135380-50-6Relevant academic research and scientific papers
LIPID COMPOUNDS AND LIPID NANOPARTICLE COMPOSITIONS
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Paragraph 00332-00333, (2022/01/12)
Provided herein are lipid compounds that can be used in combination with other lipid components, such as neutral lipids, cholesterol and polymer conjugated lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes, including vaccination. Also provided herein are lipid nanoparticle compositions comprising said lipids.
NOVEL COMPOUNDS
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Page/Page column 323; 328, (2019/11/19)
The present invention relates to substituted 5-membered nitrogen containing heteroaryl compounds, such as sulfonyl triazoles, where the heteroaryl ring is further substituted, optionally via a linking group such as -NH-, with a cyclic group which in turn is substituted at the α-position. The present invention further relates to associated salts, solvates, prodrugs and pharmaceutical compositions, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3 inhibition.
SUBSTITUTED NUCLEOSIDE ANALOGUES FOR USE AS PRMT5 INHIBITORS
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Page/Page column 132, (2017/09/27)
The present invention relates novel substituted nucleoside analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
THIENOPYRIMIDIENE DERIVATIVES AS PI3K INHIBITORS
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Page/Page column 81-82, (2009/05/28)
Thienopyrimidines of formula (I) wherein W and R1 to R4 are as defined in the claims, and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PI3 kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
PHARMACEUTICAL COMPOUNDS
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Page/Page column 47-48, (2009/01/24)
Furanopyrimidines of formula (I): wherein W represents a furan ring; R1 and R2 form, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is selected from: (a) a 4- to 7-membered saturated N-containing heterocyclic ring which includes 0 or 1 additional heteroatoms selected from N, S and O, the ring being fused to a second ring selected from a 4- to 7-membered saturated N-containing heterocyclic ring as defined above, a 5- to 12-membered unsaturated heterocyclic ring, a 5- to 7-membered saturated O-containing heterocyclic ring, a 3- to 12- membered saturated carbocyclic ring and an unsaturated 5- to 12- membered carbocyclic ring to form a heteropolycyclic ring system, the heteropolycyclic ring system being unsubstituted or substituted; (b) a 4- to 7-membered saturated N-containing heterocyclic ring which includes 0 or 1 additional heteroatoms selected from N, S and O and which further comprises, linking two constituent atoms of the ring, a bridgehead group selected from -(CR'2)n- and -(CR'2)r-O-(CR'2)s- wherein each R' is independently H or C1 - C6 alkyl, n is 1, 2 or 3, r is 0 or 1 and s is 0 or 1, the remaining ring positions being unsubstituted or substituted; and (c) a group of formula (IIb): wherein ring B is a 4- to 7-membered saturated N-containing heterocyclic ring which includes 0 or 1 additional heteroatoms selected from N, S and O and ring B' is a 3- to 12- membered saturated carbocyclic ring, a 5- to 7- membered saturated O-containing heterocyclic ring or a 4- to 7-membered saturated N-containing heterocyclic ring as defined above, each of B and B' being unsubstituted or substituted; m is 0, 1 or 2; R3 is H or C1-C6 alkyl; R4 is an indole group which is unsubstituted or substituted; and Ra is selected from R, halo, CN, C(O)NR2, halo(C1-C6)alkyl, SO2R, SO2NR2, NRSO2R, NRC(O)R, NRC(O)OR and NRC(O)NR2 wherein each R is independently H or C1-C6 alkyl; and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PI3 kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
A NOVEL SYNTHESIS OF 3,3-(SPIRO)SUBSTITUTED AZETIDINES
Froehlich, Johannes,Sauter, Fritz,Blasl, Karin
, p. 1879 - 1892 (2007/10/02)
A smooth and efficient new synthesis for 3,3-disubstituted azetidines, starting from readily available nitriles, was estabilished: α-hydroxymethylation of the starting materials, followed by O-tosylation and LiAlH4-reduction of the key intermediates thus obtained, led - via spontaneous cyclization of the intermediate amino derivatives - to 3,3-disubstituted azetidines.Scope and limitations of this new method were studied with respect to generalized applicability: the target compounds were accessible in good yields for a variety of starting materials (cyclic and acyclic di(hetero)aryl, (hetero)arylalkyl, dialkyl, as well as basic moieties).The products thus obtained may be of interest for ensuing conversions due to their unblocked nitrogen.
