cas 16154-72-6, 3-CHLORO-4-(4-METHYLPIPERAZIN-1-YL)ANILINE

Articles about 16154-72-6Total 12 be found

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PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER
The invention provides compounds of the formula (1): or a salt or tautomer thereof wherein A, R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are inhibitors of Wee1 and/or PLK1 kinase and are envisaged to be useful in the treatment of cancers.
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(2021/04/23)

The synthesis and bioactivity of pyrrolo[2,3-d]pyrimidine derivatives as tyrosine kinase inhibitors for NSCLC cells with EGFR mutations
EGFR mutations are an ongoing challenge in the treatment of NSCLC, and demand continuous updating of EGFR TKI drug candidates. Pyrrolopyrimidines are one group of versatile scaffolds suitable for tailored drug development. However not many precedents of this type of pharmacophore have been investigated in the realm of third generation of covalent EGFR-TKIs. Herein, a series of pyrrolo[2,3-d]pyrimidine derivatives able to block mutant EGFR activity in a covalent manner were synthesized, through optimized Buchwald-Hartwig C–N cross coupling reactions. Their preliminary bioactivity and corresponding inhibitory mechanistic pathways were investigated at molecular and cellular levels. Several compounds exhibited increased biological activity and enhanced selectivity compared to the control compound. Notably, compound 12i selectively inhibits HCC827 cells harboring the EGFR activating mutation with up to 493-fold increased efficacy compared to in normal HBE cells. Augmented selectivity was also confirmed by kinase enzymatic assay, with the test compound selectively inhibiting the T790 M activating mutant EGFRs (IC50 values of 0.21 nM) with up to 104-fold potency compared to the wild-type EGFR (IC50 values of 22 nM). Theoretical simulations provide structural evidence of selective kinase inhibitory activity. Thus, this series of pyrrolo[2,3-d]pyrimidine derivatives could serve as a starting point for the development of new EGFR-TKIs.
Chai, Yingying,Chen, Hai,He, Yang,Huang, Ridong,Li, Weimin,Li, Ying,Ma, Lingling,Xia, Zhenqiang,Yu, Quanwei,Zhou, Xinglong
(2021/07/28)

WEE1 inhibitors as well as preparation and application thereof
The invention relates to WEE1 inhibitors as well as preparation and application thereof. The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, solvates, polymorphs or isomers thereof, and their use in the preparation of medicaments for the treatment of diseases associated with WEE1 activity.
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(2020/10/14)

BRD4-KINASE INHIBITORS AS CANCER THERAPEUTICS
Disclosed herein are compounds that are inhibitors of BDR4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BDR4 are also disclosed. In certain aspects, disclosed are compounds of Formula I through IV.
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(2017/05/02)

POTENT DUAL BRD4-KINASE INHIBITORS AS CANCER THERAPEUTICS
Disclosed herein are compounds that are inhibitors of BRD4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BRD4 are also disclosed. In certain aspects, disclosed are compounds of Formula I-IV.
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(2016/04/26)

PYRAZOLYL-PYRIMIDINES AS KINASE INHIBITORS
Disclosed are compounds having the formula (I): wherein Z, n, R1, R1A, R3, R4, and R5 are as defined herein, and methods of making and using the same.
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Page/Page column 35

(2011/10/13)

N-(3,4-disubstituted phenyl) salicylamide derivatives
A compound represented by the following formula (I) or a salt thereof: wherein R1, R2, R3 and R4 represent hydrogen atom, a halogen atom, cyano group, nitro group, a C1-4 alkyl group, a halogenated C
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Page/Page column 44

(2008/12/07)

IMIDAZOQUINOLINES AS LIPID KINASE INHIBITORS
The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment of an inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease.
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Page/Page column 66

(2008/06/13)

