US 11,236,041 B2Granted

Type-G crystal form of fenolamine, preparation method, composition and use thereof

AssigneesInstitute of Mataria Medica, Chinese Academy of Medical Sciences, Shijiazhuang Yiling Pharmaceutical Co., Ltd.

InventorsYang Lv, Shiying Yang, Gengtao Liu, Dan Zhang, Xiuqi Bao, Ping Xie

Life of this patent

Estimating the term…

Loading patent…

Abstract

The present invention discloses a type-G crystal form of fenolamine, a preparation method thereof, and a composition and use thereof. In particular, disclosed is a type-G crystal form of the fenolamine compound (chemical name: trans-2-(2,5-dimethoxyphenyl)-3-(4-hydroxy-3-methoxyphenyl)-N-(4-hydroxyphenylethyl)acrylamide, a preparation method thereof, and a composition and use thereof. Specifically, the present invention discloses the presence of a solid of a type-G fenolamine crystal form in solid state; a method for preparing the solid of type-G crystal form; and use of the solid of the type-G fenolamine crystal form as a pharmaceutical active ingredient in the manufacture of a medicament for prevention and treatment of Parkinson's disease (PD), improvement of learning and memory disorder, and treatment of memory loss and Alzheimer's disease (AD).

Claims20

Dependent claims

A solid of a type-G fenolamine crystal form, wherein the solid of the type-G crystal form is a fenolamine hydrate and, by using powder X-ray diffraction analysis under CuKα radiation experimental conditions, has diffraction peaks at positions with 2-Theta values or d values and diffraction peaks with relative intensity peak height values or peak area values as shown below:

2-Theta
d (Å)
Height %
Area %
Peak
±0.2°
±0.2 Å
±10%
±10%
1
7.3
12.2
20
29
2
7.8
11.4
15
18
3
9.2
9.6
10
11
4
10.7
8.2
21
23
5
11.3
7.8
34
58
6
11.6
7.6
29
48
7
12.6
7.0
7
8
8
13.1
6.7
47
64
9
13.6
6.5
13
18
10
15.0
5.9
10
11
11
15.6
5.7
5
4
12
17.6
5.0
33
45
13
18.3
4.8
70
72
14
19.6
4.5
37
57
15
19.9
4.5
41
76
16
20.4
4.3
78
84
17
20.8
4.3
21
30
18
22.1
4.0
16
15
19
22.7
3.9
4
2
20
23.4
3.8
100
100
21
23.9
3.7
12
14
22
24.7
3.6
51
45
23
25.5
3.5
69
82
24
26.5
3.4
6
6
25
27.2
3.3
9
10
26
27.9
3.2
7
6
27
28.6
3.1
12
13
28
29.1
3.1
12
19
29
30.5
2.9
8
9
30
31.5
2.8
5
5
31
32.9
2.7
6
14
32
33.9
2.6
3
4
33
34.3
2.6
3
5
34
34.9
2.6
1
1
35
35.6
2.5
4
6
36
37.3
2.4
3
3
37
38.1
2.4
6
8
38
40.1
2.2
4
8
39
41.5
2.2
2
2
40
42.3
2.1
6
5

206 more elements

Dependencies are inferred from the claim text.

Facts

Application: 16/629,950Filed 7 Sep 2018
Priority: CN 201710560703.311 Jul 2017
Published: US 2020/0157042 A121 May 2020
Granted: 1 Feb 2022
Term ends: Not estimatedThe source records don’t support an estimate.

Classification17 codes

C07C 233/22
With the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom: having the carbon atom of…
A61K 9/2009
Excipients; Inactive ingredients: inorganic compounds
A61K 9/2013
Excipients; Inactive ingredients: organic compounds, e.g. phospholipids, fats
A61K 9/2018
Organic compounds, e.g. phospholipids, fats: sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates