64 results about "Receptor tyrosine kinase inhibitor" patented technology

This invention is directed to methods of preparing 4-substituted quinoline compounds as intermediates in the manufacture of receptor tyrosine kinase inhibitors and intermediate compounds used in the methods thereof, wherein the 4-substituted quinoline compound has the following general formula (I):wherein substitutions at LG″, PG, A, G, R1 and R4 are set forth in the specification.

This invention provides quinazoline analogs of Formula I:where A is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to two independent R3 groups. The invention also includes methods of using compounds of Formula I as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

This invention concerns quinazoline analogs of Formula I: where an A group is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to three independent R3 groups. The invention also includes methods of using these compounds as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Disclosed are methods and compositions for inhibiting the growth of a tumor (e.g., a malignant tumor) in a subject. In particular, combination therapies for treating a tumor in a subject by co-administering either i) an effective amount of an anti-estrogen agent or ii) an effective amount of a receptor tyrosine kinase inhibitor and an effective amount of a bispecific anti-ErbB2 / anti-ErbB3 antibody, and optionally an effective amount trastuzumab. Also disclosed is a bispecific anti-ErbB2 / anti-ErbB3 antibody for use in the therapy of a tumor in combination with either i) an anti-estrogen agent or ii) a receptor tyrosine kinase inhibitor, and optionally in use with trastuzumab.

This invention concerns quinazoline analogs of Formula I:where an A group is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to three independent R3 groups. The invention also includes methods of using these compounds as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

This invention relates to detection of specific extracellular DNA in plasma or serum fractions of human or animal blood associated with neoplastic, pre-malignant or proliferative disease. Specifically, the invention relates to detection tumor-associated DNA, and to those methods of detecting and monitoring tumor-associated DNA found in the plasma or serum fraction of blood by using DNA extraction and amplification with or without enrichment for DNA. The invention allows the selection and monitoring of patients for various cancer therapies including receptor tyrosine kinase inhibitor therapies.

A method to inhibit the growth of tumors in human patients, comprising treating the human patients with an effective amount of a combination of radiation and a non-radiolabeled protein receptor tyrosine kinase inhibitor, the overexpression of which can lead to tumorigenesis.

Compounds of Formula I: in which A, B, R<1>, R<1a>, R<2>, R<3>, R<4>, R<5> R<6>, R<7> and R<8> have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment ofdiseases mediated by class 3 and class 5 receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1.

The invention discloses ten (10) protein markers predictive of cancer resistance or responsiveness to Type III Receptor Tyrosine Kinase (RTK) inhibitors, and provides methods for identifying a cancer that is likely to be resistant to a Type III RTK-inhibiting therapeutic by examining expression and / or activity of one or more of the disclosed biomarkers in a biological sample from the cancer. Methods for identifying a compound that inhibits a cancer resistant to a Type III RTK-inhibiting therapeutic by determining the effect of the compound on one or more of the disclosed marker proteins are also provided.

The present application relates to novel quinazoline compounds as inhibitors of type I receptor tyrosine kinases, the pharmaceutical compositions comprising one or more of the compounds and salts thereof as an active ingredient, and the use of the compounds and salts thereof in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals and especially in humans.

This invention relates to detection of specific extracellular DNA in plasma or serum fractions of human or animal blood associated with neoplastic, pre-malignant or proliferative disease. Specifically, the invention relates to detection tumor-associated DNA, and to those methods of detecting and monitoring tumor-associated DNA found in the plasma or serum fraction of blood by using DNA extraction and amplification with or without enrichment for DNA. The invention allows the selection and monitoring of patients for various cancer therapies including receptor tyrosine kinase inhibitor therapies.

The present invention relates to the administration of anti-CTLA4 antibodies, particularly human antibodies against human CTLA4, such as with antibodies 3.1.1, 4.1.1, 4.8.1, 4.10.2, 4.13.1, 4.14.3, 6.1.1, ticilimumab (also known as 11.2.1 or CP-675, 206), 11.6.1, 11.7.1, 12.3.1.1, 12.9.1.1, and antibodies to the amino acid sequences of ipilimumab (also known as 10D1 or MDX-010) , with an indolinone receptor tyrosine kinase inhibitor (RTKI), for example, N-[2-diethylamino]ethyl]-5-[(Z)-(5-fluoro-2-oxo-1, 2-dihydro-3H-indole-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carbamoyl (compound 1), N-[2-(ethylamino) Ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H -pyrrole-3-carbamoyl (compound 2), and 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indole-3-ylidene)methyl] -N-[(2S)-2-Hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carbamoyl (compound 3) combination for the treatment of cancer. The present invention relates to the administration of an anti-CTLA4 antibody in combination with an indolinone RTKI, such as, in particular, Compound 1. The present invention relates to neoadjuvant, adjuvant, first-line, second-line, and third-line treatments of cancer, whether localized or metastatic, and at any point in disease progression (eg, at any stage of the cancer).

The present disclosure relates to stable formulations of receptor tyrosine kinase inhibitors (TKI), e.g., pazopanib; methods of preparation thereof; and use of the disclosed formulations in sustained delivery of the active agent to a target site. The disclosure further relates to methods of converting one polymorphic Form of a TKI to another polymorphic Form and / or an amorphous form.

Compounds of Formula I: and pharmaceutically acceptable salts thereof in which R1, R2, R3, R4, R5 and R6 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of fibrosis, bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, pain and burns in a mammal.