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PIPERAZINOTRIZOLE COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF IN DRUG PREPARATION

Provided is a piperazinotriazole compound represented by general formula I or an isomer, a pharmaceutically acceptable salt, ester, prodrug or hydrate thereof. Also provided are a method for preparing the compound, a drug composition containing the compound, and a use thereof as a high-selectivity poly(ADP-ribose)polymerase-1 (PARP 1) inhibitor in the preparation of drugs for the prevention and / or treatment of PARP-related diseases.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N779 – PubChem

Discovery of 1-Chloro-6,7-dimethoxyphthalazine

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Related Products of 70724-23-1, 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, 70724-23-1, molcular formula is C10H9ClN2O2, introducing its new discovery.

1-PIPERIDINOPHTHALAZINES AS CARDIAC STIMULANTS

A series of 1-piperidinophthalazine derivatives as phosphodiesterase inhibitors and cardiac stimulants

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Phthalazine – Wikipedia,
Phthalazine | C8H6N691 – PubChem

Final Thoughts on Chemistry for 1242156-59-7

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INHIBITORS OF BRUTON?S TYROSINE KINASE

This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-III: wherein, variables Q, R, X, X’, Y1, Y2, Y2′, Y3, Y4, Y5, m, and n are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N682 – PubChem

More research is needed about 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid

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Synthesis and evaluation of a radioiodinated tracer with specificity for poly(ADP-ribose) polymerase-1 (PARP-1) in vivo

Interest in nuclear imaging of poly(ADP-ribose) polymerase-1 (PARP-1) has grown in recent years due to the ability of PARP-1 to act as a biomarker for glioblastoma and increased clinical use of PARP-1 inhibitors. This study reports the identification of a lead iodinated analog 5 of the clinical PARP-1 inhibitor olaparib as a potential single-photon emission computed tomography (SPECT) imaging agent. Compound 5 was shown to be a potent PARP-1 inhibitor in cell-free and cellular assays, and it exhibited mouse plasma stability but approximately 3-fold greater intrinsic clearance when compared to olaparib. An 123I-labeled version of 5 was generated using solid state halogen exchange methodology. Ex vivo biodistribution studies of [123I]5 in mice bearing subcutaneous glioblastoma xenografts revealed that the tracer had the ability to be retained in tumor tissue and bind to PARP-1 with specificity. These findings support further investigations of [123I]5 as a noninvasive PARP-1 SPECT imaging agent.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N802 – PubChem

Simple exploration of 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid

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ANTI-CANCER NUCLEAR HORMONE RECEPTOR-TARGETING COMPOUNDS

The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N758 – PubChem

A new application about 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid

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A kind of Phthalazinone derivatives and its use (by machine translation)

The present invention provides novel phthalazinone compounds and isomer thereof, pharmaceutically acceptable salts, solvates, chemically protected forms, and prodrugs; which can be used as PARP inhibitor and pharmaceutical compositions containing the novel phthalazinone compounds; wherein A, R1 and X are defined as shown. The medicine is used for the treatment of: vascular diseases, neurotoxicity, or diseases improved through the inhibition of PARP activity; or used as adjuvants for the treatment of cancers, or used for enhancing the therapeutic effect of radiation or chemotherapeutic agents on tumor cells, wherein the cancers includes breast cancer, ovarian cancer, colon cancer, melanoma, lung cancer, gastrointestinal stromal tumor, brain cancer, cervical cancer, pancreatic cancer, prostate cancer, gastric cancer, chronic myeloid leukocytes hypercytosis, liver canser, lymphoma, peritoneal cancer, soft tissue sarcoma, neuroendocrine tumors, advanced solid tumors, and glioblastoma.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N769 – PubChem

The Absolute Best Science Experiment for 763114-26-7

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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. Quality Control of 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acidIn an article, once mentioned the new application about 763114-26-7.

Benzene and [4, 5] imidazo [1, 2 – a] pyrazine ketone derivative and its preparation and use (by machine translation)

The invention provides a benzene and [4, 5] imidazo [1, 2 – a] pyrazine ketone derivatives and their pharmaceutically acceptable salt, its structure is shown as formula I. The invention also discloses containing benzo [4, 5] imidazo [1, 2 – a] pyrazine ketone derivatives preparation method and its in the preparation of antineoplastic drug in the preparation and application of PARP inhibitors. (by machine translation)

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Phthalazine – Wikipedia,
Phthalazine | C8H6N774 – PubChem

The important role of 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid

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Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy

Concomitant inhibition of PARP and PI3K pathways has been recognized as a promising strategy for cancer therapy, which may expand the clinical utility of PARP inhibitors. Herein, we report the discovery of dual PARP/PI3K inhibitors that merge the pharmacophores of PARP and PI3K inhibitors. Among them, compound 15 stands out as the most promising candidate with potent inhibitory activities against both PARP-1/2 and PI3Kalpha/deltawith pIC50 values greater than 8. Compound 15 displayed superior antiproliferative profiles against both BRCA-deficient and BRCA-proficient cancer cells in cellular assays. The prominent synergistic effects produced by the concomitant inhibition of the two targets were elucidated by comprehensive biochemical and cellular mechanistic studies. In vivo, 15 showed more efficacious antitumor activity than the corresponding drug combination (Olaparib + BKM120) in the MDA-MB-468 xenograft model with a tumor growth inhibitory rate of 73.4% without causing observable toxic effects. All of the results indicate that 15, a first potent dual PARP/PI3K inhibitor, is a highly effective anticancer compound.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N786 – PubChem

The important role of 763114-26-7

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A method for preparing aurar handkerchief Nepal (by machine translation)

The invention discloses a method for preparing aurar handkerchief Nepal, comprises the following steps: step one: synthesis of (3 – oxo – 1, 3 – dihydro – isobenzofuran – 1 – yl) phosphonic acid dimethyl ester; step two: synthesis of 2 – fluoro – 5 – (3 – oxo – 1, 3H – ISO-benzofuran asian base methyl) benzonitrile; step three: synthesis of 2 – fluoro – 5 – ((4 – oxo – 3, 4 – dihydro taitai qin – 1 – yl) methyl) benzoic acid; step four: synthetic aurar handkerchief Nepal. Compared with the prior art, the invention of the preparation method of the aurar handkerchief Nepal, cheap raw materials, has little influence to environment, the equipment requirement is low, the reaction time is short, the purity of the product after the purification and the like, can improve the production efficiency. (by machine translation)

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N768 – PubChem

The important role of 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid

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Application 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.

TRICYCLIC INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE

The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-1(2H)-one derivatives. The compounds are potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP-ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N762 – PubChem