3682-19-7Relevant articles and documents
INHIBITORS OF CYCLIN-DEPENDENT KINASES
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Paragraph 00337, (2021/02/12)
Provided herein are compounds which are inhibitors of cyclin-dependent kinases (CDKs), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
Luminol or isoluminol synthesizing method by one-pot process
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, (2017/08/30)
The invention discloses a luminol or isoluminol synthesizing method by a one-pot process. The luminol or the isoluminol synthesizing method by the one-pot process includes the steps of 1) enabling 3-nitrophthalic acid or 4-nitrophthalic acid as a starting material to react with urea in an organic solvent to obtain 3-nitrophthalimide or 4-nitrophthalimide; 2) enabling the 3-nitrophthalimide or the 4-nitrophthalimide to react with a hydrazine hydrate aqueous solution to obtain 3-nitrophthalhydrazide or 4-nitrophthalhydrazide; 3) enabling the 3-nitrophthalhydrazide or the 4-nitrophthalhydrazide to react with a reducing agent in the presence of a catalyst to obtain luminol or isoluminol. The luminol or the isoluminol synthesizing method by the one-pot process has the advantages of simplicity, convenience in operation, low cost, high yield and less pollution, and can be applicable to industrialized production.
Method for preparing isoluminol from phthalylhydrazine used as raw material
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Paragraph 0045; 0052; 0053, (2016/10/08)
The invention belongs to the technical field of chemical synthesis and particularly relates to a method for preparing isoluminol from phthalylhydrazine used as a raw material. According to the method for preparing the isoluminol, the phthalylhydrazine is used as the raw material and reacts with an acetylation reagent, and diacetyl phthalylhydrazine is obtained; the diacetyl phthalylhydrazine reacts with a nitroso compound, and nitroso diacetyl phthalylhydrazine is obtained; then nitroso phthalylhydrazine is obtained through a deacetylation reaction; the isoluminol is obtained through a reduction reaction. With the adoption of the method, a large quantity of phthalylhydrazine byproducts in the existing Gabriel amine synthesis method are sufficiently utilized as the raw material, the raw material is cheap and easy to obtain, meanwhile, the synthesis process is simple, reaction conditions are mild, the yield of isoluminol products is higher, reactions are simple to operate, the application range is wider, and industrial production requirements of the products can be fully met.
PHTHALAZINE DERIVATIVES
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Page/Page column 53, (2008/12/05)
The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Methods of inhibiting BTK and SYK protein kinases
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Page/Page column 60, (2008/06/13)
Methods of inhibiting a tyrosine kinase wherein said tyrosine kinase is BTK or SYK comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to formula I are disclosed. The compounds are useful for treating auto-immune and inflammatory diseases.
NOVEL PHTHALAZINONE DERIVATIVES, AS AURORA-A KINASE INHIBITORS
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Page/Page column 159, (2008/06/13)
Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
4-Benzylamino-1-chloro-6-substituted phthalazines: Synthesis and inhibitory activity toward phosphodiesterase 5
Watanabe, Nobuhisa,Kabasawa, Yasuhiro,Takase, Yasutaka,Matsukura, Masayuki,Miyazaki, Kazuki,Ishihara, Hiroki,Kodama, Kohtarou,Adachi, Hideyuki
, p. 3367 - 3372 (2007/10/03)
We synthesized various 4-benzylamino-1-chloro-6-substituted phthalazines (15) and 4-benzylamino-1-chloro-7-substituted phthalazines (16) and evaluated their inhibitory activity toward phosphodiesterase 5 (PDE5) purified from porcine platelets. The PDE5-inhibitory activities of 15 were greater than those of the isomers (16). The preferred substituent at the 4-position of phthalazine was a (3-chloro-4-methoxybenzyl)amino group, and those at the 6- position were cyano, nitro, and trifluoromethyl groups. Compounds 15a (IC50 = 4.8 nM), 15f (3.5 nM), and 15i (5.3 nM) were more potent inhibitors than E4021 (8.6 nM). Compounds 15a and 15f also showed vasorelaxant activity in isolated porcine coronary arteries precontracted with prostaglandin F(2α) (10-5 M). The EC50 values for vasorelaxant action of 15a, 15f, and E4021 were 150, 160, and 980 nM, respectively. These results show that novel PDE5 inhibitors possessing a potent vasorelaxant effect may exist among phthalazine derivatives.
Implementation of a combinatorial cleavage and deprotection scheme. 1. Synthesis of phthalhydrazide libraries
Nielsen, John,Rasmussen, Palle H.
, p. 3351 - 3354 (2007/10/03)
Phthalhydrazide libraries are synthesized in solution from substituted hydrazines and phthalimides in several different library formats including single compounds, indexed sub-libraries and a full library. When carried out during solid-phase synthesis, this combinatorial cleavage and deprotection scheme offers the possibility for generating a diverse library of substituted phthalhydrazides. Copyright
Benzocyclobutenes. Part 4. Synthesis of Benzocyclobutene-1,2-diones by Pyrolytic Methods
Gould, Ken J.,Hacker, Nigel P.,McOmie, John F. W.,Perry, David H.
, p. 1834 - 1840 (2007/10/02)
Oxidation of the cyclic hydrazides prepared from phthalic anhydrides in the presence of anthracene gives the corresponding Diels-Alder adducts which, on flash vacuum pyrolysis, give benzocyclobutene-1,2-dione (BBD) and its 4-chloro, 3,6- and 4,5-dichloro, 4,5-dibromo, and 4,5-dimethyl derivatives in 75-98percent yield.Cyclobuta- and cyclobuta-naphthalene-1,2-dione as well as cyclobuta- and cyclobuta-pyridine-1,2-dione have been prepared similarly; the last three of these diones are very unstable.Cyclobutanaphthalene-1,2-dione has also been made by pyrolysis of benzindene-1,2,3-trione.Attempts to make thiophen and furan analogues of BBD from appropriate anthracene adducts failed as did attempts to make tetrachloro- and tetrabromo-derivatives of BBD by the pyrolysis of tetrahalogenophthalimidosulphoximides.
