633327-22-7Relevant articles and documents
Liquid crystal compound containing dibenzothipheno oxygen-containing heterocycles and application thereof featuring high dielectric constant, high clearing point, high refractive index, high K value, etc., and suitable for displays used in VA, ECB, PALC, FFS or IPS mode
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Paragraph 0043-0048, (2021/09/22)
The present invention belongs to the field of liquid crystal compound materials, and relates to a liquid crystal compound containing dibenzothieno oxygen-containing heterocycles and its applications. The chemical structural formula is shown as the following formula I. The liquid crystal compound provided by the present invention and the liquid crystal composition containing the compound have the properties of high dielectric constant, high clearing point, high refractive index, high K value, etc., and is suitable for displays used in VA, ECB, PALC, FFS or IPS mode.
POTENT HUMAN NEURONAL NITRIC OXIDE SYNTHASE INHIBITORS
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Paragraph 00370, (2021/09/04)
Disclosed are 2-aminopyridine derivative compounds for use as inhibitors of nitric oxide synthase (NOS). In particular, the field of the invention relates to 2-aminopyridine derivative compounds for use as inhibitors of neuronal nitric oxide synthase (nNOS), which are formulated as pharmaceutical compositions for treating diseases and disorders associated with nNOS such as Alzheimer's, Parkinson's, and Huntington's diseases, and amytrophic lateral sclerosis, cerebral palsy, stroke/ischemic brain damage, and migraine headaches.
Cyclic aminopyrimidine derivative and activity and application thereof for inhibiting kinase (by machine translation)
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Paragraph 0078; 0086-0088, (2020/07/02)
The cyclic aminopyrimidine derivative has the structure of a general formula (I), a pharmaceutically acceptable salt, ester or solvate thereof, can inhibit the activity of kinases, is a plurality of kinase inhibitors, can be widely applied to treatment of cancers, and has a huge clinical application prospect. General Formula (I). (by machine translation)
Compounds and their use in treatment on hepatitis B
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Paragraph 0119-0121, (2020/07/15)
The invention provides compounds, a pharmaceutical composition containing the compounds and an application of the compounds. The compound is a compound shown in a formula (I) or a stereoisomer, a tautomer, nitric oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug of the compound shown in the formula (I). The compound provided by the invention can interfere with the shell assembly process of hepatitis B virus, thereby inhibiting hepatitis B virus replication. Moreover, the compound has good absorption, relatively high biological activity and availability and low toxicity, particularly has relatively strong stability in vivo, is not easy to decompose and has long drug effect time, so that an effect of treating hepatitis B is achieved and the compound has a goodapplication prospect.
Optimization of Blood-Brain Barrier Permeability with Potent and Selective Human Neuronal Nitric Oxide Synthase Inhibitors Having a 2-Aminopyridine Scaffold
Do, Ha T.,Li, Huiying,Chreifi, Georges,Poulos, Thomas L.,Silverman, Richard B.
supporting information, p. 2690 - 2707 (2019/03/11)
Effective delivery of therapeutic drugs into the human brain is one of the most challenging tasks in central nervous system drug development because of the blood-brain barrier (BBB). To overcome the BBB, both passive permeability and efflux transporter liability of a compound must be addressed. Herein, we report our optimization related to BBB penetration of neuronal nitric oxide synthase (nNOS) inhibitors toward the development of new drugs for neurodegenerative diseases. Various approaches, including enhancing lipophilicity and rigidity of new inhibitors and modulating the pKa of amino groups, have been employed. In addition to determining inhibitor potency and selectivity, crystal structures of most newly designed compounds complexed to various nitric oxide synthase isoforms have been determined. We have discovered a new analogue (21), which exhibits not only excellent potency (Ki 30 nM) in nNOS inhibition but also a significantly low P-glycoprotein and breast-cancer-resistant protein substrate liability as indicated by an efflux ratio of 0.8 in the Caco-2 bidirectional assay.
AMINO PYRIMIDINE COMPOUND FOR INHIBITING PROTEIN TYROSINE KINASE ACTIVITY
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Paragraph 0397; 0398, (2019/06/07)
An amino pyrimidine compound for inhibiting protein tyrosine kinase activity, a pharmaceutical composition thereof, preparation therefor, and an application thereof. Specifically, an amino pyrimidine compound represented by formula (I), R1, R2, L, Y, R6, W, A, m, and n being defined in the specification, and a pharmaceutically acceptable salt, a stereoisomer, a solvent compound, a hydrate, a polymorphism, a prodrug, or an isotope variant thereof. The compound can be used for treating and/or preventing protein tyrosine kinase-related diseases such as cell proliferative diseases, cancers, and immune diseases.
SUBSTITUTED 2-HYDROGEN-PYRAZOLE DERIVATIVE SERVING AS ANTICANCER DRUG
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Paragraph 0272; 0273; 0274, (2018/02/04)
Disclosed is a substituted 2H-pyrazole derivative serving as a selective CDK4/6 inhibitor. Specifically, disclosed is a compound of formula (I) or a pharmaceutically acceptable salt thereof which serves as a selective CDK4/6 inhibitor.
Amino pyrimidine compound and preparation method and application thereof
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Paragraph 0615; 0618; 0619; 0620, (2018/11/22)
The invention relates to an amino pyrimidine compound and a preparation method and application thereof. The amino pyrimidine compound has a structure as shown in a formula I. The formula is shown in the description. The compound is an inhibitor of an epidermal growth factor receptor (EGFR) kinase. The invention further relates to a medicine composition comprising the compound, a preparation methodand application thereof in preparation of anti-tumor medicines.
3-(1H-PYRROLO[2,3-B]PYRIDIN-2-YL)-1H-INDAZOLES AND THERAPEUTIC USES THEREOF
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Paragraph 0616; 0617, (2017/02/28)
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
3-(1H-PYRROLO[2,3-C]PYRIDIN-2-YL)-1H-INDAZOLES AND THERAPEUTIC USES THEREOF
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Paragraph 0616; 0617, (2017/03/08)
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.