US2011086896A1PendingUtilityA1
Crystalline and Stable Form of Andolast
Est. expiryApr 10, 2026(expired)· nominal 20-yr term from priority
Inventors:Antonio GiordaniAntonino SantoroPaolo SeninMatteo GhirriFrancesco MakovecPaola GilottaWalter PerisLucio Claudio Rovati
A61P 37/08A61P 11/00A61P 11/06C07D 257/04
40
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Claims
Abstract
Described is a new crystalline Form A of Andolast disodium salt, triclinic, displaying a thermal event at 98-112° C. and melting with decomposition at about 400° C. (DSC). Andolast disodium Form A is a not hygroscopic solid, surprisingly stable to several humidity conditions in a temperature range acceptable for ordinary storage conditions. In addition its stability allows both chemical manufacturing and pharmaceutical manufacturing process consistency and reproducibility under conditions more viable and less expensive when compared to those used for highly hygroscopic solids.
Claims
exact text as granted — not AI-modified1 - 18 . (canceled)
19 . A method of pharmacologically treating respiratory tract diseases comprising administering crystalline Form A of N-4-(1H-tetrazol-5-yl)phenyl-4-(1H-tetrazol-5-yl)benzamide disodium salt as a powder for inhalation, wherein N-4-(1H-tetrazol-5-yl)phenyl-4-(1H-tetrazol-5-yl)benzamide disodium salt pentahydrate Form A is characterized by the following X-ray powder diffraction pattern expressed in terms of 2θ, d-spacings, and relative intensities, when CuKa radiation is used
2θ
d-value (Å)
Intensity %
14.45
6.10
23
22.10
4.02
64
22.82
3.89
45
23.63
3.76
100
24.17
3.68
41
27.10
3.29
58
27.42
3.25
31
28.59
3.12
22
30.28
2.95
39
34.06
2.63
21.
20 . A method of pharmacologically treating allergic diseases comprising administering crystalline Form A, as defined in claim 1 , of N-4-(1H-tetrazol-5-yl)phenyl-4-(1H-tetrazol-5-yl)benzamide disodium salt as a powder for inhalation, wherein N-4-(1H-tetrazol-5-yl)phenyl-4-(1H-tetrazol-5-yl)benzamide disodium salt pentahydrate Form A is characterized by the following X-ray powder diffraction pattern expressed in terms of 2θ, d-spacings, and relative intensities, when CuKa radiation is used
2θ
d-value (Å)
Intensity %
14.45
6.10
23
22.10
4.02
64
22.82
3.89
45
23.63
3.76
100
24.17
3.68
41
27.10
3.29
58
27.42
3.25
31
28.59
3.12
22
30.28
2.95
39
34.06
2.63
21.
21 . A method of pharmacologically treating asthma comprising administering crystalline Form A, as defined in claim 1 , of N-4-(1H-tetrazol-5-yl)phenyl-4-(1H-tetrazol-5-yl)benzamide disodium salt as a powder for inhalation, wherein N-4-(1H-tetrazol-5-yl)phenyl-4-(1H-tetrazol-5-yl)benzamide disodium salt pentahydrate Form A is characterized by the following X-ray powder diffraction pattern expressed in terms of 2θ, d-spacings, and relative intensities, when CuKa radiation is used
2θ
d-value (Å)
Intensity %
14.45
6.10
23
22.10
4.02
64
22.82
3.89
45
23.63
3.76
100
24.17
3.68
41
27.10
3.29
58
27.42
3.25
31
28.59
3.12
22
30.28
2.95
39
34.06
2.63
21.
22 . A method of pharmacologically treating Chronic Obstructive Pulmonary Disease (COPD) comprising administering crystalline Form A, as defined in claim 1 , of N-4-(1H-tetrazol-5-yl)phenyl-4-(1H-tetrazol-5-yl)benzamide disodium salt as a powder for inhalation, wherein N-4-(1H-tetrazol-5-yl)phenyl-4-(1H-tetrazol-5-yl)benzamide disodium salt pentahydrate Form A is characterized by the following X-ray powder diffraction pattern expressed in terms of 2θ, d-spacings, and relative intensities, when CuKa radiation is used
2θ
d-value (Å)
Intensity %
14.45
6.10
23
22.10
4.02
64
22.82
3.89
45
23.63
3.76
100
24.17
3.68
41
27.10
3.29
58
27.42
3.25
31
28.59
3.12
22
30.28
2.95
39
34.06
2.63
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