- Boron Containing PDE4 Inhibitors
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The present invention relates to boron containing compounds of Formula (I) [in-line-formulae]X—Y—Z?? Formula (I)[/in-line-formulae] that inhibit phosphodiesterase 4 (PDE4). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating diseases, conditions, or disorders ameliorated by inhibition of PDE4.
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Paragraph 0647-0648; 0697-0698
(2020/04/29)
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- Novel preparation method of drotaverine hydrochloride intermediate
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The invention discloses a novel preparation method of a drotaverine hydrochloride intermediate. The preparation method comprises the steps that 1, 4-bromopyrocatechol serves as the raw material and issubjected to an ethylation reaction under the action of iodoethane or diethyl sulfate, and 1,2-diethoxy-4-bromobenzene is prepared; 2, 1,2-diethoxy-4-bromobenzene is subjected to a Suzuki-Miyaura coupling reaction and reacts with ethyl bromoacetate or methyl bromoacetate to prepare 3,4-diethoxyphenylaceticacid ester; 3, 3,4-diethoxyphenylaceticacid is hydrolyzed to prepare 3,4-diethoxyphenylaceticacid; 4, 3,4-diethoxyphenylaceticacid ester and ammonia are prepared into 3,4-diethoxyphenylacetamide; 5, 3,4-diethoxyphenylacetamide is reduced to prepare 3,4-diethoxyphenethylamine. The direct preparation method is used; in the process of preparing 3,4-diethoxyphenyl acetonitrile, application of sodium cyanide is avoided; when 3,4-diethoxyphenethylamine is prepared, lithium aluminium hydride isused for reduction, and a pressurized hydrogenation method is prevented from being used, so that the problems about safety and environment pollution are effectively solved, the process is simple andeasy to implement, and the practicality is high.
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Paragraph 0017; 0034-0037; 0042-0045; 0052-0055; 0060-0063
(2019/06/27)
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- NEW AZIRIDINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE AS ACETYL-COA CARBOXYLASE INHIBITORS
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The invention relates to new azetidine derivatives of the formula (I) wherein Ar1, Ar2, X, R, T and L are as defined in the description, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
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Page/Page column 82; 84
(2013/07/05)
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- AZETIDINE DERIVATIVES
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Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
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Paragraph 0495; 0496; 0497; 0498; 0499; 0500
(2013/06/28)
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- 1H-IMIDAZO[4,5-c]QUINOLINONE DERIVATIVES
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The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c] quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H- imidazo[4,5-c] quinofinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c] quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1 H- imidazo[4,5-c] quinolinone derivatives; and a process for the preparation of the novel 1H- imidazo[4,5-c] quinolinone derivatives.
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Page/Page column 138
(2010/12/29)
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- 2,4-SUBSTITUTED QUINAZOLINES AS LIPID KINASE INHIBITORS
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The invention relates to compounds of the formula (I), which are appropriate for the treatment of kinase, e.g. PI3K-related, diseases, such as proliferative diseases, inflammatory diseases, obstructive airways disorders and transplantation related disease
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Page/Page column 69-70
(2008/06/13)
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- CYANOCYCLOPROPYLCARBOXAMIDES AS CATHEPSIN INHIBITORS
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The present invention relates to compounds of formula (I) for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.
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Page/Page column 133
(2009/03/07)
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- CHEMICAL COMPOUNDS
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Compounds of formula (Ia) are found to be active in inhibiting replication of flaviviridae viruses (Ia), wherein R1 and R2 are the same or different and represent hydrogen, halogen, -L-O-R3, -L-O-L-A or -L-O-L′-A′, wherein each L is the same or different and represents a direct bond or a C1-C4 alkylene group; L′ represents a direct bond or a C2-C4 alkylene group; R3 represents hydrogen, C1-C4 alkyl or C1-C4 haloalkyl; A represents a 5- to 10-membered heterocyclyl group; and A′ represents a C6-C1 aryl group; wherein at least one of R1 and R2 is -L-O-R3, -L-O-L-A or -L-O-L′-A′.
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Page/Page column 15
(2008/06/13)
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- TRIAZOLOANILINOPYRIMIDINE DERIVATIVES FOR USE AS ANTIVIRAL AGENTS
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A quinazoline derivative of formula (I), or a pharmaceutically acceptable salt thereof: formula (I) for use in treatment of prevention of a flaviviridae infection.
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Page/Page column 27-28
(2010/11/28)
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- PHOSPHORORGANISCHE VERBINDUNGEN 101. TERTIAERE PHOSPHINE MIT ORTHOALKOXYPHENYL-GRUPPEN. Synthese und Eigenschaften
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Alkylphenylethers, ortho-lithiated in good yields, are transformed according to scheme (1) to the triarylphosphines ArPPh2, Ar2PPh and Ar3P (Ar contains in all cases an ortho-alkoxy group) (Table 1.).Hydroquinonedialkylethers can be lithiated twice, forming the compounds 102 and 103.Table 2 summarizes some arylalkylethers (71 - 101) which were lithiated; table 7 presents 12 new arylalkylethers.The syntheses of triarylphosphines with one or two bulky groups (105 - 110) and of triarylphosphines with one or two 3,4-dialkoxyphenyl groups (111 - 114) are reported.The 31P-spectra of the compounds prepared are discussed with respect to the validity of the Tolman-rule.
- Horner, L.,Simons, G.
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p. 189 - 210
(2007/10/02)
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