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ES2660146T3 - Sales del inhibidor de cdk - Google Patents

Sales del inhibidor de cdk Download PDF

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Publication number
ES2660146T3
ES2660146T3 ES10715240.7T ES10715240T ES2660146T3 ES 2660146 T3 ES2660146 T3 ES 2660146T3 ES 10715240 T ES10715240 T ES 10715240T ES 2660146 T3 ES2660146 T3 ES 2660146T3
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Prior art keywords
compound
salt
salts
maleate
cdk inhibitor
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Inventor
Massimo Zampieri
Annalisa Airoldi
Maria Gioia Fornaretto
Maria Gabriella Brasca
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Nerviano Medical Sciences SRL
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Nerviano Medical Sciences SRL
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Una sal del compuesto 125 que tiene la fórmula siguiente:**Fórmula** seleccionada de maleato, malonato y glicolato, que comprenden polimorfos e hidratos de estos.

Description

imagen1
imagen2
imagen3
imagen4
propanol) y se convierte en la Forma I o III mediante el efecto de las condiciones de secado o exposición a condiciones de temperatura y humedad acentuadas (por ejemplo, almacenamiento a 40°C/75% de RH).
La Forma III es una forma de cristal de alto punto de fusión de la sal de maleato del compuesto 125 que se caracteriza
5 como una forma hidratada que muestra adsorción reversible de aproximadamente 1 mol de agua en condiciones ambientales (por ejemplo, 25°C/60% de RH). La absorción de aproximadamente 3,0÷3,5% a 25°C y 90% de humedad relativa (RH) es reversible al disminuir la RH a aproximadamente 20% ala misma temperatura.
Como un aspecto adicional, se ha encontrado que la sal de maleato del compuesto 125puede obtenerse como un sólido 10 cristalino en las relaciones molares de 0,5:1, 1:1 y 2:1.
La sal de glicolato del compuesto 125 y la sal de malonato del compuesto 125 son ligeramente higroscópicas, mostrando ambas una absorción de agua reversible de aproximadamente 2,5% a 25°C/90% de RH.
15 Las sales del compuesto 125 muestran buena solubilidad, en particular, la solubilidad de las sales de maleato, malonato y glicolato en una solución de dextrosa al 0,5% es de aproximadamente 10 mg/mL o superior.
Además de la ventaja de exhibir alta solubilidad en agua, las sales del compuesto 125, en particular, las sales de maleato, malonato, glicolato, son también particularmente adecuadas para que se fabriquen reproduciblemente en una 20 relación de ácido/base clara.
Este hallazgo hace que estas sales sean particularmente adecuadas para su uso en las formulaciones líquidas para formulaciones tanto orales, así comointravenosas.
25 Tabla1 -Descripcióndelaspropiedadesdeestadosólidodelassalesyformasdebaselibredel compuesto 125.
30
35
40
45
50
55
60
65
Compuesto 125 Sal (*)
Forma crsitalina Figura PXRD Tabla PXRD Picos significativos PXRD (2zeta, grado) (**) Figura de DSC
Maleato
I 11 7 5,3, 6,0, 11,9, 12,7, 13,5, 14,5, 17,9, 19,4, 20,9, 22,9, 23,2, 24,7 20
Maleato
II 2B, 12 8 4,8, 9,6, 11,6, 15,7, 16,0, 16,7, 19,3, 20,9, 21,3, 22,1, 23,3, 27,7, 17F
Maleato
III 5D, 13 9 6,0, 11,8, 12,3, 13,3, 14,3, 16,3, 17,8, 20,8, 22,8, 24,3, 26,4, 27,6 20
Malonato
I 1E, 7 3 11,5, 12,4, 14,3, 15,8, 18,8, 20,9, 21,8, 22,7, 23,0, 16B
