cas 944401-65-4, 5-bromo-6-fluoropyridin-2-amine

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alpha-SYNUCLEIN AGGREGATE BINDING AGENT AND IMAGING METHOD
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.
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Paragraph 0137; 0142

(2022/01/12)

CONDENSED HETEROCYCLES AS BCL-2 INHIBITORS
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.
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Page/Page column 329; 367; 483; 490; 496; 515; 522; 527; 534; 541

(2021/04/10)

1H-PYRROLO[2,3-B]PYRIDINE DERIVATIVES AS BCL-2 INHIBITORS FOR THE TREATMENT OF NEOPLASTIC AND AUTOIMMUNE DISEASES
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).
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Page/Page column 173; 178

(2021/07/02)

HOT MELT EXTRUDED SOLID DISPERSIONS CONTAINING A BCL2 INHIBITOR
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.
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Page/Page column 101; 105; 144; 233; 240; 247; 253-254; 265; ...

(2021/09/04)

TYK2 INHIBITORS AND USES THEREOF
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.
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Paragraph 00735

(2020/06/10)

Synthesis method of 2-fluoro-3, 6-dihydroxypyridine
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.
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Paragraph 0021-0024; 0034-0037; 0047-0050

(2020/03/09)

BCL-2 INHIBITORS
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.
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Page/Page column 235

(2020/03/15)

COMPOUNDS FOR TREATMENT OF EYE DISORDERS
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.
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Page/Page column 71

(2021/01/23)

COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PAIN
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.
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Page/Page column 53-55

(2019/08/26)

HETEROARYL COMPOUNDS AND USES THEREOF
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.
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Paragraph 0132-0134; 0143-0145; 0269; 0274-0275; 0294-0296

(2019/11/28)

INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
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(2019/09/30)

Oxadiazolopyridine Derivates for Use as Ghrelin O-Acyl Transferase (GOAT) Inhibitors
The present invention relates to compounds of general formula I, wherein the groups R1, R2 and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
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Paragraph 0302-0306; 0319-0322

(2018/03/01)

8-[6-[3-(AMINO)PROPOXY]-3-PYRIDYL]-1 -ISOPROPYL-IMIDAZO[4,5-C]QUINOLIN-2-ONE DERIVATIVES AS SELECTIVE MODULATORS OF ATAXIA TELANGIECTASIA MUTATED (ATM) KINASE FOR THE TREATMENT OF CANCER
The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Rl, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also discloses the use of compounds of Formula (I) and salts thereof to treat or prevent ATM mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising substituted imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; and intermediates useful in such manufacture.
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Page/Page column 77

(2017/04/11)

New tetrahydropyrido pyrimidinecarboxylic compound or salt thereof
To provide a compound having an inhibitory activity for an androgen receptor. A tetrahydropyridopyrimidine compound represented by the following general formula (I) or a pharmaceutically acceptable thereof (in the formula, X and R are as defined in the specification).
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Paragraph 0179

(2016/10/08)

IMIDAZO[4,5-C]QUINOLIN-2-ONE COMPOUNDS AND THEIR USE IN TREATING CANCER
The specification generally relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, where Q, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5- c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating ATM kinase mediated disease, including cancer, using such compounds and salts.
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Page/Page column 103-104

(2015/11/27)

Discovery and optimization of a highly efficacious class of 5-aryl-2-aminopyridines as FMS-like tyrosine kinase 3 (FLT3) inhibitors
Based on a putative binding mode of quizartinib (AC220, 1), a potent FMS-like tyrosine kinase 3 (FLT3) inhibitor in Phase III clinical development, we have designed de novo a simpler aminopyridine-based hinge binding motif. Further optimization focusing on maximizing in vivo efficacy and minimizing CYP3A4 time-dependent inhibition resulted in a highly efficacious compound (6s) in tumor xenograft model for further preclinical development.
Liu, Gang,Abraham, Sunny,Liu, Xing,Xu, Shimin,Rooks, Allison M.,Nepomuceno, Ron,Dao, Alan,Brigham, Daniel,Gitnick, Dana,Insko, Darren E.,Gardner, Michael F.,Zarrinkar, Patrick P.,Christopher, Ron,Belli, Barbara,Armstrong, Robert C.,Holladay, Mark W.
p. 3436 - 3441
(2015/08/11)

TRISUBSTITUTED HETEROCYCLIC DERIVATIVES AS ROR GAMMA MODULATORS
The present invention provides trisubstituted heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; (I) in which R1, R2, R3, Ra, X, L, m and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the trisubstituted heterocyclic derivatives of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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Page/Page column 74

(2014/09/03)

Carbon-14 radiosynthesis of the benzofuran derivative and β-amyloid plaque neuroimaging positron emission tomography radioligand AZD4694
In support of a metabolite study, the β-amyloid plaque neuroimaging positron-emission tomography radioligand AZD4694 was labeled with carbon-14 in 10 radiosynthetic steps starting from radiolabeled carbon dioxide. [ 14C]AZD4694 was labeled in t
Sandell, Johan
p. 321 - 324
(2013/07/26)

METHOD OF INHIBITING HAMARTOMA TUMOR CELLS
Dimorpholinopyrimidines are useful for inhibiting growth or proliferation of hamartoma tumor cells. Because the Dimorpholinopyrimidines inhibit the growth and proliferation of hamartoma tumor cells they are also useful in treating PTEN hamartoma tumor syndromes. The therapeutic and prophylactic treatments provided by this invention are practiced by administering to a patient in need thereof an amount of a compound of dimorpholinopyrimidine derivative that is effective to inhibit growth or proliferation of the hamartoma tumor cells.
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Page/Page column 23-24

(2012/08/28)

BIARYL COMPOUNDS AND METHODS OF USE THEREOF
Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
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Page/Page column 194

(2011/04/13)

NOVEL 2-HETEROARYL SUBSTITUTED BENZOTHIOPHENES AND BENZOFURANES 709
The present invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimers disease as well as measureing clinical efficacy of Alzheimers disease therapeutic agents.
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Page/Page column 23

(2008/12/08)

PYRIMIDINE DERIVATIVES USED AS PI-3 KINASE INHIBITORS
Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof ; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.
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Page/Page column 101

(2010/11/28)