Two Of The Cyclos Share At Least Three Ring Member (i.e., Bridged) Patents (Class 546/63)
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Publication number: 20090076059Abstract: The present application describes deuterium-enriched dianicline, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20080300405Abstract: The present invention relates to naphthalenetetracarboxylic acid derivates, to a process for their preparation and to their use, especially as an n-type semiconductor.Type: ApplicationFiled: December 22, 2006Publication date: December 4, 2008Applicant: BASF SEInventor: Martin Konemann
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Patent number: 7456177Abstract: The present invention provides a compound having the structure of formula I: wherein R1 is hydrogen, (C1–C6) alkyl, unconjugated (C3–C6) alkenyl, benzyl, YC(?O)(C1–C6) alkyl or —CH2CH2—O—(C1–C4) alkyl; X is CH2 or CH2CH2; Y is (C2–C6) alkylene; Z is (CH2)m, CF2, or C(?O), where m is 0, 1 or 2; R2 and R3 are selected independently from hydrogen, halogen, —(C1–C6) alkyl optionally substituted with from 1 to 7 halogen atoms, and —O(C1–C6) alkyl optionally substituted with from 1 to 7 halogen atoms, or R2 and R3 each together with the atom to which it is connected independently form C(?O), S?O, S(?O)2, or N?O; and is a 5- to 7-membered monocyclic heteroaryl group selected from pyridinyl, pyridone, pyridazinyl, imidazolyl, pyrimidinyl, pyrazolyl, triazolyl, pyrazinyl, furyl, thienyl, isoxazolyl, thiazolyl, oxazolyl, isothiazolyl, pyrrolyl, cinnolinyl, triazinyl, oxadiazolyl, thiadiazolyl and furazanyl groups.Type: GrantFiled: July 12, 2004Date of Patent: November 25, 2008Assignee: Pfizer Inc.Inventors: Martin P. Allen, Jotham W. Coe, Spiros Liras, Christopher J. O'Donnell, Brian T. O'Neill
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Publication number: 20080177073Abstract: 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: ApplicationFiled: January 7, 2008Publication date: July 24, 2008Inventors: Antonio Facchetti, Tobin J. Marks, He Yan
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Patent number: 7326728Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) its stereoisomers thereof, or a solvate thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Z is CONR1R2 or CH2NR1R2 and where R, R?, Ra, Rb, Rc, Rd, Z, A and B are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.Type: GrantFiled: January 13, 2005Date of Patent: February 5, 2008Assignee: Bristol-Myers Squibb CompanyInventor: Bingwei Vera Yang
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Patent number: 7205300Abstract: This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.Type: GrantFiled: January 3, 2003Date of Patent: April 17, 2007Assignee: Pfizer IncInventors: Jotham Wadsworth Coe, Paige Roanne Palmer Brooks
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Patent number: 7144882Abstract: This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.Type: GrantFiled: January 3, 2003Date of Patent: December 5, 2006Assignee: Pfizer IncInventors: Jotham Wadsworth Coe, Paige Roanne Palmer Brooks
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Patent number: 6908927Abstract: The invention relates to pyridopyranoazepine derivatives, to pharmaceutical compositions containing them, to process for preparing them, and to the method of use thereof in the treatment or prevention of disorders associated with a dysfunction of the nicotine receptors.Type: GrantFiled: February 6, 2003Date of Patent: June 21, 2005Assignee: Sanofi-SynthelaboInventors: Frédéric Galli, Samir Jegham, Alistair Lochead, Axelle Samson
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Patent number: 6887998Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.Type: GrantFiled: April 9, 2003Date of Patent: May 3, 2005Assignee: Rensselaer Polytechnic InstituteInventor: Mark P. Wentland
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Patent number: 6849619Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: February 20, 2004Date of Patent: February 1, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Albert J. Robichaud, John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
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Patent number: 6800625Abstract: The invention relates to novel 2,4-dihydro-pyrrolo[3,4-b]quinolin-9-one derivatives of the formula (I) and (IV): wherein all variables are as herein defined, pharmaceutical compositions containing the compounds and their use for the treatment of sexual dysfunction.Type: GrantFiled: June 17, 2003Date of Patent: October 5, 2004Assignee: Janssen Pharmaceutica N.V.Inventors: Weiqin Jiang, Zhihua Sui
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Patent number: 6784186Abstract: This invention relates to novel structural analogues and derivatives of compounds with general analgesic or related pharmacological activity. In particular the invention relates to derivatives of opioid compounds, particularly morphine and related compounds, in which an opioid compound is linked via the nitrogen at position 17 to a spacer group, which in turn is linked to a charged group, or a pharmaceutically acceptable salt thereof. In particularly preferred embodiments the opioid compound is morphine, codeine, or buprenorphine.Type: GrantFiled: November 20, 2000Date of Patent: August 31, 2004Inventors: Roy W. Jackson, Kamani R. Subasinghe, Alan L. A. Boura
