- Chemoselective Deoxygenation of 2° Benzylic Alcohols through a Sequence of Formylation and B(C6F5)3-Catalyzed Reduction
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A sequence of formylation and B(C6F5)3-catalyzed reduction of the resulting formate with Et3SiH enables the chemoselective deoxygenation of secondary benzylic alcohols. Primary benzylic and tertiary non-benzylic alcohols are not reduced by this protocol. The formyl group fulfills a double role as activator and self-sacrificing protecting group. The deoxygenation of these formates is fast and can be carried out in the presence of other potentially reducible groups. Neighboring-group participation was found in the deoxygenation of certain diol motifs.
- Oestreich, Martin,Richter, Sven C.
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supporting information
p. 2103 - 2106
(2021/07/22)
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- IMIDAZOLE-BASED ANTICANCER AGENTS AND DERIVATIVES THEREOF, AND METHODS OF MAKING AND USING SAME
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Imidazole-based anticancer agents and derivatives thereof, as well as methods of making and methods of using the same, are described. The imidazole-based anticancer agents are HDAC inhibitor compounds having a 1-(1H-imidazol-2-yl)ethan-1-one or 1-(1H-imidazol-2-yl)ethane-1- thione moiety.
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Paragraph 00154-00155
(2019/03/05)
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- OXADIAZOLONES AS TRANSIENT RECEPTOR POTENTIAL CHANNEL INHIBITORS
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The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
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Paragraph 0307; 0308; 0311; 0312
(2018/06/12)
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- COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY
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The present invention relates to compounds acting both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists, to processes for their preparation, to compositions comprising them, to therapeutic uses and combinations with other pharmaceutical active ingredients.
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Page/Page column 74; 75
(2014/06/24)
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- COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY
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Compounds of formula (I) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
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Page/Page column
(2014/06/24)
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- SPIRO-SUBSTITUTED OXINDOLE DERIVATIVES HAVING AMPK ACTIVITY
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The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
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Page/Page column 80
(2015/01/07)
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- SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
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Page/Page column 47
(2013/10/22)
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- PURINE DERIVATIVES
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The invention provides the compound of formula. (I) and pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and the use of the compound in therapy.
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Page/Page column 36-37
(2012/06/30)
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- BEZOTHIAZOL DERIVATIVES AS BETA2 ADRENORECEPTOR AGONISTS
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The present invention relates to compounds according to formula (I) , a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta2 adrenoreceptor agonists.
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Page/Page column 68
(2008/06/13)
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- Biphenyl compounds useful as muscarinic receptor antagonists
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The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
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Page/Page column 37
(2010/11/25)
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- 3,4,5-Trisubstituted isoxazoles as novel PPARδ agonists. Part 2
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A series of PPARδ-selective agonists was investigated and optimized for a favorable in vivo pharmacokinetic profile. Isoxazole LCI765 (17d) was found to be a potent and selective PPARδ agonist with good in vivo PK properties in mouse (Cmax = 5.1 μM, t1/2 = 3.1 h). LCI765 regulated expression of genes involved in energy homeostasis in relevant tissues when dosed orally in C57BL6 mice. A co-crystal structure of compound LCI765 and the LBD of PPARδ is discussed.
- Epple, Robert,Azimioara, Mihai,Russo, Ross,Xie, Yongping,Wang, Xing,Cow, Christopher,Wityak, John,Karanewsky, Don,Bursulaya, Badry,Kreusch, Andreas,Tuntland, Tove,Gerken, Andrea,Iskandar, Maya,Saez, Enrique,Martin Seidel,Tian, Shin-Shay
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p. 5488 - 5492
(2007/10/03)
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- Photolytic decarboxylation of α-arylcarboxylic acids mediated by HgF2 under a dioxygen atmosphere
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Mercuric fluoride (HgF2), as a light-sensitive inorganic compound, in the presence of dioxygen is able to convert various α-aryl- and α,α-diarylcarboxylic acids into the corresponding aldehydes and ketones selectively under photoirradiation via trapping of the benzylic radical by O2.
- Farhadi, Saeid,Zaringhadam, Parisa,Sahamieh, Reza Zarei
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p. 1965 - 1968
(2007/10/03)
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- Arylacetamide κ opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity
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Some κ opioid receptor agonists of the arylacetamide class, for example, ICI 199441 (1), were found to strongly inhibit the activity of cytochrome P450 2D6 (CYP2D6) (1: CYP2D6 IC50 = 26 nM). Certain analogs bearing a substituted sulfonylamino group, for example, 13, were discovered to have significantly reduced CYP2D6 inhibitory activity (13: CYP2D6 IC50 > 10 μM) while displaying high affinity toward the cloned human κ opioid receptor, good κ/δ and κ/μ selectivity, and potent in vitro and in vivo agonist activity.
- Le Bourdonnec, Bertrand,Ajello, Christopher W.,Seida, Pamela R.,Susnow, Roberta G.,Cassel, Joel A.,Belanger, Serge,Stabley, Gabriel J.,DeHaven, Robert N.,DeHaven-Hudkins, Diane L.,Dolle, Roland E.
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p. 2647 - 2652
(2007/10/03)
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- Sulfonylamino phenylacetamide derivatives and methods of their use
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Sulfonylamino phenylacetamide derivatives of the general formula are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed. In certain embodiments, the compounds of the invention that, preferably: (1) bind with high affinity to κ opioid receptors; (2) display good opioid receptor selectivity of κ versus μ and κ versus δ; and (3) do not substantially inhibit cytochrome P450 enzymatic activity, in particular CYP2D6, CYP2C9 and CYP3A4.
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- NOVEL BENSOPHENONE DERIVATIVES OR SALTS THEREOF
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A benzophenone derivative represented by the following formula: whereinR1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl;R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, ???or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.
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Page 122-123
(2010/02/07)
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- Formation of Heptafulvene in Reactions of phenylcarbene in the Gas Phases
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Flash vacuum pyrolysis of phenyl>diazomethanes produced 1-(methoxycarbonyl)benzocyclobutene, as a result of intramolecular C-H insertion in the ortho isomer of phenyl>carbene generated by carbene-carbene rearrangement, and 8-(methoxycarbonyl)heptafulvene, presumably formed by intramolecular H migration in the seven-membered ring intermediates involved in the rearrangement.
- Tomioka, Hideo,Taketsuji, Kohji
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p. 4196 - 4197
(2007/10/02)
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