The present invention disclosed 3-substituted phenylamidine compounds of general formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.4a, R.sup.4b, A and E have the same meanings as defined in description. The present invention further discloses methods for their preparation and use of the compounds of general formula (I) as a crop protection agent.

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A compound that is fluidized by light irradiation and reversibly non-fluidized and is represented by the following general formula (1):

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In the general formula (1), Ar.sub.1 and Ar.sub.2 each independently represent an aromatic hydrocarbon group optionally having a substituent or an aromatic heterocyclic group optionally having a substituent, and Y, Z.sub.1, and Z.sub.2 each independently represent a hydrogen atom or a lower alkyl group.

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.

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.

This invention relates to compounds of formula 1, 2 or 3

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a pharmaceutically acceptable salt, or solvate thereof, wherein X.sub.1, Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are as defined herein. The compounds are antimicrobial agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1, 2 or 3.

This invention relates to compounds of formula 1, 2 or 3

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a pharmaceutically acceptable salt, or solvate thereof, wherein X.sub.1, Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are as defined herein. The compounds are antimicrobial agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1, 2 or 3.

The use of an aldehyde mixture containing 70 to 95 wt % of aldehydes of formula (I) and 5 to 30 wt % of alkylbenzene compounds not corresponding to formula (I) as a blocking agent for amines results in odorless, especially economically blocked amines, which at room temperature are typically liquid and have a surprisingly low viscosity. Such blocked amines are particularly suitable as latent hardeners in isocyanate-group-containing compositions. Single-component moisture-curing polyurethane compositions formulated therewith are surprisingly stable in storage, can be used for low-emission applications without odor problems and do not trigger any problems with plasticizer migration. Surprisingly, said compositions even have advantages over corresponding compositions having latent hardeners based on purified aldehydes of formula (I), in particular with respect to viscosity, storage stability and especially strength.

The use of an aldehyde mixture containing 70 to 95 wt % of aldehydes of formula (I) and 5 to 30 wt % of alkylbenzene compounds not corresponding to formula (I) as a blocking agent for amines results in odorless, especially economically blocked amines, which at room temperature are typically liquid and have a surprisingly low viscosity. Such blocked amines are particularly suitable as latent hardeners in isocyanate-group-containing compositions. Single-component moisture-curing polyurethane compositions formulated therewith are surprisingly stable in storage, can be used for low-emission applications without odor problems and do not trigger any problems with plasticizer migration. Surprisingly, said compositions even have advantages over corresponding compositions having latent hardeners based on purified aldehydes of formula (I), in particular with respect to viscosity, storage stability and especially strength.

The invention relates to a process for the preparation of a compound represented by formula (I) wherein X is selected from the group consisting of —H, -halogen, linear or branched C1-C7 alkyl group, linear or branched C1-C5 alkoxy group, —NO.sub.2 and —CN and Y is a linear or branched C1-C7 alkyl group, comprising the steps of: 10 a) reacting a compound represented by formula (II) with a compound represented by (III) to obtain an intermediate product, wherein X is as defined with respect to formula (I), wherein Z is H, CH.sub.3 or C.sub.2H.sub.5, b) reacting the intermediate product of step a) with a compound represented by Y.sub.2SO.sub.4 (IV) wherein Y is as defined with respect to formula (I) to obtain a salt and c) hydrolyzing the salt of step b) to obtain the compound of formula (I). ##STR00001##

The invention relates to a process for the preparation of a compound represented by formula (I) wherein X is selected from the group consisting of —H, -halogen, linear or branched C1-C7 alkyl group, linear or branched C1-C5 alkoxy group, —NO.sub.2 and —CN and Y is a linear or branched C1-C7 alkyl group, comprising the steps of: 10 a) reacting a compound represented by formula (II) with a compound represented by (III) to obtain an intermediate product, wherein X is as defined with respect to formula (I), wherein Z is H, CH.sub.3 or C.sub.2H.sub.5, b) reacting the intermediate product of step a) with a compound represented by Y.sub.2SO.sub.4 (IV) wherein Y is as defined with respect to formula (I) to obtain a salt and c) hydrolyzing the salt of step b) to obtain the compound of formula (I). ##STR00001##