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Patent number: 6759065Abstract: A compound is extracted from vegetable material, wherein the vegetable material is reduced and treated with a solvent. According to the invention, the vegetable material is frozen using a liquid nitrogen and in frozen condition reduced in size. According to two important embodiments, the vegetable material comes from the ginkgo tree, in particular fresh leaves, and water is used as a solvent. The invention also relates to a pharmaceutical preparation and a cosmetic preparation comprising as active component a compound obtained by the method according to the invention.Type: GrantFiled: February 15, 2001Date of Patent: July 6, 2004Assignee: XenoBiosisInventor: Henri M. Ruijten
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Patent number: 6747039Abstract: The present invention relates to a group of aza-anthrapyrazole compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-anthrapyrazole compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.Type: GrantFiled: March 12, 2002Date of Patent: June 8, 2004Assignee: Albany Molecular Research, Inc.Inventor: Simon N. Haydar
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Patent number: 6699852Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: December 19, 2001Date of Patent: March 2, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert Robichaud, John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
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Patent number: 6639074Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.Type: GrantFiled: March 18, 2002Date of Patent: October 28, 2003Assignee: Bristol Myers Squibb CompanyInventors: Bang-Chi Chen, Kyoung S. Kim, S. David Kimball, Raj N. Misra, Mark E. Salvati, Joseph E. Sundeen, Hai-Yun Xiao, Rulin Zhao
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Patent number: 6605610Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.Type: GrantFiled: February 25, 2000Date of Patent: August 12, 2003Assignee: Pfizer IncInventors: Jotham Wadsworth Coe, Paige Roanne Palmer Brooks
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Patent number: 6566086Abstract: Methods for the detection of creatine compound levels in body fluid samples are discussed. Portable kits capable of determining creatine levels using non-invasive and visually detectable methods are also included.Type: GrantFiled: January 28, 2000Date of Patent: May 20, 2003Assignee: FAL DiagnosticsInventors: Fahad Mohammed Saleh Al Athel, Thomas W. Bell, Alisher B. Khasanov, Rima Kaddurah-Daouk
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Patent number: 6548493Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: June 15, 2000Date of Patent: April 15, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Wenting Chen, Christopher D. McClung, Emilie J. B. Calvello, David M. Zawrotny
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Patent number: 6541484Abstract: A class of substituted and/or ring-fused pyrazolo[3,4-b]pyridine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent on the pyrazole nitrogen atom adjacent the pyridine nucleus, and an optionally substituted cycloalkyl-alkoxy, aryl-alkoxy or heteroaryl-alkoxy substituent on the carbon atom adjacent the pyridine ring nitrogen atom, are selective ligands for GABAA receptors, in particular having high affinity for the &bgr;2 and/or &bgr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse neurological disorders, including anxiety and convulsions.Type: GrantFiled: June 14, 2002Date of Patent: April 1, 2003Assignee: Merck Sharp & Dohme LimitedInventors: Ian James Collins, Linda Elizabeth Keown, Leslie Joseph Street
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Patent number: 6538003Abstract: The invention relates to pyridopyranoazepine derivatives, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment or prevention of disorders associated with a dysfunction of the nicotine receptors.Type: GrantFiled: August 17, 2001Date of Patent: March 25, 2003Assignee: Sanofi-SynthelaboInventors: Frédéric Galli, Samir Jegham, Alistair Lochead, Axelle Samson
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Publication number: 20020128343Abstract: Disclosed are thermally-stable, colored, photopolymerizable compounds containing a vinyl group which are capable of being copolymerized with reactive vinyl monomers to produce colored compositions such as polyacrylates, polymethacrylates, polystyrene, etc. The compounds exhibit good thermal stability, fastness (stability) to UV-light, good solubility in the reactive monomers and good color strength.Type: ApplicationFiled: August 1, 2001Publication date: September 12, 2002Inventors: Michael John Cyr, Max Allen Weaver, Gerry Foust Rhodes, Jason Clay Pearson, Phillip Michael Cook, Jos Simon De Wit, Larry Keith Johnson
