292 results about "Angiogenesis inhibitor" patented technology

The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, incluidng angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.

3-Substituted indole carbohydrazides having the formula ##STR1## are useful for inhibiting angiogenesis. Also disclosed are angiogenesis-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.

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.

The present invention relates to a pharmaceutical cocktail, in particular, effective amounts of gemcitabine, in combination with effective amounts of docetaxel and angiogenesis inhibitor, especially a vascular endothelial growth factor (VEGF) inhibitor, such as bevacizumab for the treatment of cancer, in particular sarcoma, especially soft tissue sarcoma. Pharmaceutical compositions and methods of treating cancer, including sarcoma, especially soft tissue sarcoma (prolonging the patient's life, eliminating the tumor, improving the patient's quality of life, shrinking the tumor, prolonging survival and/or preventing the tumor's metastases) are additional aspects of the present invention.

The invention provides methods of treating a mammalian tumors comprising combination therapy with SPARC polypeptides, an angiogenesis inhibitor and paclitaxel. The invention provides also methods of treating a mammalian tumors comprising combination therapy with SPARC polypeptides and paclitaxel. Further, the invention produces kits and methods to predict therapy responses.

The present invention relates to pharmaceutical compositions comprising a sulfonamide-including compound in combination with an angiogenesis inhibitor.

Compounds having the formula

are angiogenesis inhibitors. Also disclosed are compositions containing the compounds, methods of making the compounds, and methods of treatment using the compounds.

The present invention provides an excellent drug delivery system to posterior segments. An injection according to the present invention is a periocular injection which comprises fine particles containing a drug and enables the drug to deliver to the posterior segments. The drug can be efficiently delivered to the posterior segments (such as a retina, a choroid and an optic nerve) while scarcely injuring ophthalmic tissues by administering the fine particles containing the drug periocularlly. Preferred fine particles are made of a synthetic biodegradable polymer, their average particle diameter is 50 nm to 150 μm, and the drug is dispersed in the fine particles uniformly. Preferred drugs are anti-inflammatories, immunosuppressors, antivirals, anticancer drugs, angiogenesis inhibitors, optic neural protectants, antimicrovials and antifungal agents.

Described herein are methods of inhibiting angiogenesis, and treating or preventing a disease or disorder (or symptoms thereof) associated with angiogenesis, wherein an anti-angiogenesis compound is administered to a subject.

The problems of the present invention are to find a pharmaceutical composition and a method for treating cancer that exhibit excellent anti-tumor effect. Excellent anti-tumor effect is achieved when 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, an analogous compound thereof, a pharmacologically acceptable salt thereof or a solvate thereof is used in combination with taxane.

The invention provides acid addition salts of the compounds represented by formula (1) or (2), or crystals thereof, and processes for preparing the same. The salts or crystals have HGFR inhibitory activity and excellent physical properties (solubility, safety, etc.) and are therefore useful as anti-tumor agents, angiogenesis inhibitors and inhibitors for metastasis for a various types of tumor.

Disclosed herein are soluble endoglin compounds and kits, pharmaceutical compositions, and articles of manufacture containing soluble endoglin compounds. Also disclosed herein are methods for treating an angiogenesis disorder, such as cancer, using soluble endoglin compounds, provided alone or in combination with a chemotherapeutic agent, an angiogenesis inhibitor, or an antiproliferative compound.

The invention relates to the use of designed β-sheet peptides together with radiation therapy for cancer treatment. The β-sheet peptides, which were designed using portions from several α-chemokines, exhibit activity as radiosensitizing agents, and have demonstrated synergism with radiation therapy for cancer treatment. The β-sheet peptides also exhibit activity as angiogenesis inhibitors.

Compounds having the formula

are angiogenesis inhibitors. Also disclosed are compositions containing the compounds, methods of making the compounds, and methods of treatment using the compounds.

