944401-65-4Relevant academic research and scientific papers
alpha-SYNUCLEIN AGGREGATE BINDING AGENT AND IMAGING METHOD
-
Paragraph 0137; 0142, (2022/01/12)
The present invention provides an α-synuclein aggregate binding agent that has high binding selectivity for an α-synuclein aggregate. The α-synuclein aggregate binding agent contains a compound represented by a formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof: in the formula (I), R1 and R2 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl; R3 is hydrogen or halogen; the ring A is a benzene or pyridine ring; the ring B is represented by the following formula (i) or (ii): R4 and R5 are each independently selected from the group consisting of hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl.
CONDENSED HETEROCYCLES AS BCL-2 INHIBITORS
-
Page/Page column 329; 367; 483; 490; 496; 515; 522; 527; 534; 541, (2021/04/10)
The disclosure includes compounds of Formula (A) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11, h, j, m, n, k, v, s, g, V, W, L, Z1 Q1, Q2, Q3, Q4, Q5, Q6, and Q7, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.
1H-PYRROLO[2,3-B]PYRIDINE DERIVATIVES AS BCL-2 INHIBITORS FOR THE TREATMENT OF NEOPLASTIC AND AUTOIMMUNE DISEASES
-
Page/Page column 173; 178, (2021/07/02)
The present invention relates to lH-pyrrolo[2,3-b]pyridine derivatives and related compounds as BCL-2 inhibitors for treating neoplastic, autoimmune or neurodegenerative diseases. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 162 to 233; examples 1 to 8; table; compound examples cpd-1 to cpd-135; biological examples 1 to 4).
HOT MELT EXTRUDED SOLID DISPERSIONS CONTAINING A BCL2 INHIBITOR
-
Page/Page column 101; 105; 144; 233; 240; 247; 253-254; 265; ..., (2021/09/04)
A pro-apoptotic solid dispersion comprises, a Bcl -2 family protein inhibitory compound of Formula A as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier, and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula A, the water-soluble polymeric carrier, and the surfactant to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to provide a solid matrix comprising the polymeric carrier, and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl -2 family proteins, for example cancer or an immune or autoimmune disease.
TYK2 INHIBITORS AND USES THEREOF
-
Paragraph 00735, (2020/06/10)
Described herein are compounds that are useful in treating a TYK2-mediated disorder. In some embodiments, the TYK2-mediated disorder is an autoimmune disorder, an inflammatory disorder, a proliferative disorder, an endocrine disorder, a neurological disorder, or a disorder associated with transplantation.
Synthesis method of 2-fluoro-3, 6-dihydroxypyridine
-
Paragraph 0021-0024; 0034-0037; 0047-0050, (2020/03/09)
The invention discloses a synthetic method of 2-fluoro-3, 6-dihydroxypyridine, and belongs to the field of organic chemical synthesis. The synthesis method comprises the following steps: (1), reactinga compound C with bis(pinacolato)diboron under the action of an alkali and a catalyst to obtain a compound D; and (2) reacting the compound D with hydrogen peroxide to obtain the target product 2-fluoro-3, 6-dihydroxypyridine. The method is high in selectivity, mild in reaction condition and easy to operate, and the obtained product is high in purity. In the synthetic process, the compound C is aself-made synthetic material, a raw material 2-amino-6-fluoropyridine is subjected to bromination and diazotization hydrolysis reaction to obtain the compound C, and the compound C is more economicaland cost-saving than market sales price.
BCL-2 INHIBITORS
-
Page/Page column 235, (2020/03/15)
The disclosure includes compounds of Formula (A), (A) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11, h, j, m, n, k, v, s, g, V, W, L, Z1, Q1, Q2, Q3, Q4, Q5, Q6, and Q7, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.
COMPOUNDS FOR TREATMENT OF EYE DISORDERS
-
Page/Page column 71, (2021/01/23)
Compounds of formula I as defined herein, or pharmaceutically acceptable salts, solvates or derivatives thereof, are potent inhibitors of angiogenesis and accordingly are of use in the treatment and prevention of various angiogenesis-related disorders such as cancer.
COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PAIN
-
Page/Page column 53-55, (2019/08/26)
The invention relates to compounds, pyridine derivatives, and pharmaceutical 10 compositions containing same for use in the treatment of pain. It also relates to specific compounds, compositions comprising the same and uses thereof, in particular in the treatment of pain.
HETEROARYL COMPOUNDS AND USES THEREOF
-
Paragraph 0132-0134; 0143-0145; 0269; 0274-0275; 0294-0296, (2019/11/28)
Described herein are compounds of formula (I), and pharmaceutically acceptable salts, solvates, hydrates, isotopically labeled derivatives and radiolabeled derivative thereof, and pharmaceutical compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for detecting and imaging Tau aggregates in the brain for detection of Alzheimer's disease (AD) in a subject.
