- INDAZOLES AND AZAINDAZOLES AS LRRK2 INHIBITORS
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The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.
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Page/Page column 89-90; 120-121
(2021/09/11)
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- A is ATP competitive small molecule AKT inhibitor A443654 synthetic method
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The invention discloses a synthesis method of an ATP competitive small-molecule AKT inhibitor A443654. According to the method, a compound 1 is used as a starting raw material, and the compound 6 (A-443654) is obtained through amino group protection, Suzuki reaction and protecting group removal. Usage of poisonous reagent hexamethylditin is avoided, the method is high in safety, environment-friendly, high in reaction yield and suitable for industrial large-scale production, the reaction time is shortened, and the process cost is reduced. The flow chart of the synthesis method is shown in the specification.
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- Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer
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A novel series of pyridin-3-amine derivatives were designed, synthesized, and evaluated as multitargeted protein kinase inhibitors for the treatment of non-small cell lung cancer (NSCLC). Hit 1 was first disclosed by in silico screening against fibroblast
- Zhu, Wei,Chen, Hui,Wang, Yulan,Wang, Jiang,Peng, Xia,Chen, Xianjie,Gao, Yinglei,Li, Chunpu,He, Yulong,Ai, Jing,Geng, Meiyu,Zheng, Mingyue,Liu, Hong
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p. 6018 - 6035
(2017/08/02)
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- FUSED HETEROCYCLIC COMPOUNDS FOR USE IN THE TREATMENT OF MALARIA
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A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R1 is -NR3R4 or -OR5; R2 is selected from aryl, heteroaryl, fused aryl- heterocycloalkyl and fused heteroaryl-heterocycloalkyl each of which may be optionally substituted by one or more R8 groups; R3 is H or alkyl; R4 is: (i) cycloalkyl optionally substituted by one or more -NR11R12, -NHCO2R11, -NHCOR11 and -NHSO2R11 groups; or (ii) -(CH2)n-heterocycloalkyl, wherein said heterocycloalkyl is a 4, 5 or 6-membered nitrogen-containing group optionally containing one or more CO groups, wherein said heterocycloalkyl is optionally substituted by one or more one or more (CH2)nR7 groups; (iii) -(CH2)n-heteroaryl, wherein said heteroaryl group is optionally substituted by one or more R7 groups; or (iv) alkyl substituted by one or more -NR11R12groups; or R3 and R4 are linked together with the nitrogen to which they are attached to form a 4, 5 or 6-membered heterocycloalkyl group optionally containing one or two further groups selected from CO, O, N and S, and which is optionally further substituted by one or more R7 groups; R5 is selected from alkyl, -(CH2)n-heteroaryl and -(CH2)n-heterocycloalkyl, wherein said heteroaryl and heterocycloalkyl groups are each optionally substituted by one or more R7 groups; each R11 and R12 is independently H or alkyl; and each n is independently an integer from O to 6; for use in treating or preventing a disorder associated with CDPK. Further aspects relate to the use of said compounds in the treatment of various therapeutic disorders, and more particularly as inhibitors of PfCDPK1.
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Page/Page column 121
(2011/09/19)
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- 2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity
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2,3,5-Trisubstituted pyridines have been designed as potent AKT inhibitors that are selective against ROCK1 based on the comparison between AKT and ROCK1 structures. Substitution at the 2-position of the core pyridine is the key element to provide selectivity against ROCK1. An X-ray co-crystal structure of 9p in PKA supports the proposed rationale of ROCK1 selectivity.
- Lin, Hong,Yamashita, Dennis S.,Zeng, Jin,Xie, Ren,Wang, Wenyong,Nidarmarthy, Sirishkumar,Luengo, Juan I.,Rhodes, Nelson,Knick, Victoria B.,Choudhry, Anthony E.,Lai, Zhihong,Minthorn, Elisabeth A.,Strum, Susan L.,Wood, Edgar R.,Elkins, Patricia A.,Concha, Nestor O.,Heerding, Dirk A.
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body text
p. 673 - 678
(2010/07/05)
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- 6-AMINOIMIDAZO[1,2-b]PYRIDAZINE ANALOGS AS RHO KINASE INHIBITORS FOR THE TREATMENT OF RHO KINASE-MEDIATED DISEASES AND CONDITIONS
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Methods for using 6-aminoimidazo[1,2-b]pyridazine analogs are disclosed herein to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of 6-aminoimidazo[1,2-b]pyridazine analogs, are disclosed herein.
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Page/Page column 24
(2008/12/06)
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- INHIBITORS OF AKT ACTIVITY
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Invented are novel pyridine compounds, the use of such compounds as inhibitors of PKB/AKT kinase activity and in the treatment of cancer and arthritis.
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Page/Page column 37; 76
(2010/02/14)
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