Extracurricular laboratory:new discovery of 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid

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A phthalazinone derivative and its preparation method and medical use (by machine translation)

The present invention provides a phthalazinone derivative and its preparation method and medical use. In order to O-aldehyde benzoic acid as the raw material, by reaction with methyl (3 – oxo – 1, 3 – ISO-benzofuran – 1 – yl) phosphonic acid dimethyl ester, the compound with 3 – cyano – 4 – fluorophenyl with formaldehyde in the presence of triethylamine to produce (Z, E) – 2 – fluoro – 5 – [(3 – oxoisoindoline benzofuran – 1 (3 H) – ylidene) methyl] benzonitrile, it is hydrazine hydrate is reduced to 2 – fluoro – 5 – [(4 – oxo – 3, 4 – […] – 1 – yl) methyl] benzoic acid; benzene formaldehyde or substituted aryl formaldehyde or furfural as raw materials, with malonic acid in the Knoevenagel reaction, the obtained acrylic acid or substituted the acrylic acid or furan – 2 – acrylic acid, with 1 – tert-butoxycarbonyl piperazine generating amide reaction, the product in the presence of trifluoroacetic acid takes off uncle butoxycarbonyl, the obtained product with 2 – fluoro – 5 – [(4 – oxo – 3, 4 – […] – 1 – yl) methyl] benzoic acid generating amide reaction, to obtain a series of (E)- 4 – {3 – [4 – [(3 – substituted aromatic) acryloyl] piperazine – 1 – carbonyl] – 4 – fluorobenzyl} – 2 H – phthalazine – 1 – one derivatives. The initial pharmacological activity screening results show, the invention of the general formula of the compounds have certain in vitro PARP – 1 inhibition ability and the in vitro anti-tumor cell proliferation activity. The said compound of general structure is as follows: In the above formula: Ar selected from or R1 , R2 , R3 , R3 , R4 , R5 Can be a hydrogen atom, a fluorine atom, chlorine atom, bromine atom, methyl, methoxy, trifluoromethyl, nitro. (by machine translation)

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Phthalazine – Wikipedia,
Phthalazine | C8H6N754 – PubChem

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LOW AFFINITY POLY(AD-RIBOSE) POLYMERASE 1 DEPENDENT CYTOTOXIC AGENTS

The present disclosure provides compounds of Formula (I) or (II), pharmaceutically acceptable salt, isotopic variant, stereoisomer, or a mixture thereof. Also provided are pharmaceutical compositions comprising a compound, methods of treating a poly(ADP-ribose)polymerase-1-mediated disease or disorder in a subject, methods of detecting a poly(ADP-ribose)polymerase-1-mediated neurodegenerative disease or disorder, or methods of monitoring cancer treatment in a subject. In some embodiments, the poly(ADP-ribose)polymerase-1-mediated disease or disorder is a neurodegenerative disease or cancer.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N751 – PubChem

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 763114-26-7, name is 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid, introducing its new discovery. Computed Properties of C16H11FN2O3

DUAL INHIBITORS OF PARP1 AND CDK

Disclosed herein, in various embodiments, are compounds having dual activity as PARP1 and CDK inhibitors, and pharmaceutical compositions comprising the same. In some embodiments, the present disclosure provides for methods of treating diseases or conditions in a subject in need thereof, comprising administering one or more compounds disclosed herein. In some embodiment, the disease is cancer, including breast cancer.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N737 – PubChem

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PHTHALAZINONE KETONE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL USE THEREOF

A phthalazinone ketone derivative as represented by formula (I), a preparation method thereof, a pharmaceutical composition containing the derivative, a use thereof as a poly (ADP-ribose) polymerase (PARP) inhibitor, and a cancer treatment method thereof.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N767 – PubChem

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Containing the phthalazine -1 (2 H) – one structure of PARP – 1 and PI3K double-target inhibitors (by machine translation)