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Publication number: 20020119961Abstract: A compound of the formula 1Type: ApplicationFiled: October 5, 2001Publication date: August 29, 2002Applicant: Pfizer Inc.Inventors: Laura C. Blumberg, Matthew F. Brown, Ronald P. Gladue, Christopher S. Poss
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Publication number: 20020082424Abstract: The dihydroindole C-ring found in CC-1065/duocarmycin analogs is formed by the 5-exo-trig radical cyclization of an aryl halide onto a tethered vinyl chloride forming with chlorine installed as a suitable leaving group for subsequent cyclopropane spirocyclization. The versatility of this approach is disclosed in the context of six CC-1065/duocarmycin analogs previously synthesized in this laboratory.Type: ApplicationFiled: October 30, 2001Publication date: June 27, 2002Applicant: The Scripps Research InstituteInventor: Dale L. Boger
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Patent number: 6380193Abstract: A compound of formula I: or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof.Type: GrantFiled: September 1, 1998Date of Patent: April 30, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang
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Publication number: 20010049377Abstract: Compounds having Formula I 1Type: ApplicationFiled: February 13, 1998Publication date: December 6, 2001Inventors: MICHAEL J. COGHLAN, JAMES P. EDWARDS, TODD K. JONES, MICHAEL E. KORT
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Patent number: 5965569Abstract: New polycyclic aminopyridine compounds which are acetylcholinesterase inhibitors, process for preparing them and their use. The polycyclic aminopyridine compounds correspond to the formula ##STR1## in which the various radicals have the meanings stated in the specification. The process for preparing these compounds is characterized in that ketones of general formula (II) are reacted with aminonitriles of general formula (III) and, if necessary, the compounds of formula (I) are alkylated, aralkylated or acylated, or alternatively the corresponding keto precursor is reduced. The compounds of the general formula (I) are especially suitable for the preparation of medicaments against memory disorders such as senile dementia or Alzheimer's disease.Type: GrantFiled: August 12, 1997Date of Patent: October 12, 1999Assignee: Medichem, S.A.Inventors: Pelayo Camps Garcia, Diego Munoz-Torrero Lopez-Ibarra, Diana Marina Gorbig Romeu, Joan Contreras Lascorz, Monserrat Simon Fornell, Jordi Morral Cardoner, Rachid El Achab, Albert Badia Sancho, Josep Eladi Banos Diez, Nuria Maria Vivas
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Patent number: 5856273Abstract: A compound of formula (I): ##STR1## where E is oxygen or sulphur; A is CR.sup.3 or N where R.sup.3 is hydrogen or hydrocarbyl; D completes a 5 or 6-membered non-aromatic heterocyclic ring which optionally contains additional heteroatoms selected from oxygen, nitrogen or sulphur and which is optionally substituted by an optionally substituted lower hydrocarbyl group, or an optionally substituted heteroaryl group; R.sup.1 and R.sup.2 are each independently hydrogen; optionally substituted lower hydrocarbyl, or optionally substituted heteroaryl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached, form a heterocyclic ring; Z represents halogen optionally substituted lower hydrocarbyl, optionally substituted lower hydocarbyloxy, optionally substituted lower hydrocarbylthio, hydrocarbylsulphinyl or hydrocarbylsulphonyl, cyano, nitro, CHO, NHOH, ONR.sup.7' R.sup.7", SF.sub.5 ; CO (optionally substituted lower hydrocarbyl), acylamino, COOR.sup.7, SO.sub.2 NR.sup.8 R.sup.9, CONR.sup.Type: GrantFiled: October 6, 1995Date of Patent: January 5, 1999Assignee: Zeneca LimitedInventors: Ian Trevor Kay, John Edward Duncan Barton, David John Collins, Bogdan Kowalczyk, Glynn Mitchell, John Martin Shribbs, John Micheal Cox, Nigel John Barnes, Stephen Christopher Smith
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Patent number: 5843952Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.Type: GrantFiled: July 8, 1997Date of Patent: December 1, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Fuk-Wah Sum
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Patent number: 5821248Abstract: Quinuclidine derivatives of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein m, P, Z, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined below. The compounds are substance P antagonists and, therefore, are useful in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, pain and migraine.Type: GrantFiled: March 21, 1997Date of Patent: October 13, 1998Assignee: Pfizer Inc.Inventor: John Adams Lowe, III
