- HETEROCYCLIC COMPOUNDS AS INHIBITORS OF HPK1
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This disclosure relates to heterocyclics as inhibitors of HPK1, in particular relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising said compound that useful for treatment of HPK1 mediated diseases and conditions such as cancer. (I)
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Page/Page column 180
(2021/01/29)
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- Preparation method of levo-demethyl benzene ring nonyl ester hydrochloride
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The invention belongs to the technical field of medicine preparation, and discloses a preparation method of levo-demethylated benzene ring nonyl ester hydrochloride, the molecular formula of the levo-demethylated benzene ring nonyl ester hydrochloride is shown as (1), the method comprises the following steps: (1) preparing (R)-alpha-phenyl-alpha-cyclopentyl-alpha-methyl glycolate; (2) preparing anintermediate, wherein the intermediate is N-benzyl-3-azabicyclo-[3.3. 1]-non-9 [alpha]-alcohol; and (3) carrying out transesterification on the (R)-alpha-phenyl-alpha-cyclopentyl-alpha-methyl glycolate and N-benzyl-3-azabicyclo-[3.3. 1]-non-9 alpha-ol, removing benzyl on N through catalytic hydrogenation to obtain a crude product of L-demethyl benzene ring nonyl ester, salifying, and recrystallizing to obtain the L-hydrochloric acid demethyl benzene ring nonyl ester. The method is environmentally friendly and suitable for large-scale production.
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Paragraph 0067; 0070; 0071
(2020/09/09)
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- POLYCYCLIC TLR7/8 ANTAGONISTS AND USE THEREOF IN THE TREATMENT OF IMMUNE DISORDERS
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The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as toll-like receptor 7/8 (TLR7/8) antagonists. In Formula (I), Ring A is aryl or heteroaryl; Ring B is aryl or heteroary; and X is C(R4)2, O, NR4, S, S(R4), or S(R4)2.
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Paragraph 00903
(2017/07/06)
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- TBK/IKK INHIBITOR COMPOUNDS AND USES THEREOF
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The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
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Paragraph 1138; 1139
(2017/01/23)
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- INDAZOLE- AND PYRROLOPYRIDINE-DERIVATIVE AND PHARMACEUTICAL USE THEREOF
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The present invention relates to a novel indazole- or pyrrolopyridine-derivative, represented by the formula (1) below, that has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same. Formula (1) [wherein each substituent is as defined in claim 1]
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Page/Page column 206; 207
(2013/02/27)
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- An approach to azabicyclo[ n.3.1]alkanes by double mannich reaction
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Chlorotrimethylsilane-promoted double Mannich annulation of ketones using N,N-bis(methoxymethyl)benzylamine has been explored. It has been shown that the structure of the substrate drastically influenced the outcome of the reaction. The method allows azabicyclo[n.3.1]alkane derivatives (n=2-5) to be obtained in good yields. Georg Thieme Verlag Stuttgart New York.
- Mityuk, Andrey P.,Denisenko, Aleksandr V.,Dacenko, Oleksandr P.,Grygorenko, Oleksandr O.,Mykhailiuk, Pavel K.,Volochnyuk, Dmitriy M.,Shishkin, Oleg V.,Tolmachev, Andrey A.
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experimental part
p. 493 - 497
(2010/04/26)
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- Cyanomethylamines and azidomethylamines: new general methods of the synthesis and transformations
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Simple and efficient methods have been developed to obtain cyanomethylamines and azidomethylamines using reactions of methoxymethylamines with TMSCN and TMSN3, respectively. In the case of dimethylformamide dimethylacetal, only one MeO group wa
- Nabiev, Orudzh G.,Nabizade, Zargalam O.,Kostyanovsky, Remir G.
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body text
p. 281 - 283
(2010/01/18)
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- Substituted tricyclics
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A class of novel tricyclics is disclosed together with the use of such compounds for inhibiting sPLA2mediated release of fatty acids for treatment of conditions such as septic shock.
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- Substituted tricyclics useful in sPLA2 induced diseases
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A class of novel tricyclics is diclosed of the formula (I) : is phenyl or pyridyl wherein the nitrogen is at the 5-, 6-, 7- or 8-position; one of B or D is nitrogen and the other is carbon; is cyclohexenyl, phenyl, pyridyl, wherein the nitrogen is at the 1 -, 2-, or 3position, or a 6-membered hetero-cyclic ring having one heteroatom selected from the group consisting of sulfur or oxygen at the 1-, 2- or 3-position, and nitrogen at the 1 -, 2-, 3- or 4-position; is a double or single bond; together with the use of such compounds for inhibiting SPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.
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