51656-90-7Relevant articles and documents
Stereoselective Diboration of Spirocyclobutenes: A Platform for the Synthesis of Spirocycles with Orthogonal Exit Vectors
Nóvoa, Luis,Trulli, Laura,Parra, Alejandro,Tortosa, Mariola
supporting information, p. 11763 - 11768 (2021/04/26)
The diastereo- and enantioselective diboration of spirocyclobutenes provides a platform for the rapid preparation of a wide variety of chiral spirocyclic building blocks. The chemoselective functionalization of the carbon-boron bond in the products, including a stereospecific sp3-sp2 Suzuki–Miyaura cross-coupling reaction, provides a powerful tool to control the directionality and the nature of the exit vectors in the spirocyclic framework.
PYRAZOLE CARBOXAMIDE COMPOUNDS FOR TREATMENT OF HBV
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Page/Page column 58-59, (2021/10/30)
The present disclosure provides, in part, pyrazole carboxamide compounds, and pharmaceutical compositions thereof, useful for disruption of HBV core protein assembly, and methods of treating Hepatitis B (HBV) infection.
PYRIDAZINONE DERIVATIVE
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Paragraph 0174, (2021/06/03)
Provided are: a pyridazinone derivative and/or a pharmaceutically acceptable salt thereof, which is useful as a therapeutic agent and/or a prophylactic agent for diseases in which Nav1.1 is involved and various central nervous system diseases; and a medicine containing the pyridazinone derivative and/or the pharmaceutically acceptable salt thereof as an active ingredient. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof. [In the formula, M1 represents a saturated or partially unsaturated C4-12 carbocyclic group or the like; R1 and R2 independently represent a hydrogen atom or the like; M2 represents a group represented by formula (2a) or the like; X1a, X1b and X1c independently represent N or the like; X2, X3 and X4 independently represent CR3 or the like; A1 and A2 independently represent N or the like; and R3 represents a hydrogen atom or the like.]
KINASE INHIBITORS
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Page/Page column 119; 120, (2021/10/15)
Disclosed herein are protein kinase inhibitors, in particular Bruton's tyrosine kinase (BTK) inhibitors, pharmaceutical compositions comprising them, processes for preparing them and uses of such protein kinase inhibitors to treat or prevent diseases, disorders and conditions associated with kinase function. In particular, the present invention relates to selective BTK inhibitors.
STAT DEGRADERS AND USES THEREOF
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Paragraph 000981; 000982, (2020/10/19)
The present invention provides compounds, compositions thereof, and methods of using the same.
N-(PYRIDIN-2-YLSULFONYL)CYCLOPROPANECARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF A CFTR MEDIATED DISEASE
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Page/Page column 222, (2020/07/14)
The invention relates to heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.
SPIRO COMPOUND AS INDOLEAMINE-2,3-DIOXYGENASE INHIBITOR
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Paragraph 0228; 0229, (2020/12/29)
Disclosed in the present invention are an indoleamine-2,3-dioxygenase inhibitor and a preparation method therefor. The inhibitor of the present invention has a structure as represented by general formula (I), wherein the definitions of Ar, E, Y, X, V, D, W, B, ring A and ring B are as shown in the description and claims. Also disclosed in the present invention is a preparation method for the inhibitor. The compound of general formula (I) of the present invention can be used as an indoleamine-2,3-dioxygenase inhibitor for preparing a medicament for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.
Rhodium-Catalyzed Intermolecular Cyclopropanation of Benzofurans, Indoles, and Alkenes via Cyclopropene Ring Opening
Jeyaseelan, Rubaishan,Lautens, Mark,Ross, Rachel J.
supporting information, (2020/06/29)
The generation of metal carbenoids via ring opening of cyclopropenes by transition metals offers a simple entry into highly reactive intermediates. Herein, we describe a diastereoselective intermolecular rhodium-catalyzed cyclopropanation of heterocycles and alkenes using cyclopropenes as carbene precursors with a low loading of a commercially available rhodium catalyst. The reported method is scalable and could be performed with catalyst loadings as low as 0.2 mol %, with no impact to the reaction yield or selectivity.
MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE
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Page/Page column 26, (2019/05/22)
Provided are IDO1 inhibitor compounds of Formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases.
MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE
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Paragraph 00727, (2019/03/05)
The present disclosure provides for compounds of Formula (I) wherein A2, A3, A4, A6, A7, A8, A15, RA, R5, R9, R10A, R10B, R11, R12, R13, R14, R16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).