: Disclosed are novel compounds represented by the following structural formula: R-X-Y; and physiologically acceptable salts thereof. R is a tricyclic core of a cannabinoid or substituted cannabinoid. X is a covalent bond, —CH2— or —CHR1—, wherein R1 a C1 to C3 substituted or unsubstituted alkyl group. Y is a heterocyclic ring, a substituted heterocyclic ring, a carbocyclic ring, a substituted carbocyclic ring, a fused bicyclic ring system, a substituted fused bicyclic ring system, a bridged bicyclic ring system, a substituted bridged bicyclic ring system, a bridged tricyclic ring system or a substituted bridged tricyclic ring system. Also disclosed is a method of stimulating a CB1 and/or CB2 receptor in a subject. The method comprises administering to the subject a therapeutically effective amount of R-X-Y.Type: GrantFiled: December 4, 2002Date of Patent: September 6, 2005Assignee: The University of ConnecticutInventors: Alexandros Makriyannis, Dai Lu, Atmaram Khanolkar
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Patent number: 6887533Abstract: 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: GrantFiled: March 24, 2004Date of Patent: May 3, 2005Assignee: Clariant International, Ltd.Inventors: Wolfgang Schmidt, Barbara Hornung, Rainer Wingen
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Publication number: 20040245498Abstract: Compounds of the formula (I) 1Type: ApplicationFiled: March 24, 2004Publication date: December 9, 2004Inventors: Wolfgang Schmidt, Barbara Hornung, Rainer Wingen
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Patent number: 6750244Abstract: 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: GrantFiled: April 2, 2001Date of Patent: June 15, 2004Assignee: NPS Pharmaceuticals, Inc.Inventors: Alan L. Mueller, Scott T. Moe
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Patent number: 6730519Abstract: 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: GrantFiled: December 4, 2001Date of Patent: May 4, 2004Assignee: The University of MississippiInventors: Mahmoud A. Elsohly, Samir A. Ross
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Patent number: 6696569Abstract: 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: GrantFiled: April 11, 2001Date of Patent: February 24, 2004Assignee: Lumigen, Inc.Inventors: Hashem Akhavan-Tafti, Zahra Arghavani, Renuka DeSilva
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Patent number: 6620842Abstract: 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: GrantFiled: February 15, 2002Date of Patent: September 16, 2003Assignee: Indena SpAInventors: Ezio Bombardelli, Piero Valenti
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Publication number: 20030158127Abstract: 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: ApplicationFiled: July 3, 2001Publication date: August 21, 2003Applicant: MALLINCKRODT INC.Inventors: Raghavan Rajagopalan, Gary L. Cantrell, Samuel I. Achilefu, Joseph E. Bugaj, Richard B. Dorshow
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Patent number: 6608089Abstract: 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: GrantFiled: February 15, 2002Date of Patent: August 19, 2003Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Piero Valenti
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Patent number: 6472414Abstract: 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: GrantFiled: May 18, 1999Date of Patent: October 29, 2002Assignee: Bristol-Myers Squibb CompanyInventors: 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
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Patent number: 6465625Abstract: Highly specific biocatalytic reactions have been used to create a population of taxol derivatives.Type: GrantFiled: June 19, 2000Date of Patent: October 15, 2002Assignee: Albany Molecular Research, Inc.Inventors: Jonathan S. Dordick, Douglas S. Clark, Peter C. Michels, Yuri L. Khmelnitsky
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Publication number: 20020137225Abstract: A compound represented by the following formula (I): 1Type: ApplicationFiled: May 8, 2002Publication date: September 26, 2002Applicant: Daiichi Pure Chemicals Co., Ltd.Inventors: Tetsuo Nagano, Hirotatsu Kojima
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Publication number: 20020091150Abstract: The present invention is a compound of formula 1Type: ApplicationFiled: December 10, 2001Publication date: July 11, 2002Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jurgen Wichmann, Thomas Johannes Woltering
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Patent number: 6403812Abstract: 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: GrantFiled: May 30, 2000Date of Patent: June 11, 2002Assignee: The Perkin-Elmer CorporationInventors: Steven M. Menchen, Linda G. Lee, Charles R. Connell, N. Davis Hershey, Vergine Chakerian, Sam L. Woo, Steven Fung