2-AMINO-4-HYDROXY-5-PYRIMIDINECARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF T CELL ACTIVATION FOR THE TREATMENT OF INFLAMMATORY DISEASES
The present invention relates to pyrimidine or pyridine carboxamides or pharmaceutically-acceptable salts thereof. Also included is a method of treatment of inflammation, inhibition of T cell activation and proliferation, arthritis, rheumatoid arthritis,
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Page/Page column 72

(2008/06/13)

2-AMINOPYRIMIDINE AND 2-AMINOPYRIDINE-4-CARBAMATES FOR USE IN THE TREATMENT OF AUTOIMMUNE DISEASES
The present invention relates to pyrimidine or pyridine carbamate compounds having the general Formula (1) and pharmaceutically acceptable salts or derivatives thereof. Also included are methods of treatment of various diseases and conditions, including inflammation, inhibition of T cell activation and proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, the methods comprising administering a therapeutically-effective amount a compound of Formula I, or a salt or derivative form thereof, as described above.
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Page 83

(2010/02/10)

SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
The present invention relates to tetracyclic pyrimidines or pyridines or pharmaceutically-acceptable salts or derivatives thereof. Also included are methods of use of the tetracyclic pyrimidines or pyridines including use related to treating inflammation,
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Page/Page column 79

(2010/02/11)

SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
The present invention relates to hydroxybenzimidazole pyrimidines or pyridines or pharmaceutically-acceptable salts thereof. Also included is a method of treatment of inflammation, inhibition of T cell activation and proliferation, arthritis, rheumatoid arthritis, psoriatic arthritis, osteoarthritis, organ transplant, acute transplant or heterograft or homograft rejection, transplantation tolerance induction, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, including ulcerative colitis, Crohn's disease, lupus, contact hypersensitivity, delayed-type hypersensitivity, and gluten-sensitive enteropathy, type 1 diabetes, psoriasis, contact dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, glomerulonephritis, serum sickness, uticaria, allergic diseases, asthma, hayfever, allergic rhinitis, scleracielma, mycosis fungoides, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet's disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary's syndrome, atopic dermatitis, systemic schlerosis, morphea, atopic dermatitis, colon carcinoma or thymoma in a mammal comprising administering a therapeutically-effective amount a compound as described above.
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Page/Page column 83

(2010/02/11)

Chemical Properties

Appearance/Colour :Kind of white to yellow powder
Melting Point: 141 °C
Boiling Point: 382.135 °C at 760 mmHg
Flash Point:184.909 °C
Density: 1.207 g/cm³
Vapor Pressure: 4.83E-06mmHg at 25°C
Refractive Index: 1.598
PKA: 7.54±0.42(Predicted)
PSA: 32.50000
LogP: 2.25810

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16154-72-6

Articles about 16154-72-6Total 12 be found

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Chemical Properties

Appearance/Colour :Kind of white to yellow powder

Melting Point: 141 °C

Boiling Point: 382.135 °C at 760 mmHg

Flash Point:184.909 °C

Density: 1.207 g/cm³

Vapor Pressure: 4.83E-06mmHg at 25°C

Refractive Index: 1.598

PKA: 7.54±0.42(Predicted)

PSA: 32.50000

LogP: 2.25810

Global suppliers and manufacturers of 16154-72-6total 37 suppliers on LookChem

Article Database

16154-72-6

Articles about 16154-72-6Total 12 be found

More Articles about upstream products of 16154-72-6

More Articles about downstream products of 16154-72-6

Chemical Properties

Appearance/Colour :Kind of white to yellow powder

Melting Point: 141 °C

Boiling Point: 382.135 °C at 760 mmHg

Flash Point:184.909 °C

Density: 1.207 g/cm3

Vapor Pressure: 4.83E-06mmHg at 25°C

Refractive Index: 1.598

PKA: 7.54±0.42(Predicted)

PSA: 32.50000

LogP: 2.25810

Global suppliers and manufacturers of 16154-72-6total 37 suppliers on LookChem

Density: 1.207 g/cm³