The present invention relates to novel angiogenic-inhibitory compounds of formula (I) 1 and pharmaceutically acceptable salts thereof, wherein: Y is a direct bond or a linker group selected from a group of CH.sub.2, NH, NR.sub.1, S, SO, SO.sub.2, or O; Z is CO, CS, SO, SO.sub.2, or C.dbd.NH; R.sup.1 is H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, acyl, alkoxyacyl, aryloxyacyl, or aminoacyl groups; R.sup.2 is O, S, or NH; A is one to three cycloalkyl or aryl ring groups, in which any of these ring groups may be connected with other ring through a single bond or fused with at least one other ring, and these ring groups are optionally substituted at one or more positions with alkyl, alkoxy, aryl, aryloxy, arylalkyl, arylalkyloxy, hydroxyl, halogen, trihalomethyl, S(O)R, SO.sub.2NRR', SO.sub.3R, SR, B(OR).sub.2, PR.sub.3, P(O)(OR).sub.2, OP(O)(OR).sub.2, NO.sub.2, NRR', OR, CN, C(O)R, NHC(O)R, (CH.sub.2).sub.nCO.sub.2R, or CONRR', wherein R and R' are each independently selected from the group consisting of H, alkyl, alkoxy, aryl, aryloxy, arylalkyl, and arylalkyloxy and n is 0-11; and B is alkyl, arylalkyl, or one to three cycloalkyl or aryl ring groups, in which any of ring groups may be connected with other ring through a single bond or fused with at least one other ring; and these alkyl, arylalkyl or ring groups are optionally substituted at one or more positions with alkyl, alkoxy, aryl, aryloxy, arylalkyl, arylalkyloxy, hydroxyl, halogen, trihalomethyl, S(O)R, SO.sub.2NRR', SO.sub.3R, SR, B(OR).sub.2, PR.sub.3, P(O)(OR).sub.2, OP(O)(OR).sub.2, NO.sub.2, NRR', OR, CN, C(O)R, NHC(O)R, (CH.sub.2).sub.nCO.sub.2R, or CONRR', wherein R and R' are each independently selected from the group consisting of H, alkyl, alkoxy, aryl, aryloxy, arylalkyl, and arylalkyloxy and n is 0-11, pharmaceutical composition comprising them and their use.

The invention features methods and compositions for inhibiting angiogenesis in a tissue or detecting angiogenesis using antagonists of denatured or proteolyzed forms of laminin.

Though copper is elevated in the tumor tissue and plasma of patients with various malignancies, the molecular targets for copper binding agents in angiogenesis and tumor progression remain poorly understood. It is disclosed that one anti-angiogenic target for the copper binding agent tetrathiomolybdate is intracellular CuZn-superoxide dismutase (SOD1). A second generation tetrathiomolybdate analog, ATN-224, inhibits endothelial cell (EC) proliferation in vitro, binds to SOD1 and inhibits its activity without displacing bound copper ATN-224 can accumulate in ECs and inhibit CuZnSOD activity with an IC₅₀ similar to the IC₅₀ for EC proliferation, resulting in increased generation of intracellular reactive oxygen species. Inhibition of EC proliferation by ATN-224 in vitro is substantially reversed by a synthetic porphyrin SOD mimetic. Similar results were observed in vivo, where inhibition of angiogenesis by ATN-224 in a Matrigel plug model was also reversed by MnTBAP. Thus, a distinct molecular target for copper depletion therapy has been identified and SOD1 is now validated as a target for anti-angiogenesis. Methods for screening, or designing, such SOD1 inhibitors for use as angiogenesis inhibitors and anti-cancer agents are disclosed.

There is provided medicaments, particularly a vascular endothelial growth factor (VEGF) inhibitor which is useful as a therapeutic drug for solid tumors, diabetic retinopathy and the like diseases in which angiogenesis is taking a role. That is, since a novel 3-quinolin-2(1H)-ylideneindolin-2-one derivative or a salt thereof has good VEGF inhibitory action, angiogenesis inhibitory action and anti-tumor action, it is useful as ideal VEGF inhibitor, angiogenesis inhibitor and anti-tumor agent.

The invention relates to an anticancer slow-release gel injection which contains slow-release microspheres containing an angiogenesis inhibitor, an amphiphilic block polymer, a solvent and a slow-release agent, wherein the composition of the amphiphilic block polymer and the non-organic solvent exhibit the property of temperature-sensitive gelation. After the in vivo injection, the injection turns into a stagnant and biodegradable water-insoluble gel and the gel slowly releases the drug contained therein for a plurality of weeks to a plurality of months. After the intratumoral or peritumoral injection, the anticancer slow-release gel injection can significantly reduce the general drug reactions and is used for treating tumors of different stages. The angiogenesis inhibitor is selected from SU5416, SU6668, bosutinib, sprycel, erlotinib, vandetanib, gefitnib, canertinib, lapatinib, lestaurtinib, masitinib, vatalanib, mubritinib, tandutinib, nilotinib, marimastat, nilotinib, pelitinib, telatinib, sunitinib, sorafenib, zarnestra, sirolimus, imatinfb, lenalidomide and thalidomide.