- Synthesis of Conformationally Locked and C-Linked Analogues of Imidazole-Based Ketene Dithioacetal Fungicides
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First examples with the unknown tricyclic 4,8 b -dihydro-3 aH -indeno[1,2- d ][1,3]dithiole ring system have been prepared. Also, imidazoles linked in ring position 5 to a ketene dithioacetal and 1,3-dithiane derivatives with an exocyclic cyano- and imidazole-substituted C-C double bond are completely new. All these compounds are either conformationally locked, C-linked or six-ring analogues of the antifungal agent luliconazole. Synthesis and fungicidal activity of these sterol biosynthesis inhibitors are reported.
- Gagnepain, Julien,Jeanmart, Stephane,Bonvalot, Damien,Jacob, Olivier,Lamberth, Clemens
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supporting information
p. 59 - 62
(2019/01/04)
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- CARBAMATE DERIVATIVE COMPOUNDS, PROCESSES FOR PREPARING THEM AND THEIR USES
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The present invention relates to a pharmaceutical composition for treating or preventing CNS disorders containing a carbamate derivative compound and/or pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or prevention CNS disorders comprising administering a carbamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of CNS disorders.
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Paragraph 402-404; 426-428
(2017/09/15)
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- Synthesis of 9H-Indeno [1, 2-b] pyrazine and 11H-indeno [1, 2-b] quinoxaline derivatives in one-step reaction from 2-bromo-4-chloro-1-indanone
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The reaction of 2-bromo-4-chloro-1-indanone with 2, 3-diaminomaleonitrile, benzene-1, 2-diamine and 4-methylbenzene-1, 2-diamine in glacial acetic acid gave 8-chloro-9H-indeno[1, 2-b]pyrazine-2, 3-dicarbonitrile, 1-chloro-11H-indeno[1, 2-b]quinoxaline and
- Jasouri,Khalafy,Badali,Prager
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scheme or table
p. 105 - 107
(2012/07/14)
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- Selective bromination of 4-chloro-1-indanone and synthesis of (4-chloro-2, 3-dihydro-1H-indene-2-yl)methanamine
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The synthesis of 4-chloro-1-indanone in four steps from 2-chlorobenzaldehyde was investigated. Bromination of this compound under various conditions occurred in the cyclopentanone ring, producing mono- and dibromo derivatives. Cyanation of 2-bromo-4-chlor
- Jasouri,Khalafy,Badali,Piltan
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- THERAPEUTIC FLUOROETHYLCYANO GUANIDINES
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Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
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Page/Page column 13
(2008/12/04)
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- SUBSTITUTED FLUOROETHYL UREAS AS ALPHA 2 ADRENERGIC AGENTS
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Therapeutic compounds, and methods, compositions, and medicaments related thereto are disclosed herein.
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Page/Page column 18; 19
(2008/12/04)
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- Synthesis of 1-indanones via intramolecular cyclodehydration of 3-arylpropionic acids catalyzed by heteropoly acid as heterogeneous catalyst
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Intramolecular cyclodehydration of 3-arylpropionic acids catalyzed by heteropoly acids was investigated for the first time. Several 3-arylpropionic acids were refluxed and dehydrated in chlorobenzene in the presence of 0.2 equivalent of heteropoly acids, and 1-indanones were obtained in good yield. At the same time, intermolecular Friedel-Crafts acylation were observed in this experiment. Copyright Taylor & Francis Group, LLC.
- Lan, Kun,Shan, Zi-Xing
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p. 2171 - 2177
(2008/02/05)
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- Synthesis of 1-indanones by intramolecular Friedel-Crafts reaction of 3-arylpropionic acids catalyzed by Tb(OTf)3
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Intramolecular Friedel-Crafts acylation reaction of 3-arylpropionic acids was efficiently catalyzed by Tb(OTf)3 at 250°C to give 1-indanones. Even deactivated 3-arylpropionic acids with halogen atoms on the aromatic ring can be cyclized in moderation to good yields.
- Cui, Dong-Mei,Zhang, Chen,Kawamura, Masato,Shimada, Shigeru
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p. 1741 - 1745
(2007/10/03)
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- 4-SUBSTITUTED IMIDAZOLE-2-THIONES AND IMIDAZOL- 2-ONES AS AGONISTS OF THE ALPHA- 2B AND ALPHA-2C ADRENERGIC RECEPTORS
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Compounds of Formula (I): where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula (I) are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula (I) where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.
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Page 119, 120
(2008/06/13)
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- Indanylidenes. 1. Design and synthesis of (E)-2-(4,6-difluoro-1-indanylidene)acetamide, a potent, centrally acting muscle relaxant with antiinflammatory and analgesic activity
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The design of rigid cyclic analogues derived from cinnamamide 1, (E)-N-cyclopropyl-3-(3-fluorophenyl)prop-2-enamide, and β-methylcinnamamide 2, (E)-N-cyclopropyl-3-(3-fluorophenyl)but-2-enamide, has led to the discovery of the potent, centrally acting muscle relaxant (E)-2-(4,6-difluoro-1-indanylidene)acetamide, 17. Compound 17 also possesses potent antiinflammatory and analgesic activity. This paper describes the synthesis and the muscle relaxant, antiinflammatory, and analgesic structure-activity relationships of 17 and 67 of its analogues. Compound 17 has been taken into phase I clinical trials.
- Musso, David L.,Cochran, Felicia R.,Kelley, James L.,McLean, Ed W.,Selph, Jeffrey L.,Rigdon, Greg C.,Orr, G. Faye,Davis, Ronda G.,Cooper, Barrett R.,Styles, Virgil L.,Thompson, James B.,Hall, William R.
