C07C239/14

Affinity illudofulvene conjugates
11591295 · 2023-02-28 · ·

In an embodiment of the invention, a composition for treating a cell population comprises a medicant. The medicant moiety can be an illudofulvene analog. In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The affinity moiety can be an antibody, an antibody fragment, a receptor protein, a peptidic growth factor, an anti-angiogenic protein, a specific binding peptide, protease cleavable peptide, a glycopeptide, a peptide, a peptidic toxin, a protein toxin and an oligonucleotide. The affinity moiety can be covalently bound to the medicant via a linker.

AFFINITY ILLUDOFULVENE CONJUGATES
20230212113 · 2023-07-06 · ·

In an embodiment of the invention, a composition for treating a cell population comprises a medicant. The medicant moiety can be an illudofulvene analog. In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The affinity moiety can be an antibody, an antibody fragment, a receptor protein, a peptidic growth factor, an anti-angiogenic protein, a specific binding peptide, protease cleavable peptide, a glycopeptide, a peptide, a peptidic toxin, a protein toxin and an oligonucleotide. The affinity moiety can be covalently bound to the medicant via a linker.

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##

Hypocrellin derivative substituted both in a peri-position and in 2-position by amino, preparation method, and application thereof

The present invention discloses a hypocrellin derivative substituted both in a pen-position and in a 2-position by an amino, and a preparation method and use thereof. A general structural formula of the derivative is as represented by formulas I-a to I-d: ##STR00001## The hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino prepared in the present invention has a maximum absorption wavelength of 600-650 nm and a molar extinction coefficient reaching about 20000-40000 M.sup.−1cm.sup.−1. Compared with unmodified hypocrellin or hypocrellin having only a 2-position modified, an absorption spectrum of the derivative is significantly red-shifted and the molar extinction coefficient is greatly improved, and the derivative can efficiently produce reactive oxygen species such as singlet oxygen in a photosensitive condition. In the same condition, the hypocrellin derivative substituted both in a pen-position and in a 2-position by an amino involved in the present invention, when used as a photosensitizer, has a stronger ability to photo-dynamically inactivate tumor cells than the first and second generation commercial photosensitizers.

Monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and preparation method and application thereof

The invention discloses a monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and a preparation method and application thereof. The amphiphilic hypocrellin derivative substituted by a group containing PEG, a quaternary ammonium salt or the like prepared according to the invention has an obvious red shift in its absorption spectrum and a significantly enhanced molar extinction coefficient, compared with the parent hypocrellin, can efficiently produce singlet state oxygen and other reactive oxygen species under photosensitive conditions; has different amphiphilicities and increased biocompatibility with cells or tissues by regulating its hydrophilicity and hydrophobicity; can meet the requirements of different clinical drugs, and solves the requirements of different drug delivery methods for different drug hydrophilicity and lipophilicity. Under identical conditions, the amphiphilic hypocrellin derivative photosensitizer according to the invention has higher ability to photodynamically inactivate tumor cells than the first and second generation commercial photosensitizers.

Monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and preparation method and application thereof

The invention discloses a monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and a preparation method and application thereof. The amphiphilic hypocrellin derivative substituted by a group containing PEG, a quaternary ammonium salt or the like prepared according to the invention has an obvious red shift in its absorption spectrum and a significantly enhanced molar extinction coefficient, compared with the parent hypocrellin, can efficiently produce singlet state oxygen and other reactive oxygen species under photosensitive conditions; has different amphiphilicities and increased biocompatibility with cells or tissues by regulating its hydrophilicity and hydrophobicity; can meet the requirements of different clinical drugs, and solves the requirements of different drug delivery methods for different drug hydrophilicity and lipophilicity. Under identical conditions, the amphiphilic hypocrellin derivative photosensitizer according to the invention has higher ability to photodynamically inactivate tumor cells than the first and second generation commercial photosensitizers.

HYPOCRELLIN DERIVATIVE SUBSTITUTED BOTH IN A PERI-POSITION AND IN 2-POSITION BY AMINO, PREPARATION METHOD, AND APPLICATION THEREOF

The present invention discloses a hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino, and a preparation method and use thereof. A general structural formula of the derivative is as represented by formulas I-a to I-d:

##STR00001##

The hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino prepared in the present invention has a maximum absorption wavelength of 600-650 nm and a molar extinction coefficient reaching about 20000-40000 M.sup.−1cm.sup.−1. Compared with unmodified hypocrellin or hypocrellin having only a 2-position modified, an absorption spectrum of the derivative is significantly red-shifted and the molar extinction coefficient is greatly improved, and the derivative can efficiently produce reactive oxygen species such as singlet oxygen in a photosensitive condition. In the same condition, the hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino involved in the present invention, when used as a photosensitizer, has a stronger ability to photo-dynamically inactivate tumor cells than the first and second generation commercial photosensitizers.