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Patent number: 5811551Abstract: We have found that indoles of structural formula (III): ##STR1## can be cost-effectively synthesized in high yield by the palladium-catalyzed coupling/ring closure of a 2-halo- or 2-trifluoromethylsulfonyl-aniline and a cyclic ketone derivative. The process of the present invention is particularly useful to form indoles containing acid-labile substituents such as triazole, acetyl, ketal, cyano, and carbamate, or indoles having a good leaving group in the benzyl position. The advantages of the present process are that it does not require the use of triphenyl phosphine or tetrabutyl ammonium chloride or lithium chloride.Type: GrantFiled: August 7, 1997Date of Patent: September 22, 1998Assignee: Merck & Co., Inc.Inventors: Cheng-Yi Chen, Robert D. Larsen
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Patent number: 5741788Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: November 17, 1995Date of Patent: April 21, 1998Assignee: Novo Nordisk A/SInventors: Preben H. Olesen, Per Sauerberg
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Patent number: 5604246Abstract: This invention is directed to 2-aminoalkyl-5-aminoalkylamino substituted isoquino[8,7,6-cd]indazole-6-(2H)-ones and to 2-aminoalkyl-5-aminoalkylamino substituted-isoquino[5,6,7-cd]indazole-6(2H)-ones. These compounds have been shown to have antitumor activity.Type: GrantFiled: December 7, 1994Date of Patent: February 18, 1997Assignees: Boehringer Mannheim Italia SpA, Univ. of VermontInventors: A. Paul Krapcho, Ernesto Menta, Ambrogio Oliva, Silvano Spinelli
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Patent number: 5569655Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: July 29, 1994Date of Patent: October 29, 1996Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5554620Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment of neurodegenerative disorders or neurotoxic injuries utilizing them, wherein the substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts have the formula: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and p are as defined in the specification.Type: GrantFiled: July 29, 1994Date of Patent: September 10, 1996Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5514685Abstract: The invention concerns the compounds of formulae ##STR1## wherein the substituents have various significances. They can be prepared by various methods, e.g. acylation, reduction, alkylation, etc. They are indicated for use as pharmaceuticals, in particular as immunosuppressant, antiproliferative and antiinflammatory agents.Type: GrantFiled: May 15, 1995Date of Patent: May 7, 1996Assignee: Sandoz Ltd.Inventor: Karl Baumann
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Patent number: 5252612Abstract: Described is a new immunosuppressant, L-683,756, a bisdemethylated, ring rearranged derivative of L-683,590, produced under fermentation conditions utilizing the microorganism, Actinoplanacete sp. (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.Type: GrantFiled: June 24, 1992Date of Patent: October 12, 1993Assignee: Merck & Co., Inc.Inventors: Byron H. Arison, Edward S. Inamine, Shieh-Shung T. Chen, Linda S. Wicker
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Patent number: 5250537Abstract: 5,6,7,8,9,10-Hexahydro-7,10-iminocyclohept[b]indole, 6,7,8,9,10,11-hexahydro-7,11-imino-5H-cyclooct[b]indole and substituted derivatives are effective in the treatment of psychoses with limited liability to produce concomitant adverse extrapyramidal symptoms. These compounds are also useful for treating other central nervous system and cardiovascular disorders.Type: GrantFiled: March 13, 1992Date of Patent: October 5, 1993Assignee: Scios Nova Inc.Inventors: Richard E. Mewshaw, Carl Kaiser, Mary E. Abreu
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Patent number: 5227487Abstract: Novel fluorescent dyes based on the rhodol structure are provided. The new reagents contain functional groups capable of forming a stable fluorescent product with functional groups typically found in biomolecules or polymers including amines, phenols, thiols, acids, aldehydes and ketones. Reactive groups in the rhodol dyes include activated esters, isothiocyanates, amines, hydrazines, halides, acids, azides, maleimides, aldehydes, alcohols, acrylamides and haloacetamides. The products are detected by their absorbance or fluorescence properties. The spectral properties of the fluorescent dyes are sufficiently similar in wavelengths and intensity to fluorescein or rhodamine derivatives as to permit use of the same equipment. The dyes, however, show less spectral sensitivity to pH in the physiological range than does fluorescein, have higher solubility in non-polar solvents and have improved photostability and quantum yields.Type: GrantFiled: April 16, 1990Date of Patent: July 13, 1993Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, James E. Whitaker