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p. 399 - 408
(2007/10/03)
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- Tricyclic pyrazoles. Part 1: synthesis and biological evaluation of novel 1,4-dihydroindeno[1,2-c]pyrazol-based ligands for CB1and CB2 cannabinoid receptors.
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Cannabinoids receptors, cellular elements of the endocannabinoid system, have been the focus of extensive studies because of their potential functional role in several important physiological and pathological processes. To further evaluate the properties of CB receptors, especially CB(1) and CB(2) subtypes, we have designed, using SR141716A as a benchmark, a new series of rigid 1-aryl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamides. Compounds 1 were synthesized from substituted 1-aryl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxylic acids and requisite amines. The various analogues were assayed for binding both to the brain and peripheral cannabinoid receptors (CB(1) and CB(2)). Seven of the new compounds displayed very high in vitro CB(2) binding affinities, especially 1a, 1b, 1c, 1e, 1g, 1h and 1j which showed K(i) values of 0.34, 0.225, 0.27, 0.23, 0.385, 0.037 and 0.9 nM, respectively. Compounds 1a, 1b, 1c and 1h showed the highest selectivity for CB(2) receptor with K(i)(CB(1)) to K(i)(CB(2)) ratios of 6029, 5635, 5814 and 9810, respectively. Noticeably, 1h exhibited the highest affinity and selectivity for CB(2) receptors.
- Mussinu, Jean Mario,Ruiu, Stefania,Mule, Antonio C,Pau, Amedeo,Carai, Mauro A M,Loriga, Giovanni,Murineddu, Gabriele,Pinna, Gerard A
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p. 251 - 263
(2007/10/03)
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- Transition metal compound, ligand system, catalyst system and its use for the polymerization of olefins
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Ligand systems containing indenyl structures, transition metal compounds of the metallocene type and catalyst systems comprising such transition metal compounds are described. The novel transition metal compounds can be used in the polymerization of olefi
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- Substituted dihydroisoquinolinones and related compounds as potentiators of the lethal effects of radiation and certain chemotherapeutic agents; selected compounds, analogs and process
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The invention is selected, novel, and known analogs of isoquinolinones of the formula and pharmaceutically acceptable salts thereof; novel pharmaceutical compositions; and a method for enhancing the lethal effects for tumor cells to treatment having DNA damaging activity such as ionizing radiation or with chemotherapeutic agents.
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- Rhodium Complex-Catalyzed Desilylative Cyclocarbonylation of 1-Aryl-2-(trimethylsilyl)acetylenes: A New Route to 2,3-Dihydro-1H-inden-1-ones
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Under water gas shift reaction conditions, 1-aryl-2-(trimethylsilyl)acetylenes undergo Rh-catalyzed desilylative cyclocarbonylation to give 2,3-dihydro-1H-inden-1-ones and trimethylsilanol.A wide variety of functional groups, such as methoxy, chloro, acetyl, ethoxycarbonyl, cyano, and trifluoromethyl, are tolerated on the aromatic ring under the reaction conditions.The products were obtained in good to excellent yield whether the substituent on the aromatic ring was electron-donating or electron-withdrawing.The cyclizations of substrates bearing a meta substituent onthe aromatic ring regiospecifically gave 5-substituted-2,3-dihydro-1H-inden-1-ones except when the meta substituent was a methoxy group.The desilylative cyclocarbonylation is an alternative to the conventional preparation of 2,3-dihydro-1H-inden-1-ones, an intramolecular Friedel-Crafts acylation.A possible mechanism for the process is described.
- Takeuchi, Ryo,Yasue, Hiroyuki
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p. 5386 - 5392
(2007/10/02)
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- Phenyl or bicyclo-alkenylfluoro amide pesticides
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Compound of the formula (I): or a salt thereof, wherein Q1 is a phenyl ring or a fused bicyclic ring system containing 9 or 10 ring carbon atoms at least one ring being aromatic, or Q1 is a dihalovinyl group; Q is an alkyl chain containing 1 to 12 carbon atoms and optionally containing one or two oxygen atoms and/or an unsaturated group --CR7 =CR8 --, or --C=C--, wherein R7 and R8 are selected from hydrogen or halo; a is 0 or 1; b is 0 or 1; the sum of a and b is 0 or 1; R2, R3, R4, R5 and R6 are the same or different, and are independently selected from hydrogen, halo and C1-4 alkyl; R1 is selected from hydrogen and C1-6 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C1-6 alkoxy are disclosed which have pesticidal activity. Pesticidal formulations containing the compounds of the formula (I), their use in the control of pests and methods for their preparation are also disclosed.
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- SYNTHESE TOTALE DE STEROIDES A CYCLE C AROMATIQUE
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The ring-C aromatic analogue 4 of 4-androstene 3,17-dione and its 11 hydroxylated(methoxylated) derivatives 20a(b) were prepared by a practical synthetic route.The key steps of the sequence are achieved in superacid: the cyclisation of diarylethane 5a to phenanthrenone 17, and the hydroxylation by hydrogenperoxide of ketone 4 to phenol 20a.
- Berrier, C.,Gesson, J. P.,Jacquesy, J. C.,Renoux, A.
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p. 4973 - 4980
(2007/10/02)
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- Pharmaceutical compositions and method of inhibiting phenylethanolamine N-methyltransferase
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Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase using 2-indanamine compounds having 4 and/or 5 substituents.
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- CHLORINATED 1-AMINOINDANE N-METHYL TRANSFERASE INHIBITORS
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4-Chloro and 4,5-, 5,6- and 6,7-dichloro-1-aminoindanes, useful as inhibitors of norephineprine N-methyl transferase
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