Patent classifications
C07K5/08
COMPOSITIONS AND METHODS FOR MODULATING INFLAMMATION AND WOUND HEALING
Compositions and methods for modulating inflammation and wound healing are provided.
INHIBITORS OF HUMAN EPIDIDYMUS PROTEIN 4
The present disclosure provides compounds of Formula I for use in the treatment of medical disorders by the inhibition of human epididymal protein 4 (HE4).
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INHIBITORS OF HUMAN EPIDIDYMUS PROTEIN 4
The present disclosure provides compounds of Formula I for use in the treatment of medical disorders by the inhibition of human epididymal protein 4 (HE4).
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TARGETED NITROXIDE AGENTS
Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
TARGETED NITROXIDE AGENTS
Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF, OR METAL COMPLEX THEREOF
The present invention provides a compound represented by the formula (1) or a salt thereof, or a complex of the compound or the salt with a metal, in the formula (1), A.sup.1 represents a chelate group; R.sup.1 represents a hydrogen atom or the like; R.sup.2 represents a hydrogen atom or the like; and Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4, and Z.sup.5 are the same or different and each represent a nitrogen atom or CR.sup.3 or the like wherein R.sup.3 represents a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group or the like; L.sup.1 represents a group represented by the formula (3) wherein R.sup.13, R.sup.14, R.sup.15, and R.sup.16 are the same or different and each represent a hydrogen atom or the like; L.sup.2 represents an optionally substituted C.sub.1-6 alkylene group; and L.sup.3 represents as optionally substituted C.sub.1-6 alkylene group.
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NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF, OR METAL COMPLEX THEREOF
The present invention provides a compound represented by the formula (1) or a salt thereof, or a complex of the compound or the salt with a metal, in the formula (1), A.sup.1 represents a chelate group; R.sup.1 represents a hydrogen atom or the like; R.sup.2 represents a hydrogen atom or the like; and Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4, and Z.sup.5 are the same or different and each represent a nitrogen atom or CR.sup.3 or the like wherein R.sup.3 represents a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group or the like; L.sup.1 represents a group represented by the formula (3) wherein R.sup.13, R.sup.14, R.sup.15, and R.sup.16 are the same or different and each represent a hydrogen atom or the like; L.sup.2 represents an optionally substituted C.sub.1-6 alkylene group; and L.sup.3 represents as optionally substituted C.sub.1-6 alkylene group.
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Tripeptide Propylene Oxide Derivative and Preparation Method and Application thereof
The present invention discloses a tripeptide propylene oxide derivative or a pharmaceutically acceptable salt thereof, and a preparation method and application thereof. The structure of the tripeptide propylene oxide derivative is shown in formula I. Compared with the prior art, the present invention provides tripeptide epoxy ketone compounds with a novel structure and a function of inhibiting proteasome. As 20S proteasome inhibitors, the tripeptide epoxy ketone compounds can block tumor cell proliferation and induce tumor cell apoptosis, so the tripeptide epoxy ketone compounds can be used for the treatment and prevention of a plurality of human and animal diseases such as malignant tumors, and the effect is significantly better.
Tripeptide Propylene Oxide Derivative and Preparation Method and Application thereof
The present invention discloses a tripeptide propylene oxide derivative or a pharmaceutically acceptable salt thereof, and a preparation method and application thereof. The structure of the tripeptide propylene oxide derivative is shown in formula I. Compared with the prior art, the present invention provides tripeptide epoxy ketone compounds with a novel structure and a function of inhibiting proteasome. As 20S proteasome inhibitors, the tripeptide epoxy ketone compounds can block tumor cell proliferation and induce tumor cell apoptosis, so the tripeptide epoxy ketone compounds can be used for the treatment and prevention of a plurality of human and animal diseases such as malignant tumors, and the effect is significantly better.
Process for preparing eptifibatide
The present invention provides processes for preparation of eptifibatide that involve coupling of amino acids in a (2+5), (4+3) and (3+4) sequence method. The invention further provides products produced by the described processes, novel compounds that can be used as synthetic intermediates for the preparation of eptifibatide.