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Patent number: 5225554Abstract: A process for synthesizing polyoxa tetracyclics which involves the ozonolysis of a single-ring-structure vinyl silane with resulting direct formation of the desired multiple ring material. The polyoxa tetracyclic compounds have the formula ##STR1## The vinyl silanes have the structure ##STR2## The vinyl silanes are new chemical compounds as are corresponding primary ozonide and dioxetane intermediates. In a preferred embodiment, this invention provides a total synthesis of the antimalarial artemisinin.Type: GrantFiled: July 18, 1990Date of Patent: July 6, 1993Assignee: SRI InternationalInventors: Mitchell A. Avery, Clive Jennings-White
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Patent number: 5177082Abstract: The invention relates to compounds of the formulas ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen or lower alkyl, and the dotted ( . . . ) line is an optional double bond, and their pharmaceutically acceptable acid addition salts. The compounds of formulas I, II and III possess marked anticholinesterase activity and are useful as analeptic agents and as agents for the treatment of senile dementia and myasthenia gravis.Type: GrantFiled: October 18, 1990Date of Patent: January 5, 1993Inventors: Chao-mei Yu, Xi-can Tang, Jia-sen Liu, Yan-yi Han
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Patent number: 5145965Abstract: Novel 2,6-methanopyrrolo-3-benzazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: March 11, 1991Date of Patent: September 8, 1992Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Allen, David G. Wettlaufer
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Patent number: 5112830Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl, or oxygen-bridged diaryllowerallyl; A is a direct bond or (CHR.sub.3).sub.m, m being 1-3; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl; Y is O, S or NR.sub.7 ; and each R.sub.2, each R.sub.3 and R.sub.Type: GrantFiled: January 10, 1991Date of Patent: May 12, 1992Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Richard C. Effland
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Patent number: 5098909Abstract: A method of treatment of cough and/or bronchoconstriction in mammals, including humans, which method comprises the administration to the mammal in need of such treatment, an effective amount of a 5-HT.sub.3 receptor antagonist.Type: GrantFiled: July 10, 1989Date of Patent: March 24, 1992Assignee: Beecham Group, p.l.c.Inventor: Andrew J. Williams
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Patent number: 5037985Abstract: Novel 2,6-methanopyrrolo-3-benzazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: February 22, 1990Date of Patent: August 6, 1991Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Allen, David G. Wettlaufer
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Patent number: 5013627Abstract: Positively charged electrophotographic toners contain, besides customary resin and pigment particles, an additive which increases the cationic charge and has the general formula(X.sup.1).sup.- K.spsp.+.sup.1 -Y.sup.1 -A-Y.sup.2 -K.spsp.+.sup.2 (X.sub.2).sup.- (I)wherein the symbols have the meaning mentioned in the description.Type: GrantFiled: August 7, 1989Date of Patent: May 7, 1991Assignee: Bayer AktiengesellschaftInventors: Horst Harnisch, Roderich Raue
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Patent number: 4985430Abstract: There are disclosed a 9-acylamino-tetrahydroacridine derivative represented by the following formula (I): ##STR1## wherein R ##STR2## are as defined in the specification, its optical antipode or pharmaceutically acceptable acid addition salt thereof and a memory enhancing agent containing the same as an active ingredient.Type: GrantFiled: December 2, 1988Date of Patent: January 15, 1991Assignee: Mitsubishi Kasei CorporationInventors: Shuji Morita, Ken-Ichi Saito, Kunihiro Ninomiya, Akihiro Tobe, Issei Nitta, Mamoru Sugano
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Patent number: 4973593Abstract: Compounds of the formulae: ##STR1## are useful as anti-hypertensives.Type: GrantFiled: August 4, 1987Date of Patent: November 27, 1990Assignee: Research Corporation Technologies, Inc.Inventor: Abram N. Brubaker
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Patent number: 4963683Abstract: A process for synthesizing polyoxa tetracyclics which involves the ozonolysis of a single-ring-structure vinyl silane with resulting direct formation of the desired multiple ring matrial. The polyoxa tetracyclic compounds have the formula ##STR1## The vinyl silanes have the structure ##STR2## The vinyl silanes are new chemical compounds as are corresponding primary ozonide and dioxetane intermediates. In a preferred embodiment, this invention provides a total synthesis of the antimalarial artemisinin.Type: GrantFiled: February 15, 1989Date of Patent: October 16, 1990Assignee: SRI InternationalInventors: Mitchell A. Avery, Clive Jennings-White
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Patent number: 4929622Abstract: Novel 2,6-methanopyrrolo-3-benzazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: November 16, 1988Date of Patent: May 29, 1990Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard C. Allen, David G. Wettlaufer