- Efficient pyridinylmethyl functionalization: Synthesis of 10,10-bis[(2-fluoro-4-pyridinyl)methyl]-9(10H)-anthracenone (DMP 543), an acetylcholine release enhancing agent
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2-Fluoro-4-methylpyridine (3) is efficiently functionalized by chlorination, hydrolysis and methane-sulfonylation into the novel alkylating agent 7. This mesylate is used for the bisalkylation of anthrone under carefully defined conditions to prepare the cognition enhancer drug candidate 1. This process proceeds in up to 37% overall yield and is adaptable for large scale synthesis.
- Pesti,Huhn,Yin,Xing,Fortunak,Earl
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- SUBSTITUTED GUANIDINE DERIVATIVE
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The present invention provides a compound of general formula (I) (wherein, R1, X, p and q are as described in the present description and claims), or a pharmacologically acceptable salt thereof, and a pharmaceutical composition containing that compound.
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Paragraph 1401; 1402
(2018/06/23)
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- Substituted purinon derivatives and medicinal use thereof
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The invention relates to substituted purinon derivatives represented by formula (I), and pharmaceutically acceptable salts, isomers, prodrugs and medicinal compositions thereof. Above compounds are stimulants of soluble guanylate cyclase. In the formula (I), R1 represents a thienyl group or a substituted pyridyl group, R2 represents -NH2 or -NHCH3, and R3 represents hydrogen or a C1-C4 alkyl group. The invention also discloses a preparation method of the compounds and an application of the compounds as medicines, especially an application as cardiovascular disease treatment medicines.
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Paragraph 0071-0072
(2018/05/07)
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- Substituted pyrazolopyridine derivatives and medicinal use thereof
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The invention relates to substituted pyrazolopyridine derivatives represented by formula (I), and pharmaceutically acceptable salts, isomers, prodrugs and medicinal compositions thereof. Above compounds are stimulants of soluble guanylate cyclase. In the formula (I), R1 represents a thienyl group or a substituted pyridyl group, R2 represents -NH2, -NHCH3 or -NHC(=O)CH(CH3)2, R3 represents hydrogenor a C1-C4 alkyl group, and R4 represents a C1-C6 alkyl group. The invention also discloses a preparation method of the compounds and an application of the compounds as medicines, especially an application as cardiovascular disease treatment medicines, such as anti-pulmonary arterial hypertension medicines.
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Paragraph 0106; 0107
(2018/05/07)
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- Modular Route to Azaindanes
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A convergent radical based route to azaindanes is described, relying on the degenerative addition transfer of various substituted S-(pyridylmethyl)-O-ethyl dithiocarbonates (xanthates) to functional alkenes followed by radical cyclization onto the pyridine ring activated by protonation with trifluoroacetic acid. In one case, a richly decorated cyclohepta[b]pyridine could be assembled swiftly by allowing the first adduct to N-phenylmaleimide to undergo addition to N-allylphthalimide prior to cyclization.
- Huang, Qi,Zard, Samir Z.
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supporting information
p. 3895 - 3898
(2017/07/26)
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- HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS JAK INHIBITORS
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The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
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Page/Page column 88
(2011/05/06)
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- METHYL SULFANYL PYRMIDMES USEFUL AS ANTIINFLAMMATORIES, ANALGESICS, AND ANTIEPILEPTICS
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The present invention relates to pyrimidine derivatives of Formula (Ia) and (Ib) (including tautomers, isomers, prodrugs, and pharmaceutically acceptable salts thereof). Said compounds are useful in the treatment of pain (such as neuropathic pain), inflammation, and epilepsy (by acting as anticonvulsants). Methods of medical treatment making use of said compounds, as well as additional compounds of Formula (IIa) and (IIb), are also disclosed.
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Page/Page column 98
(2010/12/18)
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- BETA-AMYLOID PROTEIN PRODUCTION/SECRETION INHIBITORS
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Provided are novel compounds having an inhibitory activity against production or secretion of β-amyloid protein. They embrace compounds represented by the following formula (1): and capable of being replaced with a variety of substituents; and salts thereof, and solvates of any one of them.
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- Potentiators of glutamate receptors
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The present invention relates to potentiators of metabotropic glutamate receptor function and specifically provides compounds of formula I, compositions thereof and methods of using the same.
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