- NEW CHEMICAL COMPOUNDS
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The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, Qa, Qb, QH, L and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
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Page/Page column 35-36
(2012/04/23)
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- HETEROCYCLIC CARBOXYLIC ACID AMIDES AS PDK1 INIHIBITORS
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The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, Qa, Qb, QH, L and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
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Page/Page column 65
(2011/11/06)
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- 1H - IMIDAZO [4, 5 - C] QUINOLINES
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The present invention encompasses compounds of general formula (1), wherein the groups R1 to R7, Qa, Qb, L, n and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations containing such compounds and their use as medicaments.
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Page/Page column 58
(2011/12/04)
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- NEW CHEMICAL COMPOUNDS
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The present invention encompasses compounds of general formula (1) wherein the units W, A, L, Q1 and QH are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use as medicaments having the above-mentioned properties.
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Page/Page column 105
(2010/04/03)
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- Synthesis of 2′-C-methyl ribonucleoside analogues with modified heterocyclic base moieties
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Recently, 2′-C-methyl nucleoside analogues have been reported to exhibit potent anti-hepatitis C virus (HCV) activity through inhibition of HCV RNA replication without significant cytotoxicity. As a part of our continuous efforts of searching for novel antiviral agents, we now report the synthesis of heterobase-modified 2′-C-methyl ribonucleoside analogues. Copyright Taylor & Francis Group, LLC.
- Kim, Myong Jung
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experimental part
p. 2988 - 2999
(2010/11/05)
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- Synthesis of regioisomeric 6,9-(chlorofluoro)-substituted benzo[g]quinoline-5,10-diones, benzo[g]isoquinoline-5,10-diones and 6-chloro-9-fluorobenzo[g]quinoxaline-5,10-dione
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Treatment of difluoro or chloro fluoro-substituted benzyl bromides 5a-c with zinc dust in tetrahydrofuran leads to the corresponding benzylic zinc bromides 6a-c. These organometallics on treatment with chlorosubstituted heterocyclic esters 4A and 4B mediated by nickel catalysis undergo couplings to yield dihalobenzyl substituted heterocyclic esters 7Aa-c and 7Ba-c. Treatment of 4c with 6c under Pd catalysis leads to 7Cc. The acids 8, prepared by hydrolysis of these esters, with treatment of fuming sulfuric acid undergo cyclizations and oxidations to yield the desired regioisomeric dihalo-substituted heterocyclic quinones 2.
- Krapcho, A. Paul,Gallagher, Cynthia E.,Hammach, Abdelhakim,Ellis, Michael,Menta, Ernesto,Oliva, Ambrogio
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- Methyl 3-(triphenylphosphoranylideneamino)pyrazine-2-carboxylate: Synthesis, crystal structure and use in pteridin-4(3H)-ones synthesis
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The title iminophosphorane 6 has been prepared from methyl 3-aminopyrazine-2-carboxylate 1 by a modified Kirsanov method using a triphenylphosphine-hexachloroethane-triethylamine system. The crystal structure of 6 illustrated an iminophosphorane function (N=P bond). 2,3-Disubstituted pteridin-4(3H)-ones were obtained in a one-pot reaction of 6 with isocyanates, followed by heterocyclization on addition of alcohols or amines.
- Okawa, Tomohiro,Eguchi, Shoji,Kakehi, Akikazu
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p. 247 - 254
(2007/10/03)
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