486460-21-3Relevant articles and documents
Method for preparing quinoline TGF-β1 inhibitor
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Paragraph 0052; 0070; 0099-0101, (2021/10/27)
The invention belongs to the field of pharmaceutical chemistry, and relates to a preparation method of quinoline TGF-β1 inhibitor, in particular to I ((4 -) propyl 1 - (tetrahydro -3 - pyran - 2H - yl) -4 - pyrazole - 1H -yloxy) -4 - (-7 - (trifluoromethyl) 3 -5 dihydro 6 - [- 1] triazolo [2, 4] pyrazine 4 (8H) 3 - a -7-yl) quinoline or a salt thereof. A process for the preparation of a hydrate, solvate or crystal.
Quinoline compound Preparation method and application thereof
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Paragraph 0047; 0076-0078, (2021/10/27)
The invention belongs to the field of pharmaceutical chemistry, and particularly relates to a quinoline compound, a preparation method thereof and application thereof as reference control product in 4 - ((1 - cyclopropyl -3 - (tetrahydro - 2H - pyran -4 - yl) - 1H - pyrazole -4 -yloxy) -7 - (3 -trifluoromethyl) -5, 6 - dihydro - [1, 2] pyrazino [4, 4] pyrazine 3 - a (8H) -7 -yl) quinoline bulk drug.
Crystal form of quinoline TGF-beta1 inhibitor
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Paragraph 0073; 0102-0104, (2021/10/27)
The invention belongs to the field of medical chemistry, and relates to a crystal form of a quinoline TGF-beta1 inhibitor as well as a preparation method and application of the crystal form, in particular to a crystal form of 4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-yl) oxy)-7-(3-(trifluoromethyl)-5, 6-dihydro-[1, 2, 4] triazolo [4, 3-a] pyrazine-7 (8H)-yl) quinoline as shown in a formula (I) and a preparation method of the crystal form. The crystal form can be used for preparing medicines for treating and/or preventing cancers, tissue hyperplasia diseases, fibrosis or inflammatory diseases.
Medicinal salt of quinoline TGF-beta1 inhibitor and preparation method thereof
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Paragraph 0044; 0073-0075, (2021/10/27)
The invention belongs to the field of medical chemistry, and relates to a medicinal salt of a quinoline TGF-beta1 inhibitor, or a hydrate, a solvate or a crystal thereof, and a preparation method and application thereof. Specifically, the invention relates to a medicinal salt of 4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-yl) oxy)-7-(3-(trifluoromethyl)-5, 6-dihydro-[1, 2, 4] triazolo [4, 3-a] pyrazine-7 (8H)-yl) quinoline as shown in a formula (I), or a hydrate, a solvate or a crystal thereof, and a preparation method thereof. The medicinal salt or the hydrate, the solvate or the crystal thereof can be used for preparing medicines for treating and/or preventing cancers, tissue hyperplasia diseases, fibrosis or inflammatory diseases.
Sitagliptin synthesis method
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Paragraph 0032; 0036; 0037; 0052-0060, (2018/07/07)
The invention discloses a sitagliptin synthesis method, which comprises: carrying out a reaction on a compound represented by a formula IV, (R)-(+)-tert-butyl sulfinamide and hydrogen under the catalysis of a catalyst to obtain a compound represented by a formula V; and carrying out a hydrolysis reaction on the compound represented by the formula V to obtain a compound represented by a formula VI,ie., sitagliptin. According to the present invention, the method has advantages of easily available raw materials, simple steps, high yield and mild reaction conditions, and is suitable for industrial production. The formulas IV, V and VI are defined in the specification.
Methods for Treating Cognitive Disorders Using Inhibitors of Histone Deacetylase
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Paragraph 0716, (2017/01/23)
This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.
Mannich base derivatives of 1,2,4-triazocyclo [4,3-alpha] condensed piperazine as well as preparation method and application of Mannich base derivatives
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Paragraph 0037; 0038; 0039, (2017/08/02)
Mannich base derivatives of 1,2,4-triazocyclo [4,3-alpha] condensed piperazine have the structural formula shown as general formula I in the specification. The Mannich base derivatives have the following advantages: according to a preparation method, substitutive derivatives are prepared from 1,2,4-triazocyclo [4,3-alpha] condensed piperazine by introducing different substituent groups into 1,2,4-triazocyclo [4,3-alpha] condensed piperazine, a novel structure with higher biological activity is discovered, novel structure-activity relationship and biological activity laws are summarized; the prepared Mannich base derivatives have higher bactericidal activity and herbicidal activity, have high in-vitro inhibitory activity for plant pathogens such as fusarium wilt pathogen of cucumbers, cercospora arachidicola, Macrophoma kawatsukai, rhizoctonia cerealis pathogen, alternaria solani of tomatoes, gibberella zeae and the like and can be used for controlling fungus and weed damage to plants, and bactericidal or herbicidal composition further comprises a vector acceptable in agriculture, forestry and hygiene.
BETA-AMINO HETEROCYCLIC DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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Paragraph 0209, (2015/12/30)
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
AMINOQUINAZOLINE DERIVATIVES AND THEIR SALTS AND METHODS OF USE
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Paragraph 0283-0284, (2014/08/19)
The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
Exploring the unexplored practical and alternative synthesis of 3-(trifluoromethyl)-triazolopiperazine the key intermediate for Sitagliptin
Nitlikar, Lakshmikant H.,Darandale, Sunil N.,Shinde, Devanand B.
, p. 348 - 352 (2013/07/26)
The practical synthesis of 3-(trifluoromethyl)-triazolopiperazine the key intermediate of Sitagliptin and 3-(trifluoromethyl)-triazolopyridine was carried out employing industrially feasible transformations. The other advantage of this method is the new environment friendly approach to synthesize triazolopiperazine and triazolopyridines by eliminating the commonly used trifluoroacetic anhydride and polyphosphoric acid.