260 results about "Camptothecin derivative" patented technology

The present Invention relates to a method of treating abnormal cell growth in a subject, comprising administering to said subject having abnormal cell growth: (a) a compound selected from the group consisting of a camptothecin, a camptothecin derivative, or a pharmaceutically acceptable salt, solvate or prodrug of said compounds; (b) a pyrimidine derivative or a pharmaceutically acceptable salt, solvate or prodrug of said pyrimidine derivative; and (c) an anti-tumor agent selected from the group consisting of antiproliferative agents, kinase inhibitors, angiogenesis inhibitors, growth factor inhibitors, cox-I inhibitors, cox-II inhibitors, mitotic inhibitors, alkylating agents, anti-metabolites, intercalating antibiotics, growth factor inhibitors, radiation, cell cycle inhibitors, enzymes, topoisomerase inhibitors, biological response modifiers, antibodies, cytotoxics, anti-hormones, anti-androgens and combinations thereof.

Provided are methods relating to compositions that include a CDP-topoisomerase inhibitor, e.g., a CDP-camptothecin or camptothecin derivative conjugate, e.g., CRLX101.

The present invention relates to a nanoparticle composition comprising a camptothecin derivative, solid polyethyleneglycol and an anti-associative agent, and the process for preparing the same. Specifically, the present invention provides a composition comprising a nanoparticle of the camptothecin derivative, which is prepared by solid-dispersing the poorly water soluble camptothecin derivative in polyethyleneglycol and dissolving the solid dispersions in an aqueous solution containing an anti-associative agent. The composition of the present invention stabilizes the camptothecin derivative lactone form in body fluid for effective anticancer activity.

Camptothecin-based compounds are useful for treating a neoplasm in mammalian subjects by administering such compound to the subjects in combination with radiotherapy, i.e., the treatment of tumors with radioactive substances or radiation from a source external to the subject. Camptothecin-based compounds are modified by positioning at least one electron-affinic group around the camptothecin structure to enhance their value in combination with radiotherapy. New Camptothecin-based compounds are disclosed that are useful for treating cancer by administering the novel compounds alone or in combination with radiotherapy.

This invention discloses a new camptothecin derivate of 20-position esterification, its preparation, containing their medicine combination, and its usage of using it as medicine, especially as antitumor drug.

The invention relates to a novel amphiphilic-block-copolymer-based pro-camptothecin drug, which is a compound of methoxy polyethylene glycol- polylactic acid and camptothecin derivatives (mPEG-X-PLA-T), wherein, mPEG refers to methoxy polyethylene glycol; X refers to linking group, for example, succinic acid; PLA refers to polylatic acid; T refers to drug molecule, that is, camptothecin derivatives such as, camptothecin, 10-hydroxycamptothecine, 7-ethyl-10- hydroxycamptothecine. Polylactic acid is connected with camptothecin derivatives through ester bond.

The present invention relates to a semi-solid filling medium which comprises a camptothecin derivative; a pharmaceutically acceptable carrier matrix which is a polyglycolized glyceride; and an effective thickening-reducing and stabilizing-promoting amount of one or more pharmaceutically acceptable excipients.

The invention discloses camptothecin and a self-emulsifying medicine precursor of a derivative thereof. The self-emulsifying medicine precursor is prepared by the covalent union of medicine molecules and hydrophilic radicals, wherein the medicine molecules are camptothecin molecules or camptothecin derivative molecules, and the medicine carrying quantity of the precursor is as high as more than 50%. The invention also discloses application of the self-emulsifying medicine precursor. The self-emulsifying medicine precursor can form micelles or vesicles with nano size in water, can be used as a medicine carrier used for loading one or a plurality of other anticancer medicines, such as CPT derivatives, yew alcohol, turmeric essence, methotrexate, irinotecan, danshinolic acid, matrine, doxorubicine and the like, can form a nano medicine carrying a plurality of medicines and can realize the synergic treatment of the medicines.

(20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an aminoalkanoic acid or an imidoalkanoic acid and camptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating cancer.

The present invention provides a pharmaceutical composition comprising at least one hydrophobic camptothecin derivative or a pharmaceutically acceptable salt of said derivative and a polyethylene glycol (PEG) conjugated phospholipid. Also provided is a method to inhibit cancer cells in a subject in need thereof by administering the pharmaceutical composition of the present invention.

