- METTL3 INHIBITORY COMPOUNDS
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The present invention relates to compounds of formula (I) that function as inhibitors of METTL3 (N6-adenosine-methyltransferase 70 kDa subunit) enzyme activity: X-Y-Z5 (I) wherein X, Y and Z are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, and autoimmune diseases, as well as other diseases or conditions in which METTL3 activity 10 is implicated.
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Paragraph 00872; 00894-00895
(2020/10/20)
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- Discovery of imidazopyridine derivatives as highly potent respiratory syncytial virus fusion inhibitors
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A series of imidazolepyridine derivatives were designed and synthesized according to the established docking studies. The imidazopyridine derivatives were found to have good potency and physical-chemical properties. Several highly potent compounds such as 8ji, 8jl, and 8jm were identified with single nanomolar activities. The most potent compound 8jm showed an IC50 of 3 nM, lower microsome clearance and no CYP inhibition. The profile of 8jm appeared to be superior to BMS433771, and supported further optimization.
- Feng, Song,Hong, Di,Wang, Baoxia,Zheng, Xiufang,Miao, Kun,Wang, Lisha,Yun, Hongying,Gao, Lu,Zhao, Shuhai,Shen, Hong C.
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supporting information
p. 359 - 362
(2015/03/30)
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- GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
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Paragraph 000821
(2015/04/15)
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- HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
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Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.
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Page/Page column 49
(2012/07/27)
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- METHYL SULFANYL PYRMIDMES USEFUL AS ANTIINFLAMMATORIES, ANALGESICS, AND ANTIEPILEPTICS
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The present invention relates to pyrimidine derivatives of Formula (Ia) and (Ib) (including tautomers, isomers, prodrugs, and pharmaceutically acceptable salts thereof). Said compounds are useful in the treatment of pain (such as neuropathic pain), inflammation, and epilepsy (by acting as anticonvulsants). Methods of medical treatment making use of said compounds, as well as additional compounds of Formula (IIa) and (IIb), are also disclosed.
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Page/Page column 133
(2010/12/18)
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- HYPOXIA ACTIVATED DRUGS OF NITROGEN MUSTARD ALKYLATORS
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Hypoxia activated drug compounds having a structure of formula(I) are useful in the treatment of cancer and other hyperproliferative diseases.
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- CHEMICAL COMPOUNDS
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The present invention provides compounds of formula (I) including salts, solvates, and pharmaceutically acceptable derivatives thereof, pharmaceutical formulations containing them, processes for their preparation, and methods of treatment using them.
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Page/Page column 46-47
(2010/11/28)
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- AMIDE DERIVATIVES BEARING A CYCLOPROPYLAMINOACARBONYL SUBSTITUENT USEFUL AS CYTO KINE INHIBITORS
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The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are each hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by cytokines.
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Page/Page column 62
(2010/02/12)
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- Heterocyclic compounds having anti-diabetic activity and their use
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Compounds of formula (I): STR1 [wherein: X represents an unsubstituted or substituted indolyl, indolinyl, azaindolyl, azaindolinyl, imidazopyridyl or imidazopyrimidinyl group; Y represents an oxygen or sulfur atom; Z represents a 2,4-dioxothiazolidin-5-ylidenylmethyl, 2,4-dioxothiazolidin-5-ylmethyl, 2,4-dioxooxazolidin-5-ylmethyl, 3,5-dioxooxadiazolidin-2-ylmethyl or N-hydroxyureidomethyl group; R represents a hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, a hydroxy group, a nitro group, an aralkyl group or a unsubstituted or substituted amino group; and m is an integer of from 1 to 5] have hypoglycemic and anti-diabetic activities.
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- N-MYRISTOYL TRANSFERASE INHIBITORS
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The invention relates to a compound of formula (I): which can be used as N-myristoyltransferase inhibitors, in which R1 represents hydrogen, substituted or unsubstituted (C1-C6) alkyl, substituted or unsubstituted phenyl, (C3-C7) cycloalkyl methyl, substituted or unsubstituted (imidazolyl-2-yl)methyl, substituted or unsubstituted (indol-3-yl)methyl or (1-azaindolizin-2-yl)methyl, R2, R3, which are identical or different, represent hydrogen or (C1-C6) alkyl, or when R1 represents hydrogen, R2 and R3 form with the carbon and nitrogen atoms to which they are attached, a mono-, bi- or tricyclic heterocycle, X represents -CO-, -SO2-, -PO(OH)-, Y represents -COR5 or --POR6R6', R4 represents substituted or unsubstituted, linear or branched (C6 -C21) alkyl in which, depending on the individual case, one or more methylene may be replaced by oxygen or sulfur or by a p-phenylene ring, their isomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid or base.
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- Benzimidazoles, process for their preparation and preparations containing same
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Novel compounds of the formula pharmaceutical compositions containing such compounds as active ingredient, and the use of the compounds in medicine.
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