150401-96-0Relevant academic research and scientific papers
GALNAC-TGFBR1 INHIBITOR CONJUGATES FOR THE TREATMENT OF LIVER DISEASES
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Page/Page column 287-289, (2021/04/17)
Conjugates comprising GalNAc moiety and a TGFβR1 inhibitor are provided. In some embodiments, the conjugates are useful for the treatment of viral infections, cancer, and fibrosis.
CRYSTAL FORM AND SALT FORM OF TGF-BRI INHIBITOR AND PREPARATION METHOD THEREFOR
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Paragraph 0085-0087, (2021/03/19)
Disclosed in the present invention are a crystal form and salt form of a TGF-βR1 inhibitor and a preparation method therefor, and further disclosed is an application of the crystal form and the salt form in preparation of medicines for treating cancers.
Growth Factor Receptor antagonists. Preparation method and application thereof
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Paragraph 0075-0080, (2021/11/10)
The invention relates to a small molecule antagonist for transforming growth factor β receptors, a method for preparing the small molecule antagonist, and application of the small molecule antagonist in preparation of drugs. The small molecule antagonist for transforming the growth factor β receptor has the application of treating and/or preventing various diseases mediated by ALK5, and has great clinical application potential.
BENZOTRIAZOLE-DERIVED AND UNSATURATED AMIDE COMPOUND USED AS TGF- R1 INHIBITOR
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Paragraph 0089; 0090, (2019/04/29)
A benzotriazole-derived α and β-unsaturated amide compound used as TGF-βR1 inhibitor or a pharmaceutically acceptable salt thereof, the structure of the compound being as shown in formula (I).
SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF CANCERS, INCLUDING HEPATOCELLULAR CARCINOMA, AND AS INHIBITORS OF HEPATITIS VIRUS REPLICATION
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Paragraph 0160, (2013/04/24)
Pharmaceutical compositions of the invention are presented which comprise substiuted aminothiazoles derivatives. The substiuted aminothiazoles derivatives have a disease-modifying action in the treatment of diseases associated with unregulated cell growth. Such diseases include cancers such as hepatocellular carcinoma, and viral infections from a hepatitis virus.
A concise synthesis of quinazolinone TGF-β RI inhibitor through one-pot three-component Suzuki-Miyaura/etherification and imidate-amide rearrangement reactions
Li, Hong-yu,Wang, Yan,McMillen, William T.,Chatterjee, Arindam,Toth, John E.,Mundla, Sreenivasa R.,Voss, Matthew,Boyer, Robert D.,Sawyer, J. Scott
, p. 11763 - 11770 (2008/03/13)
A simple and efficient synthesis of dihydropyrrolopyrazole boronic acid intermediate (5) has been developed. Utilization of a three-component Suzuki-Miyaura/etherification with microwave heating led to advanced compound 11 in high yield and with easy purification. Reaction of compound 11 with methanesulfonyl chloride at room temperature furnished the 1,3 O-N rearranged product (12), which is postulated to proceed via an intramolecular mechanism. The outlined synthesis provides a highly efficient and high-yielding route that is amenable to rapid analog synthesis.
TGF-BETA INHIBITORS
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Page/Page column 14, (2008/06/13)
The present invention is directed to inhibitors of TGF-BETA of Formula (I).
FUSED PYRAZOLE DERIVATIVES AS TGF-BETA SIGNAL TRANSDUCTION INHIBITORS FOR THE TREATMENT OF FIBROSIS AND NEOPLASMS
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Page/Page column 19, (2010/02/14)
The disclosed invention is directed to compounds of the formula: Formula (I) and methods of using these compounds.
NOVEL COMPOUNDS AS PHARMACEUTICAL AGENTS
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Page 29, (2010/02/07)
The current invention relates to compounds of the formula:(Ia) and the pharmaceutically acceptable salts thereof and their use as TGF-beta signal transduction inhibitors for treating cancer and other diseases in a patient in need thereof by administration of said compounds.