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Patent number: 6372907Abstract: 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: GrantFiled: September 14, 2000Date of Patent: April 16, 2002Assignee: Apptera CorporationInventors: Linda G. Lee, Ronald J. Graham, William E. Werner, Elana Swartzman, Lily Lu
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Publication number: 20020039795Abstract: 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: ApplicationFiled: October 26, 1998Publication date: April 4, 2002Applicant: Elsohly Et AlInventors: MAHMOUD A. ELSOHLY, SAMIR A. ROSS
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Patent number: 6365416Abstract: A method of preparing THC using extraction of plant material with a non-polar solvent followed by vacuum distillation and chromatography.Type: GrantFiled: October 26, 1998Date of Patent: April 2, 2002Assignee: The University of MississippiInventors: Mahmoud A. Elsohly, Samir A. Ross
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Patent number: 6355650Abstract: 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: GrantFiled: July 21, 2000Date of Patent: March 12, 2002Assignee: Atlantic Technology Ventures, Inc.Inventor: Sumner H. Burstein
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Patent number: 6340691Abstract: 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: GrantFiled: January 27, 2000Date of Patent: January 22, 2002Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, Derek C. Cole, James M. Chen, Jamie M. Davis, George T. Grosu
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Patent number: 6329377Abstract: 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: GrantFiled: January 18, 2000Date of Patent: December 11, 2001Assignee: Cephalon, Inc.Inventor: Sankar Chatterjee
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Publication number: 20010041802Abstract: 1Type: ApplicationFiled: February 28, 2001Publication date: November 15, 2001Inventors: 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
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Patent number: 6288234Abstract: 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: GrantFiled: June 4, 1999Date of Patent: September 11, 2001Assignee: Advanced Medicine, Inc.Inventor: John H. Griffin
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Publication number: 20010012901Abstract: The present invention relates to a linker shown by the following formula (I):Type: ApplicationFiled: March 21, 2001Publication date: August 9, 2001Applicant: Fujisawa Pharmaceutical Co. Ltd.Inventors: Akito Tanaka, Hideo Tsutsumi
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Patent number: 6245807Abstract: 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: GrantFiled: February 24, 1998Date of Patent: June 12, 2001Assignee: Dana-Farber Cancer InstituteInventors: Arthur Pardee, Chiang J. Li
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Patent number: 6211201Abstract: 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: GrantFiled: June 29, 1999Date of Patent: April 3, 2001Assignee: ICN Pharmaceuticals, Inc.Inventors: Colin Granger, Robert Orr, Kandasamy Ramasamy
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Patent number: 6191278Abstract: 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: GrantFiled: November 3, 1999Date of Patent: February 20, 2001Assignee: PE CorporationInventors: Linda G. Lee, Ronald J. Graham, William E. Werner, Elana Swartzman, Lily Lu
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Patent number: 6172058Abstract: 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: GrantFiled: April 3, 1998Date of Patent: January 9, 2001Assignee: Lilly, SAInventors: Concepci{acute over (o)}n Pedregal Tercero, Ivan Collado Cano, Angel Maz{acute over (o)}n Ruiz
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Patent number: 6166226Abstract: 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: GrantFiled: December 8, 1998Date of Patent: December 26, 2000Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, John P. Wolfe, Michael Palucki
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Patent number: 6136961Abstract: 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: GrantFiled: June 29, 1998Date of Patent: October 24, 2000Assignee: EnzyMed, Inc.Inventors: Jonathan S. Dordick, Douglas S. Clark, Peter C. Michels, Yuri L. Khmelnitsky
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Patent number: 6127415Abstract: 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: GrantFiled: April 14, 1999Date of Patent: October 3, 2000Assignee: Galderma Research & Development, S.N.C.Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
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Patent number: 6124484Abstract: 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: GrantFiled: July 17, 1998Date of Patent: September 26, 2000Assignee: Isis Pharmaceuticals, Inc.Inventors: Yogesh S. Sanghvi, Zhiqiang Guo
