164 results about "Macrocycle Compounds" patented technology

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure provides solid forms of Compound A, as described herein. The disclosure also provides pharmaceutical compositions comprising the disclosed solid forms and methods of using the disclosed solid forms and pharmaceutical compositions (e.g., to treat cancer).

Disclosed herein are compounds useful for the inhibition of KRAS G12D, G12V, G12A, G12S, G12R, G13D, Q61H, Q61L, Q61R or G12C. The compounds have a general Formula (I): or pharmaceutically acceptable salts thereof, wherein the variables of Formula (I) are as defined herein. Also provided herein are pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a KRAS G12D, G12V, G12A, G12S, G12R, G13D, Q61H, Q61L, Q61R or G12C disorder

Disclosed herein are compounds useful for the inhibition of KRAS G12D, G12V, G12A, G12S, G12R, G13D, Q61H, Q61L, Q61R or G12C. The compounds have a general Formula (I) or pharmaceutically acceptable salts thereof, wherein the variables of Formula (I) are as defined herein. Also provided herein are pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a KRAS G12D, G12V, G12A, G12S, G12R, G13D, Q61H, Q61L, Q61R or G12C disorder.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The present invention relates to a macrocyclic compound and a therapeutic use thereof. Disclosed in the present invention is a compound of formula (I), a pharmaceutically acceptable salt of said compound, a solvate of said compound, or a solvate of said pharmaceutically acceptable salt, and a use thereof in the preparation of a drug for treating cancer.

The invention provides a novel macrocyclic compound, a gadolinium chelate thereof, a method for preparing the compound and application of the compound as a magnetic resonance contrast agent. The compound has pertinence on magnetic resonance detection of liver focal lesions and can be used for liver specific imaging.

The present invention relates to macrocyclic compounds and therapeutic uses thereof. Disclosed are compounds of formula (I), or pharmaceutically acceptable salts thereof, solvates thereof or solvates of the pharmaceutically acceptable salts, and their use in the preparation of medicaments for the treatment of cancer.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The present disclosure provides compounds of formula (I), pharmaceutical compositions thereof, and uses thereof in the treatment and / or prevention of diseases or conditions associated with CDK9 kinase activity. JPEG2025538275000286.jpg3450

The present invention relates to a nitrogen-containing macrocycle derivative regulator, a preparation method therefor, and a use thereof. In particular, the present invention relates to a compound represented by general formula (A), a preparation method therefor, a pharmaceutical composition containing said compound, and a use thereof as a regulator in the preparation of a drug for treating metabolic diseases and related diseases, each substituent in general formula (A) being as defined in the description.

The invention relates to a macrocyclic compound, a pharmaceutical composition and application of the macrocyclic compound. The macrocyclic compound has a structural formula as shown in a formula I. The macrocyclic compound is a TYK2 allosteric inhibitor with high blood brain barrier passing ability and high selectivity, and can be used for regulating TYK2 mediated diseases.

To provide a method for producing a bipyridine derivative, which enables obtaining a high-purity target compound (including an intermediate) without performing purification by column chromatography, provides a high yield, and is industrially advantageous.SOLUTION: A method for producing a bipyridine derivative represented by formula (3) comprises a step of obtaining a metal complex as an intermediate. In the formula, each of R13 to R20 is a hydrogen atom or a substituent; a plurality of R13 to R20 may be the same or different; at least one of six R14 to R16 is a substituent; at least one of two R17 is a hydrogen atom; any two substituents of R13 to R20 may be linked to each other to form a ring; R17 to R20 may contain a pyrrolyl group which may contain a halogen atom or a substituent; and at least one of R14 to R16 may have a halogen atom or a substituent.SELECTED DRAWING: None

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The present disclosure relates to a macrocyclic compound represented by formula I, a pharmaceutical composition containing the compound or a pharmaceutically acceptable salt, prodrug, solvate, polymorph, isomer and stable isotopic derivative thereof, a preparation method therefor, and a use thereof as a TRK, ROS1, c-Met, CSF1 and / or ALK inhibitor.

The present disclosure relates to macrocyclic compounds, pharmaceutical compositions containing macrocyclic compounds, and methods of using macrocyclic compounds to treat disease, such as cancer.

The invention discloses a macrocyclic compound as well as a pharmaceutical composition and application thereof. The present invention provides a compound represented by formula (I), a solvate thereof, a pharmaceutically acceptable salt thereof, or a solvate of the pharmaceutically acceptable salt thereof. The compounds of the present disclosure are useful as inhibitors of TNF [alpha] and are useful in the treatment of inflammation and autoimmune diseases.

The present disclosure relates to indazole containing macrocyclic compounds, pharmaceutical compositions containing macrocyclic compounds, and methods of using macrocyclic compounds to treat disease, such as cancer.

The disclosure provides solid forms of Compound A, as described herein. The disclosure also provides pharmaceutical compositions comprising the disclosed solid forms and methods of using the disclosed solid forms and pharmaceutical compositions (e.g., to treat cancer).

Provided in the present invention are a macrocyclic compound as represented by formula (I'), or an isotopic variant, tautomer, stereoisomer, prodrug, polymorph, hydrate, or solvate thereof, or a pharmaceutically acceptable salt thereof. Further provided in the present invention are a method for preparing the compound, a pharmaceutical composition containing the compound, and the use of the compound in the prevention and treatment of KRAS-mediated diseases such as tumors.

The present disclosure relates to solid forms of Compound 1, or a pharmaceutically acceptable form thereof, a pharmaceutically acceptable salt of Compound 1, or pharmaceutically acceptable solvate thereof, pharmaceutical compositions comprising the same, methods of preparing the same, and methods of treating cancer dependent on a farnesylated protein, using the same.

The present disclosure relates to indazole macrocyclic compounds, pharmaceutical compositions containing macrocyclic compounds, and methods of using macrocyclic compounds to treat disease, such as cancer comprising administering a therapeutically effective amount of a compound to a subject in need thereof.

The invention belongs to the technical field of pharmaceutical chemistry, radiopharmaceutical chemistry and clinical nuclear medicine, and particularly relates to a rotaxane protection-based radioactive halogen labeled compound as well as a preparation method and application thereof. A rotaxane protection-based radioactive halogen labeled compound comprises: a macrocyclic compound having a cavity, the macrocyclic compound comprising one of cyclodextrin, cucurbituril, calixarene and pillararene; a radioactive halogen-labeled compound: the radioactive halogen-labeled position is located in the cavity of the macrocyclic compound; and the end-capping group is positioned at the opening end of the cavity, is connected to two ends of the radioactive halogen-labeled compound and is used for preventing the radioactive halogen-labeled compound from sliding out of the cavity. The rotaxane protection-based radioactive halogen labeled compound provided by the invention has good in-vivo stability, and solves the problem of poor in-vivo stability caused by dissociation of radioactive halogen and a tracer agent in the existing radioactive halogen labeled compound.

The present application relates to RAS inhibitors. The invention features macrocyclic compounds capable of inhibiting Ras proteins and pharmaceutical compositions and protein complexes thereof, and their use in the treatment of cancer.