Patent classifications
C07D319/06
Processes and intermediates for preparing MCL1 inhibitors
The present disclosure provides methods for preparing MCL1 inhibitors or a salt thereof and related key intermediates.
Processes and intermediates for preparing MCL1 inhibitors
The present disclosure provides methods for preparing MCL1 inhibitors or a salt thereof and related key intermediates.
NOVEL AMINO ACID DERIVATIVES
- Naoki OKADA ,
- Kyosuke UEDA ,
- Masatoshi TAKUWA ,
- Shunichi NAKANO ,
- Kotaro TOKUMOTO ,
- Tomoko ASHIZAWA ,
- Shuhei YAMAKOSHI ,
- Yutaka KOBAYASHI ,
- Katsuma MATSUI ,
- Ayumu MATSUDA ,
- Masatoshi MATSUMOTO ,
- Keiichi MASUYA ,
- Atsushi YOSHIZAWA ,
- Masahiko KINEBUCHI ,
- Takeru EHARA ,
- Masami YAMADA ,
- Kouki MORIMOTO ,
- Yoshihide MIZUKOSHI ,
- Haruaki KURASAKI ,
- Motoki MURAI ,
- Kentarou FUKUMOTO ,
- Douglas Robert CARY
A novel amino acid derivative is provided, wherein the amino acid derivative is expected to improve solubility of polypeptides comprising the derivative therein.
Compound used as autophagy regulator, and preparation method therefor and uses thereof
It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators. ##STR00001##
POLYMERISABLE COMPOUNDS AND THE USE THEREOF IN LIQUID-CRYSTAL DISPLAYS
The present invention relates to polymerisable compounds, to processes and intermediates for the preparation thereof, to liquid-crystal (LC) media comprising them, and to the use of the polymerisable compounds and LC media for optical, electro-optical and electronic purposes, in particular in LC displays, especially in LC displays of the polymer sustained alignment (PS, PSA) and self-aligning (SA) type.
POLYMERISABLE COMPOUNDS AND THE USE THEREOF IN LIQUID-CRYSTAL DISPLAYS
The present invention relates to polymerisable compounds, to processes and intermediates for the preparation thereof, to liquid-crystal (LC) media comprising them, and to the use of the polymerisable compounds and LC media for optical, electro-optical and electronic purposes, in particular in LC displays, especially in LC displays of the polymer sustained alignment (PS, PSA) and self-aligning (SA) type.
Lipids and compositions for the delivery of therapeutics
The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention formula (I) provides lipids having the following structure XXXIII wherein: R.sub.1 and R.sub.2 are each independently for each occurrence optionally substituted C.sub.10-C.sub.30 alkyl, optionally substituted C.sub.10-C.sub.30 alkenyl, optionally substituted C.sub.10-C.sub.30 alkynyl, optionally substituted C.sub.10-C.sub.30 acyl, or -linker-ligand; R.sub.3 is H, optionally substituted C.sub.1-C.sub.10 alkyl, optionally substituted C.sub.2-C.sub.10 alkenyl, optionally substituted C.sub.2-C.sub.10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O). ##STR00001##
Lipids and compositions for the delivery of therapeutics
The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention formula (I) provides lipids having the following structure XXXIII wherein: R.sub.1 and R.sub.2 are each independently for each occurrence optionally substituted C.sub.10-C.sub.30 alkyl, optionally substituted C.sub.10-C.sub.30 alkenyl, optionally substituted C.sub.10-C.sub.30 alkynyl, optionally substituted C.sub.10-C.sub.30 acyl, or -linker-ligand; R.sub.3 is H, optionally substituted C.sub.1-C.sub.10 alkyl, optionally substituted C.sub.2-C.sub.10 alkenyl, optionally substituted C.sub.2-C.sub.10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O). ##STR00001##
Polymerizable compound, and liquid crystal composition and liquid crystal display element in which the compound is used
The compound is represented by general formula (i). In the compound, in a group K.sup.i1, at least two secondary carbon atoms in an alkyl group (a linear alkyl, halogenated alkyl, or cyanogenated alkyl group having 3 to 40 carbon atoms) are replaced with —C(═X.sup.i1)— and/or —CH(—CN)—, where X.sup.i1 is an oxygen atom, a sulfur atom, NH, or NR.sup.13; in addition, a group A.sup.i2, a group A.sup.i3, or the group K.sup.i1 includes, as a substituent, at least one P.sup.i1-Sp.sup.i1- group, where P.sup.i1 is a polymerizable group, and SP.sup.i1 is a spacer group or a single bond. The liquid crystal composition including the compound represented by general formula (i) can be adsorbed onto substrates between which a liquid crystal layer is held, and, consequently, without the use of an alignment film, liquid crystal molecules can be maintained in a state in which the liquid crystal molecules are aligned in a vertical direction. ##STR00001##
Polymerizable compound, and liquid crystal composition and liquid crystal display element in which the compound is used
The compound is represented by general formula (i). In the compound, in a group K.sup.i1, at least two secondary carbon atoms in an alkyl group (a linear alkyl, halogenated alkyl, or cyanogenated alkyl group having 3 to 40 carbon atoms) are replaced with —C(═X.sup.i1)— and/or —CH(—CN)—, where X.sup.i1 is an oxygen atom, a sulfur atom, NH, or NR.sup.13; in addition, a group A.sup.i2, a group A.sup.i3, or the group K.sup.i1 includes, as a substituent, at least one P.sup.i1-Sp.sup.i1- group, where P.sup.i1 is a polymerizable group, and SP.sup.i1 is a spacer group or a single bond. The liquid crystal composition including the compound represented by general formula (i) can be adsorbed onto substrates between which a liquid crystal layer is held, and, consequently, without the use of an alignment film, liquid crystal molecules can be maintained in a state in which the liquid crystal molecules are aligned in a vertical direction. ##STR00001##