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Patent number: 6054448Abstract: 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: GrantFiled: October 17, 1997Date of Patent: April 25, 2000Assignee: Eli Lilly and Company LimitedInventors: Barry Peter Clark, John Richard Harris
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Patent number: 5977077Abstract: 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: GrantFiled: March 20, 1996Date of Patent: November 2, 1999Assignee: Interlab CorporationInventors: Rolf Walter Winter, Michael Kevin Riscoe, David J. Hinrichs
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Patent number: 5965605Abstract: 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: GrantFiled: December 29, 1997Date of Patent: October 12, 1999Assignee: Heska CorporationInventors: Y.-S. Edmond Cheng, Yuan Liu, John Chu, Jean-Pierre Kinet, Marie-Helene Jouvin, Yukio Sudo, Xiuqi Qian
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Patent number: 5932726Abstract: 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: GrantFiled: April 11, 1997Date of Patent: August 3, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Michael Ernest Pierce, Anusuya Choudhury, Rodney Lawrence Parsons, Jr., Lilian Alicia Radesca
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Patent number: 5919846Abstract: 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: GrantFiled: February 19, 1998Date of Patent: July 6, 1999Assignee: Milliken Research CorporationInventors: Raj Batlaw, John W. Miley
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Patent number: 5877030Abstract: 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: GrantFiled: May 31, 1995Date of Patent: March 2, 1999Inventors: Julius Rebek, Jr., Thomas Carell, Edward A. Wintner
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Patent number: 5847166Abstract: 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: GrantFiled: October 10, 1996Date of Patent: December 8, 1998Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, John P. Wolfe, Michael Palucki
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Patent number: 5827877Abstract: 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: GrantFiled: May 7, 1996Date of Patent: October 27, 1998Assignee: Cephalon, Inc.Inventor: Sankar Chatterjee
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Patent number: 5811389Abstract: 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: GrantFiled: June 24, 1996Date of Patent: September 22, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Wilhelm Bannwarth, Fernand Gerber, Alfred Grieder, Andreas Knierzinger, Klaus Muller, Daniel Obrecht, Arnold Trzeciak
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Patent number: 5770382Abstract: 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: GrantFiled: June 7, 1995Date of Patent: June 23, 1998Assignee: Ligand Pharmaceuticals, Inc.Inventors: Chan Kou Hwang, Steven K. White, Beth Ann Badea, Alex M. Nadzan
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Patent number: 5770378Abstract: 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: GrantFiled: June 7, 1995Date of Patent: June 23, 1998Assignee: 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
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Patent number: 5770383Abstract: 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: GrantFiled: June 7, 1995Date of Patent: June 23, 1998Assignee: 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
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Patent number: 5760246Abstract: 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: GrantFiled: December 17, 1996Date of Patent: June 2, 1998Inventors: 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
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Patent number: 5686586Abstract: 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: GrantFiled: October 4, 1996Date of Patent: November 11, 1997Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Braham Shroot, Jacques Eustache, Oliver Watts, Jean-Michel Bernardon, Philippe Nedoncelle
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Patent number: 5654442Abstract: 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: GrantFiled: March 8, 1995Date of Patent: August 5, 1997Assignee: The Perkin-Elmer CorporationInventors: Steven M. Menchen, Linda G. Lee, Charles R. Connell, N. Davis Hershey, Vergine Chakerian, Sam L. Woo, Steven Fung
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Patent number: 5633357Abstract: 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: GrantFiled: March 4, 1994Date of Patent: May 27, 1997Assignee: Synthetic Technology CorporationInventors: Marcus A. Tius, Mark R. Hagadone
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Patent number: 5614550Abstract: 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: GrantFiled: February 27, 1996Date of Patent: March 25, 1997Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Koza Oda, Sadao Ishihara, Fujio Saito, Hiroyuki Koike, Teiichiro Koga, Eiichi Kitazawa, Hiroshi Kogen, Ichiro Hayakawa