- Preparation method 2 - chloro -3 - bromoaniline
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The invention discloses a preparation method of 2 - chloro -3 - bromoaniline, and the specific steps of the preparation method are as follows: (1) the compound II and the bromosuccinimide are subjected to electrophilic substitution reaction to generate the compound III. (2) The sulfonic acid group of the compound III was removed to give compound IV. (3) Compound IV is reduced to compound I with a safety powder, i.e. said 2 - chloro -3 - bromoaniline. To the invention, 4 - chlorine -3 - nitrobenzene sulfonic acid is used as a starting raw material in a full synthetic route process, reagents with large toxicity and large pollution are avoided, and meanwhile, the raw materials are low in price and higher in yield.
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- PREPARATION AND APPLICATION OF CLASS OF N-CONTAINING HETEROCYCLIC COMPOUNDS HAVING IMMUNOREGULATORY FUNCTION
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The present invention discloses the preparation and application of heterocyclic compound having immunoregulatory function. Specifically, the present invention discloses a compound having a structure according to Formula I, wherein the definition of each g
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Paragraph 0066-0068
(2021/06/10)
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- COUMARIN-LIKE CYCLIC COMPOUND AS MEK INHIBITOR AND USE THEREOF
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Disclosed are a class of coumarin-like cyclic compounds as MEK inhibitors and pharmaceutical compositions comprising the compounds, and the use of same in the preparation of a drug for treating MEK-related diseases. Particularly disclosed are compounds as shown in formula (I) and pharmaceutically acceptable salts thereof or tautomers thereof.
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Paragraph 0205-0207
(2020/05/30)
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- NOVEL HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS
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This invention relates to certain novel pyrazine derivatives (Formula I) as SHP2 inhibitors which is shown as formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, this invention is directed to fused heterocycl
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Paragraph 0091; 0094
(2019/11/29)
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- SUBSTITUTED QUINAZOLINE COMPOUNDS AND THEIR USE AS INHIBITORS OF G12C MUTANT KRAS, HRAS AND/OR NRAS PROTEINS
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Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R, R1, R2a, R2b, R2c, A, B, L1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
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- NOVEL HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS
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Provided are certain pyrazine derivatives (I) as SHP2 inhibitors which is shown as formula (I), their synthesis and their use for treating a SHP2 mediated disorder. More particularly, provided are fused heterocyclic derivatives useful as inhibitors of SHP
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Page/Page column 30
(2018/01/19)
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- INHIBITORS OF KRAS G12C
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Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
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- Approaches to the synthesis of 2,3-dihaloanilines. Useful precursors of 4-functionalized-1 H-indoles
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2,3-Dihaloanilines have been proved as useful starting materials for synthesizing 4-halo-1H-indoles. Subsequent or in situ functionalization of the prepared haloindoles allows the access to a wide variety of 2,4- or 2,3,4-regioselectively functionalized indoles in good overall yields. As no efficient synthetic routes to 2,3-dihaloanilines have been described in the literature, different approaches to the preparation of these 1,2,3-functionalized aromatic precursors are now presented. The most general one involves a Smiles rearrangement from the corresponding 2,3-dihalophenols and allows the preparation of 2,3-dihaloanilides in a straightforward and synthetically useful manner.
- Guilarte, Veronica,Castroviejo, M. Pilar,Garcia-Garcia, Patricia,Fernandez-Rodriguez, Manuel A.,Sanz, Roberto
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p. 3416 - 3437
(2011/06/28)
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- Compounds and Compositions as Protein Kinase Inhibitors
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The present invention provides compounds of Formula I or II: wherein R1, R1b, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds of Formula (I) or (II) and pharmaceutical compositions thereof are useful for the treatment of B-Raf-associated diseases.
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- FUSED PYRIMIDINE DERIVATIVE AND USES THEREOF
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A compound represented by the formula (I) wherein ring A is a 5-membered aromatic heterocycle optionally having substituent(s), R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s), W is an oxygen atom or a sulfur atom, X1 and X2 may be the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s) or a heterocyclic group, or, X1 and X2 in combination optionally form an oxygen atom, a sulfur atom or =NR2, ring B is an aromatic ring optionally further having substituent(s), Y is a bond, C1-6 alkylene C2-6 alkenylene or C2-6 alkynylene, optionally having substituent(s), and Z is a group represented by formula: -SOnR3, or a group represented by formula: -COR4, or a salt thereof, is useful as a pharmaceutical agent having GnRH antagonistic action.
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Page/Page column 72
(2008/06/13)
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- 4 AND 5-Halo substituted 2-indanamine compounds
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2-Indanamine compounds having 4 and 5-halo substituents are inhibitors of phenylethanolamine N-methyltransferase.
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