AFFINITY ILLUDOFULVENE CONJUGATES
20210155583 · 2021-05-27 · ·

In an embodiment of the invention, a composition for treating a cell population comprises a medicant. The medicant moiety can be an illudofulvene analog. In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The affinity moiety can be an antibody, an antibody fragment, a receptor protein, a peptidic growth factor, an anti-angiogenic protein, a specific binding peptide, protease cleavable peptide, a glycopeptide, a peptide, a peptidic toxin, a protein toxin and an oligonucleotide. The affinity moiety can be covalently bound to the medicant via a linker.

Regulators for controlling linear and pseudo-ring expansion polymerization of vinyl monomers

New regulator compounds for a novel polymerization process for vinyl monomers, which yields polymers with improved control over composition and nearly full to full conservation of architectural integrity up to high conversion. The regulator compounds are defined by according to anyone of the Formulas 1A, 1B, 1C, 1D, 1E, 1F, 1G, 1H and 1I: ##STR00001## wherein R.sup.1 stands for an optionally substituted secondary or tertiary alkyl or secondary or tertiary aralkyl; Z.sup.1 stands for CN or a carboxylic acid ester of formula C(O)OR.sup.21; Z.sup.2 may be chosen from the group of CN, carboxylic acid, salts of carboxylic acids, carboxylic acid ester, carboxylic acid amides, (hetero)aryl, alkenyl and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently chosen from the group of H, alkyl, aralkyl, (hetero)aryl, CN and carboxylic acid ester of formula C(O)OR.sup.22; R.sup.7 stands for a primary alkyl or primary aralkyl, CN or hydrogen; Y stands for a bridging group and n is 2, 3, 4, 5 or 6; in case R.sup.1 stands for tertiary alkyl or tertiary aralkyl, R.sup.6 stands for a primary alkyl or primary aralkyl, CN or a carboxylic acid ester of formula C(O)OR.sup.26; in case R.sup.1 stands for a secondary alkyl or secondary aralkyl, R.sup.6 stands for a primary or secondary alkyl or primary or secondary aralkyl, CN, a carboxylic acid ester of formula C(O)OR.sup.26 or a phosphonic acid ester of formula P(O)(OR.sup.27).sub.2, a (hetero)aryl or an alkenyl; R.sup.21, R.sup.22, R.sup.26 and R.sup.27 each independently stand for alkyl or aralkyl having from 1-30 carbon atoms, optionally containing heteroatoms.

Regulators for controlling linear and pseudo-ring expansion polymerization of vinyl monomers

New regulator compounds for a novel polymerization process for vinyl monomers, which yields polymers with improved control over composition and nearly full to full conservation of architectural integrity up to high conversion. The regulator compounds are defined by according to anyone of the Formulas 1A, 1B, 1C, 1D, 1E, 1F, 1G, 1H and 1I: ##STR00001## wherein R.sup.1 stands for an optionally substituted secondary or tertiary alkyl or secondary or tertiary aralkyl; Z.sup.1 stands for CN or a carboxylic acid ester of formula C(O)OR.sup.21; Z.sup.2 may be chosen from the group of CN, carboxylic acid, salts of carboxylic acids, carboxylic acid ester, carboxylic acid amides, (hetero)aryl, alkenyl and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently chosen from the group of H, alkyl, aralkyl, (hetero)aryl, CN and carboxylic acid ester of formula C(O)OR.sup.22; R.sup.7 stands for a primary alkyl or primary aralkyl, CN or hydrogen; Y stands for a bridging group and n is 2, 3, 4, 5 or 6; in case R.sup.1 stands for tertiary alkyl or tertiary aralkyl, R.sup.6 stands for a primary alkyl or primary aralkyl, CN or a carboxylic acid ester of formula C(O)OR.sup.26; in case R.sup.1 stands for a secondary alkyl or secondary aralkyl, R.sup.6 stands for a primary or secondary alkyl or primary or secondary aralkyl, CN, a carboxylic acid ester of formula C(O)OR.sup.26 or a phosphonic acid ester of formula P(O)(OR.sup.27).sub.2, a (hetero)aryl or an alkenyl; R.sup.21, R.sup.22, R.sup.26 and R.sup.27 each independently stand for alkyl or aralkyl having from 1-30 carbon atoms, optionally containing heteroatoms.