The invention relates to the field of pharmaceutical chemistry, in particular relates to a containing phthalazine – 1 (2 H) – one and triazine or pyrimidine structure of PARP – 1 and PI3K double-target inhibitor (I), processes for their preparation, and pharmaceutical compositions containing these compounds. The pharmacodynamics experiment proves that the compounds of this invention have anti-tumor efficacy. (by machine translation)

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Phthalazine – Wikipedia,
Phthalazine | C8H6N775 – PubChem

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Amino-substituted tetrahydro pyrido pyrimidine compound or its salts and its preparation method and application (by machine translation)

The invention discloses an amino substituted tetrahydro pyrido pyrimidine compound or its salts and its preparation method and application. The compound or its salts having the following general structure or , Wherein R1 , R2 Is C1 – 5 alkyl or amino; R3 With a N 5 – 6 […] members of the heterocyclic radical, the heterocyclic substituent is a nitrogen-containing, containing alkyl-substituted nitrogen or oxygen-containing heterocyclic group. The compound or its pharmaceutically acceptable salt has potent PARP1 inhibitory activity, can be used for treating diseases or cancer drug used for prevention and/or treating PARP1 related diseases. (by machine translation)

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N772 – PubChem

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Phthalazine derivative as well as preparation method and application thereof (by machine translation)

The invention discloses a phthalazine derivative and a preparation method and application, thereof, belongs to the field, of pharmaceutical chemistry, and the preparation method and application of the phthalazine derivative are good PARP and HDAC double-target inhibitor. and the design method, disclosed by the invention can simultaneously inhibit (PARP and) to play both inhibitors at the same time and fully exert the combination effect, of the two inhibitors to obtain a low-toxicity HDAC high-efficiency targeting anti-tumor inhibitor, PARP, The invention discloses a preparation method and application of the phthalazine, derivative PARP, HDAC with, HDAC, protein action/at the tail part of the phthalazine derivative as well, as a preparation method. and application of the phthalazine derivative in the field of pharmaceutical chemistry. (by machine translation)

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Phthalazine – Wikipedia,
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763114-26-7, Name is 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid, belongs to phthalazine compound, is a common compound. name: 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acidIn an article, once mentioned the new application about 763114-26-7.

Preparation method of (by machine translation)

The invention relates to a method. 2 – (2 – (4 – Fluoro -3 – carboxyphenyl) acetyl) benzoate and hydrazine reagent undergo a chemical reaction to give 2 – fluorine -5 – ((4 – oxo -3, 4 – dihydrophthalazine -1 – yl) methyl) benzoic acid compound, followed 2 – fluorine -5 – ((4 – oxo -3, 4 – dihydrophthalazine -1 – yl) methyl) benzoic acid and 1 – cyclopropylcarbamoyl piperazine to achieve the preparation. In addition, 2 – (2 – (4 -fluoro -3 – carboxyphenyl) acetyl) benzoate firstly reacts with 1 -cyclopropylformyl piperazine and then undergoes chemical reaction with hydrazine reagent to complete preparation. (by machine translation)

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Phthalazine – Wikipedia,
Phthalazine | C8H6N770 – PubChem

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Related Products of 763114-26-7, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 763114-26-7, molcular formula is C16H11FN2O3, introducing its new discovery.

4- [3- (4-CYCLOPROPANECARBONYL-PIPERAZINE-l-CARBONYL) -4-FLUORO-BENZYL] -2H-PHTHALAZIN-1-ONE

4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-l-one as crystalline Form L, methods of obtaining form L, pharmaceutical compositions comprising Form L and methods of using Form L and compositions comprising Form L

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N761 – PubChem

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PHTHALAZINONE DERIVATIVES

A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; X and Y are selected from CH and CH, CF and CH, CH and CF and N and CH respectively; RC is selected from H, C1-4 alkyl; and R1 is selected from C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl, which groups are optionally substituted; or RC and R1 together with the carbon and oxygen atoms to which they are attached form a spiro-C5-7 oxygen-containing heterocyclic group, which is optionally substituted or fused to a C5-7 aromatic ring.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N747 – PubChem