IP Library Granted Patent US 12,503,469
Granted Patent B2
US 12,503,469 · App. 17/526,129 · Granted Dec 23, 2025

Forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3-4-b]pyridino-3-yl]pyrimidino-5-yl} methyl carbamate

Inventors: Birgit Keil (Duesseldorf, DE); Franz-Josef Mais (Duesseldorf, DE); Winfried Joentgen (Cologne, DE); Alfons Grunenberg (Wuppertal, DE)
Assignee: Adverio Pharma GmbH
C07D471/04A61K31/519
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Quick Facts
Patent No.
US 12,503,469
App. No.
17/526,129
Granted
Dec 23, 2025
Kind
B2
Abstract

This present invention relates to forms of methyl {4.6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3.4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I, Modification II, mono-DMSO solvate, sesqui-DMSO solvate and ¼-ethyl acetated solvate.

Claims (8)

1 . A pharmaceutical composition comprising a compound of the formula (I)

and a pharmaceutically acceptable carrier, in which 100 percent by weight relative to the total weight of all forms of the compound of formula (I) in the composition is in crystalline form of Modification (I), wherein the compound of the formula (I) is characterized by an X-Ray powder diffractogram comprising peak maxima of the 2 Theta angle of 6.7, 9.1 and 17.8.

2 . A method for the treatment of pulmonary arterial hypertension comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 1 to a patient in need thereof.

3 . A method for the treatment of pulmonary hypertension associated with thromboembolism (CTEPH) comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 1 to a patient in need thereof.

4 . A method for the treatment of pulmonary arterial hypertension comprising administering a composition comprising a therapeutically effective amount of a compound of the formula (I)

and a pharmaceutically acceptable carrier, in which more than 90 percent by weight relative to the total weight of all forms of the compound of formula (I) in the composition is in the crystalline form of Modification I, to a patient in need thereof, wherein the compound of the formula (I) has an X-Ray powder diffractogram comprising peak maxima of the 2 Theta angle of 6.7, 9.1 and 17.8.

5 . A method for the treatment of pulmonary hypertension associated with thromboembolism (CTEPH) comprising administering a composition comprising a therapeutically effective amount of a compound of the formula (I)

and a pharmaceutically acceptable carrier, in which more than 90 percent by weight relative to the total weight of all forms of the compound of formula (I) in the composition is in the crystalline form of Modification I, to a patient in need thereof, wherein the compound of the formula (I) has an X-Ray powder diffractogram comprising peak maxima of the 2 Theta angle of 6.7, 9.1 and 17.8.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 1, 2025
From: KEIL, BIRGIT; MAIS, FRANZ-JOSEF; JOENTGEN, WINFRIED; GRUNENBERG, ALFONS
To: BAYER PHARMA AKTIENGESELLSCHAFT
Reel/Frame 072436/0131 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 1, 2025
From: BAYER PHARMA AKTIENGESELLSCHAFT
To: BAYER INTELLECTUAL PROPERTY GMBH
Reel/Frame 072988/0097 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 1, 2025
From: BAYER INTELLECTUAL PROPERTY GMBH
To: ADVERIO PHARMA GMBH
Reel/Frame 072988/0106 →