303 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 provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.

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 invention relates to a peptide for high performance inhibition of angiogenesis and method for preparing same and use, wherein high performance blood vessel production inhibiting agent RGD-ED with integration compatibility is designed, the inhibiting agent comprises polypeptide polypeptide-valine-arginine-arginine-alanine-aspartate-arginine-alanine-alanine-valine-praline, its one or two ends are connected with polypeptides containing arginine-glycine-aspartic acid sequence. The RGD-ED provided by the invention can be synthesized. The invention also discloses the expression of one RGD-ED in bacillus coli through gene engineering method, wherein the RGD-ED is prepared through the steps of inclusion body protein segregation, dissolution and renaturation, and ion-exchange chromatography segregation and purification.

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.

The present invention provides a composition and a kit for treating tumors, which permits a sulfonamide-containing heterocyclic compound to exhibit its angiogenesis inhibitory activity and antitumor activity more effectively. According to the present invention, the sulfonamide-containing heterocyclic compound can be used in treating cancers more effectively by combination with a VEGF inhibitor / FGF inhibitor.

The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.

The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EGF dependency of a tumor cell for proliferation and / or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and / or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.

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.

This invention relates to compounds of formula (I) and (II) that are useful in treating vascular endothelial growth factor (VEGF)-mediated disorders, particularly endometriosis and acute macular degenerative disorder. The invention also relates to a topical system for the treatment of acute macular degenerative disorder comprising a VEGF inhibitor.

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.

The present invention provides methods of treating a parasitic infection, a lymphoid malignancy or an autoimmune disorder in a subject by administering to the subject a therapeutically effective amount of an angiogenesis inhibitor compound comprising a MetAP-2 inhibitory core coupled to a peptide.

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 a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof.A compound represented by the formula (I):wherein each symbol is as defined in the specification, except a particular compound, or a salt thereof, and a pharmaceutical agent containing the compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor or a cancer metastasis suppressor.

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.