The invention provides a butyrylcholinesterase variant having the amino acid sequence selected from SEQ ID NOS: 4, 6, 8, 10, 12, 14, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 66, 68, 70, 72, 74, 76, 78, 80, 82, 84, 86, 88, 90, 92, 94, 96, 98, 100, 102, 104, 106, 108, 110, 112, 114, 116, 118, 120, 122, 124, 126, 128, 130, 132, 134, 136, 138, 140, 142, 144, 146, 148, 150, 152, 154, 156, 158, 160, 162, 164, 166, 168, 170, 172, 174, 176, 178, 180, 182, 184, 186, 188, 190, 192, 194, and 196, or functional fragment thereof. In addition, the invention provides a method of converting a camptothecin derivative to a topoisomerase inhibitor by contacting the camptothecin derivative with a butyrylcholinesterase variant selected from SEQ ID NOS: 2, 4, 6, 8, 10, 12, 14, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 66, 68, 70, 72, 74, 76, 78, 80, 82, 84, 86, 88, 90, 92, 94, 96, 98, 100, 102, 104, 106, 108, 110, 112, 114, 116, 118, 120, 122, 124, 126, 128, 130, 132, 134, 136, 138, 140, 142, 144, 146, 148, 150, 152, 154, 156, 158, 160, 162, 164, 166, 168, 170, 172, 174, 176, 178, 180, 182, 184, 186, 188, 190, 192, 194, and 196, or functional fragment thereof, under conditions that allow conversion of a camptothecin derivative to a topoisomerase inhibitor. Further, the invention provides a method of treating cancer by administering to an individual an effective amount of a butyrylcholinesterase variant selected from SEQ ID NO: 2, 4, 6, 8, 10, 12, 14, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 66, 68, 70, 72, 74, 76, 78, 80, 82, 84, 86, 88, 90, 92, 94, 96, 98, 100, 102, 104, 106, 108, 110, 112, 114, 116, 118, 120, 122, 124, 126, 128, 130, 132, 134, 136, 138, 140, 142, 144, 146, 148, 150, 152, 154, 156, 158, 160, 162, 164, 166, 168, 170, 172, 174, 176, 178, 180, 182, 184, 186, 188, 190, 192, 194, and 196, or functional fragment thereof, exhibiting increased capability to convert a camptothecin derivative to a topoisomerase inhibitor compared to butyrylcholinesterase.

The present invention is to prepare efficiently 2'-amino-5'-hydroxypropiophenone corresponding to the AB-ring part of camptothecin (CPT) skeleton and a tricyclic ketone corresponding to the CDE-ring part in order to provide efficiently CPT by the total synthesis, which is a starting material for irinotecan hydrochloride and various kinds of camptothecin derivatives, and to provide stably CPT and its derivatives.

A method for treating diseases associated with abnormal cell proliferation comprises delivering to a patient in need of treatment a compound selected from the group consisting of 20(S)-camptothecin, analog of 20(S)-camptothecin, derivative of 20(S)-camptothecin, prodrug of 20(S)-camptothecin, and pharmaceutically active metabolite of 20(S)-camptothecin, in combination with an effective amount of one or more agents selected from the group consisting of alkylating agent, antibiotic agent, an alkylating agent, antibiotic agent, antimetabolic agent, hormonal agent, plant-derived agent, anti-angiogenesis agent and biologic agent. The method can be used to treat benign tumors, malignant or metastatic tumors, leukemia and diseases associated with abnormal angiogenesis.

An insecticide for the pests in homopteran, thysanoptera, lepidoptera and coleoptera is prepared from camptothecine or its derivative, emulsifier, penetrant and organic solvent through proportional mixing.

The invention provides a butyrylchinesterase variant, a method of converting a camptothecin derivative to a topoisomerase inhibitor by contacting the camptothecin derivative with a butyrylcholinesterase variant and a method of treating cancer by administering to an individual an effective amount a butyrylcholinesterase variant exhibiting increased capability to convert a camptothecin derivative to a topoisomerase inhibitor compared to butyrylcholinesterase.

A lipoid nanoparticle of camptothecine-phosphatide composition is prepared from phosphatide, 10-hydroxy camptothecine or its derivative and lipoid. Its preparing process is also disclosed.

Various 14-Nitro, 14-amino, and 14-substituted amino camptothecin derivatives are useful in the treatment of cancer and other hyperproliferative diseases. Various 14-nitro camptothecin derivatives are conveniently prepared by reacting a camptothecin derivative with fuming nitric acid, optionally employing acetic anhydride as a solvent.

(20) esters of camptothecin analogs are provided. The compounds are (20) esters of an aminoalkanoic acid or an imidoalkanoic acid and homocamptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the homocamptothecin ring. The compounds are useful for treating cancer.

Disclosed is the agricultural pesticide containing camptothecine or camptothecine derivatives and the use thereof, wherein the pesticide comprises camptothecine or its derivatives 0.02-2.0%, emulsifying agent 1.0-20%,penetrating agent 0.5-10%, and balancing organic solvent. The pesticide can be used for controlling agronomic crop downy mildew, leaf streak, pythium blight, head blight, root and stem rot, rhizoctonia rot, damping-off, wilt,bitter rot, powdery mildew, black shank, brown spot, leaf scab, ring rot, black pox, gray mold,phytophthora rot, ulcer disease, black spot, bacterial wilt, angular leaf spot, leaf streak and leaf scar.

The invention provides a novel camptothecin derivative expressed by a structural formula 3 as shown in the specification, and a preparation method and the antitumor application of the novel camptothecin derivative. Activity tests prove that the designed and synthesized camptothecin derivative 3 has an excellent anti-hepatoma effect and is expected to be applied clinically as a cantharidin anti-tumor medicine. Besides, the synthesis method of the camptothecin derivative 3 is easily available in raw materials, low in cost, simple in synthesis routine, high in yield and easy to operate and implement.