- SPIROHYDANTOIN COMPOUNDS AND THEIR USE AS SELECTIVE ANDROGEN RECEPTOR MODULATORS
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The present invention relates to a compound of formula (1-1 ) in free form or in pharmaceutically acceptable salt form in which the substituents are as defined in the specification; to its preparation, to its use as a medicament and to medicaments comprising it. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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Page/Page column 73
(2013/09/12)
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- 2-METHYLENE-5-SUBSTITUTED-METHYLENECYCLOPENTANONE DERIVATIVES AND USE THEREOF
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The invention relates to 2-methylene-5-substituted-methylenecyclopentanone derivatives of formula I, and the use thereof. The derivatives of formula I as active components are useful for preparing a medicine for the treatment and/or prevention of cancer diseases such as breast cancer, lung cancer, colon cancer, rectal cancer, stomach cancer, prostate cancer, bladder cancer, uterus cancer, pancreatic cancer and ovary cancer. The active compounds of the invention may be used as an anticancer drug alone or used in combination with one or more other antitumor drugs. A combined therapy can be carried out by administrating each therapeutic component concurrently, subsequently or separately.
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- 2-METHYLENE-5-SUBSTITUTED METHYLENE CYCLOPENTANONE DERIVATIVES AND USE THEREOF
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The invention relates to 2-methylene-5-substituted-methylenecyclopentanone derivatives of formula I, and the use thereof. The derivatives of formula I as active components are useful for preparing a medicine for the treatment and/or prevention of cancer diseases such as breast cancer, lung cancer, colon cancer, rectal cancer, stomach cancer, prostate cancer, bladder cancer, uterus cancer, pancreatic cancer and ovary cancer. The active compounds of the invention may be used as an anticancer drug alone or used in combination with one or more other antitumor drugs. A combined therapy can be carried out by administrating each therapeutic component concurrently, subsequently or separately.
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Page/Page column 17
(2010/11/19)
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- Microbiological transformations 60. Enantioconvergent baeyer-villiger oxidation via a combined whole cells and ionic exchange resin-catalysed dynamic kinetic resolution process
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A dynamic kinetic resolution process was applied to an enantioconvergent microbial Baeyer-Villiger oxidation of benzyloxycyclopentanone, rac-1. This was achieved by combining a whole cell-based kinetic resolution and an anion exchange resin-catalysed in s
- Gutierrez, Maria-Concepcion,Furstoss, Roland,Alphand, Veronique
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p. 1051 - 1059
(2007/10/03)
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- Synthesis and photoinitiated radical cyclization of allyl- and propynyloxymethyl substituted cyclopentanones to tetrahydrocyclopenta[c]furanols
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Bicyclic cyclopentafuranols were formed by photoinitiated radical cyclization of allyl- and propinyloxymethyl substituted cyclopentanones with high regioselectivity. The irradiations were carried out at a wavelength of 300 nm in aprotic solvents such as benzene and acetonitrile. We could also show that reductive photoinduced electron transfer (PET) of the propynyloxymethyl substituted cyclopentanone 5 does not lead to any cyclization. The starting materials were synthesized in good yields following known procedures.
- Tzvetkov, Nikolay T.,Mattay, Jochen
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p. 7751 - 7755
(2007/10/03)
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- Design, new synthesis, and calcilytic activity of substituted 3H-pyrimidin-4-ones
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Design, new synthesis, structure-activity relationship studies and calcium receptor antagonist (calcilytic) properties of novel 3H-pyrimidin-4-ones are described.
- Shcherbakova, Irina,Huang, Guangfei,Geoffroy, Otto J.,Nair, Satheesh K.,Swierczek, Krzysztof,Balandrin, Manuel F.,Fox, John,Heaton, William L.,Conklin, Rebecca L.
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p. 2537 - 2540
(2007/10/03)
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- Synthesis and anticancer activity of 2-alkylaminomethyl-5-diaryl- methylenecyclopentanone hydrochlorides and related compounds
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Eleven new diaryl-methylenecyclopentanone Mannich hydrochlorides and related compounds were synthesized with different modification on Mannich base and α,β-unsaturated bonds. The glutathione-binding ability, glutathione-s-transferase π (GSTπ) inhibition a
- Wang, Jingli,Zhao, Linxiang,Wang, Rui,Lu, Min,Chen, Duo,Jing, Yongkui
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p. 1285 - 1291
(2007/10/03)
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- Cathodic cyclisation of N-(oxoalkyl)pyridinium salts - Formation of tricyclic indolizidine and quinolizidine derivatives in aqueous medium
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The cathodic cyclisation of N-(oxoalkyl)pyridinium salts, derived from 4-methylpyridine and cyclic ketones, afforded functionalised tricyclic indolizidine and quinolizidine derivatives in high yields. Through systematic variation of the ring size of the k
- Heimann, Jens,Schaefer, Hans J.,Froehlich, Roland,Wibbeling, Birgit
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p. 2919 - 2932
(2007/10/03)
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- Highly efficient heterogeneous acetalization of carbonyl compounds catalyzed by a titanium cation-exchanged montmorillonite
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The titanium cation-exchanged montmorillonite efficiently catalyzed the selective acetalization of various carbonyl compounds as a recyclable solid acid. This heterogeneous catalyst has an advantage of a strikingly simple workup procedure over conventional homogeneous acids.
- Kawabata, Tomonori,Mizugaki, Tomoo,Ebitani, Kohki,Kaneda, Kiyotomi
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p. 8329 - 8332
(2007/10/03)
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- Facile synthesis of unsaturated lactones via intramolecular Wittig reaction
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The phosphoranes 3 formed from the reaction of a variety of keto alcohols 1 and (triphenylphosphoranylidene)ethenone 2 undergo intramolecular Wittig cyclization to afford the unsaturated lactones in moderate yields.
- Kumar, Pradeep,Saravanan
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p. 2161 - 2168
(2007/10/03)
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- 26,28-methylene-1α, 25-dihydroxyvitamin D2 compounds
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Vitamin D2 analogs in which a cyclopentane ring is introduced into the side chain of 1α,25-dihydroxyvitamin D2 The compounds are characterized by a marked intestinal calcium transport activity while exhibiting much lower activity tha
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- An Efficient Baeyer-Villiger Approach to 6-(Hydroxymethyl)tetrahydro-2H-pyran-2-one Derivatives
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An efficient (64percent overall yield) five step preparation of 6-(tert-butyldiphenylsiloxymethyl)tetrahydro-2H-pyran-2-one from ethyl 2-oxocyclopentane carboxylate is reported.
- Taylor, Richard J. K.,Wiggins, Karen,Robinson, David H.
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p. 589 - 590
(2007/10/02)
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- Cyclit-Reaktionen, II. Darstellung von Bausteinen zur Synthese carbocyclischer Furanose-Analoga
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The four isomeric hydroxycyclopentenmethanols 6a to 9a can easily be made by allylhydroxylation of the epoxides 2 and 4 with phenyl selenide.In a second way the pair 8a and 9a has been synthesized from 11 via 15.As the preparation of 20 demonstrates, the functionalisation of 6a to 9a to carbocyclic furanoses is possible.The dicarboxylic diethyl esters 23 and 33 can be converted into models for carbocyclic ketofuranoses.
- Paulsen, Hans,Maass, Uwe
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p. 346 - 358
(2007/10/02)
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