25600-25-3Relevant academic research and scientific papers
BENZIMIDAZOLONE DERIVED INHIBITORS OF BCL6
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Paragraph 00367, (2018/12/13)
The present invention relates to compounds of Formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: wherein X1, X2, R1, R2 and R3 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, as well as other diseases or conditions in which BCL6 activity is implicated.
NOVEL PYRAZOLO PYRIMIDINE DERIVATIVES AND THEIR USE AS MALT1 INHIBITORS
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Page/Page column 43, (2015/12/31)
The present invention describes new pyrazolo-pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein, R1 is halogen, cyano, or C1-C3alkyl optionally substituted by halogen; R2 is C1-C6alkyl optionally substituted one or more times by C1-C6alkyl, C2-C6alkenyl, hydroxyl, N,N-di-C1-C6alkyl amino, N-mono-C1-C6alkyl amino, O-Rg, Rg, phenyl, or by C1-C6alkoxy wherein said alkoxy again may optionally be substituted by C1-C6alkoxy, N,N-di-C1-C6alkyl amino, Rg or phenyl; C3-C6cycloalkyl optionally substituted by C1-C6alkyl, N,N-di-C1-C6alkyl amino or C1-C6alkoxy-C1-C6alkyl, and/or two of said optional substituents together with the atoms to which they are bound may form an annulated or spirocyclic 4 - 6 membered saturated heterocyclic ring comprising 1 - 2 O atoms; phenyl optionally substituted by C1-C6alkoxy; a 5 - 6 membered heteroaryl ring having 1 to 3 heteroatoms selected from N and O said ring being optionally substituted by C1-C6alkyl which may be optionally substituted by amino or hydroxy; Rg; or N,N-di-C1-C6alkyl amino carbonyl; and R is phenyl independently substituted two or more times by Ra, 2-pyridyl independently substituted one or more times by Rb, 3-pyridyl independently substituted one or more times by Rc, or 4-pyridyl independently substituted one or more times by Rd; which are generally interacting with MALT1 proteolytic and/or autoproteolytic activity, and in particular which may inhibit said activity. The present invention further describes the synthesis of said new pyrazolo-pyrimidine derivatives, their use as a medicament, especially by interacting with MALT1 proteolytic and/or autoproteolytic activity.
Process for treating homoserin compounds
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Paragraph 0144-0146, (2017/01/02)
The present invention relates to the preparation of a useful compound which can be used as an intermediate product for preparing an important compound in the industrial field from a homoserine-based compound and provides a process for treating a homoserine-based compound, capable of simply mass producing a useful compound from a homoserine-based compound with excellent efficiency.(AA) Homoserine-based compound(BB) Product(CC) GBL derivative(DD) Halo-GBL(EE, FF, GG) GBL puranone(HH) Puranone(II) Dialkyl succinate(JJ) Step 1(KK) Step 2(LL) Step 3(MM) Step 4(NN) Step 5(OO) Step 6(PP) Step 7COPYRIGHT KIPO 2016
(-)-Echinobetaine A: Isolation, structure elucidation, synthesis, and SAR studies on a new nematocide from a Southern Australian marine sponge, Echinodictyum sp.
Capon, Robert J.,Vuong, Dat,Lacey, Ernest,Gill, Jennifer H.
, p. 179 - 182 (2008/09/18)
A nematocidal agent present in a southern Australian marine sponge of the genus Echinodictyum has been isolated and identified by detailed spectroscopic analysis and total synthesis as the novel betaine (-)-echinobetaine A (6). Preliminary SAR investigations have been undertaken.