imagen5
imagen6 imagen7 imagen8 24,8 imagen9
Glicolato
I 1D, 6 2 6,6, 11,8, 12,2, 12,7, 16,1, 17,5, 19,4, 21,9, 23,6, 23,9, 25,9, 27,8 17B
Triclorhidrato
I 1B, 4B, 8 4 7,7, 8,2, 10,6, 11,1, 17,6, 22,1, 23,2, 24,4, 25,1, 26,4,28,1,31,9 18A
Diclorhidrato
I 4C, 9 5 7,7, 8,1, 11,0, 22,1, 26,4, 25,1, 31,8, 24,3, 28,1, 10,6, 17,6, 23,0 18B
Clorhidrato
I 4D, 10 6 4,6, 5,2, 5,4, 8,1, 8,4, 9,4, 10,2, 10,6, 14,6, 21,0, 23,5, 24,9 18C
Base libre
I 1A, 2A, 3A, 4A, 14 10 5,6, 9,3, 10,9, 11,4, 14,4, 14,5, 17,3, 19,3, 19,6, 21,8, 22,4, 25,5 16A, 17A
Base libre
II 15 11 6,1, 10,3, 11,4, 11,9, 12,6, 14,5, 18,5, 18,9, 20,3, 23,0, 24,8, 25,7 No disponible
6
imagen10
imagen11
imagen12
imagen13
imagen14
imagen15
imagen16
Tabla 2 -Compuesto 125, sal de glicolato
Posición (grado)
Intensidad (CPS) Intensidad relativa
6, 6
525, 9 16, 5
9, 7
504, 5 15, 8
10, 6
277, 1 8, 7
10, 9
190, 9 6, 0
11, 8
2122, 7 66, 6
12, 2
1133, 9 35, 6
12, 7
852, 3 26, 7
13, 1
130, 6 4, 1
13, 8
74, 4 2, 3
15, 6
122, 5 3, 8
16, 1
525, 5 16, 5
16, 5
516, 8 16, 2
17, 3
198, 8 6, 2
17, 5
720, 2 22, 6
18, 1
86, 9 2, 7
19, 4
3187, 8 100, 0
20, 1
312, 9 9, 8
20, 4
355, 5 11, 2
20, 7
99, 6 3, 1
21, 0
189, 7 6, 0
21, 2
280, 3 8, 8
21, 9
1167, 1 36, 6
22, 5
386, 5 12, 1
22, 8
240, 3 7, 5
23, 6
1620, 6 50, 8
23, 9
1419, 2 44, 5
25, 9
1221, 0 38, 3
27, 8
859, 2 27, 0
28, 3
164, 6 5, 2
29, 2
152, 9 4, 8
30, 3
196, 2 6, 2
30, 7
203, 4 6, 4
31, 1
107, 6 3, 4
32, 5
156, 7 4, 9
33, 1
167, 6 5, 3
14
imagen17
-Compuesto 125, sal de triclorhidrato, Forma I
Posición (grado)
Intensidad (CPS) Intensidad relativa
5, 4
183, 0 11, 1
7, 7
1483, 0 90, 0
8, 2
1642, 0 99, 6
10, 6
245, 7 14, 9
11, 1
1648, 3 100, 0
12, 2
95, 6 5, 8
13, 1
234, 0 14, 2
14, 6
138, 4 8, 4
15, 3
76, 9 4, 7
15, 6
72, 7 4, 4
16, 2
25, 6 1, 6
17, 3
182, 0 11, 0
17, 6
316, 5 19, 2
18, 4
37, 0 2, 3
20, 3
141, 4 8, 6
21, 2
196, 6 11, 9
21, 6
48, 8 3, 0
22, 1
561, 9 34, 1
22, 6
182, 1 11, 1
23, 1
195, 4 11, 9
23, 2
244, 8 14, 9
24, 4
268, 1 16, 3
24, 9
167, 1 10, 1
25, 1
318, 6 19, 3
25, 4
160, 4 9, 7
26, 4
641, 3 38, 9
28, 1
343, 9 20, 9
28, 6
104, 3 6, 3
30, 9
229, 2 13, 9
31, 9
387, 6 23, 5
33, 5
98, 6 6, 0
16
Tabla 5 -Compuesto 125, sal de diclorhidrato
Posición (grado)
Intensidad (CPS) Intensidad relativa
5, 3
236, 3 12, 0
7, 7
1965, 7 100, 0
8, 1
1922, 5 97, 8
10, 6
288, 0 14, 7
11, 0
1694, 4 86, 2
13, 1
263, 9 13, 4
14, 6
210, 1 10, 7
15, 3
77, 1 3, 9
15, 5
107, 8 5, 5
17, 3
139, 2 7, 1
17, 6
279, 9 14, 2
18, 5
56, 2 2, 9
20, 1
47, 1 2, 4
20, 3
175, 7 8, 9
21, 2
185, 8 9, 5
21, 5
115, 8 5, 9
22, 1
545, 4 27, 8
22, 6
233, 9 11, 9
23, 0
270, 8 13, 8
23, 2
240, 9 12, 3
23, 4
91, 7 4, 7
24, 3
312, 2 15, 9
24, 9
200, 5 10, 2
25, 1
523, 9 26, 7
25, 4
209, 4 10, 7
26, 4
526, 5 26, 8
27, 2
83, 2 4, 2
28, 1
296, 7 15, 1
28, 5
169, 9 8, 6
30, 8
258, 4 13, 1
31, 8
445, 9 22, 7
33, 5
155, 1 7, 9
17
Tabla 6 -Compuesto 125, sal de clorhidrato
imagen18
Posición (grado)
Intensidad (CPS) Intensidad relativa
4, 6
191, 7 53, 9
5, 2
201, 1 56, 6
5, 4
172, 8 48, 6
7, 6
49, 7 14, 0
8, 1
355, 4 100, 0
8, 4
111, 5 31, 4
9, 4
112, 8 31, 7
10, 2
115, 5 32, 5
10, 6
176, 1 49, 5
11, 1
73, 5 20, 7
12, 0
23, 8 6, 7
12, 4
70, 4 19, 8
13, 5
76, 4 21, 5
13, 8
59, 7 16, 8
14, 0
74, 2 20, 9
14, 6
110, 4 31, 1
14, 8
45, 2 12, 7
16, 7
20, 2 5, 7
17, 0
40, 7 11, 5
17, 5
51, 5 14, 5
18, 7
43, 6 12, 3
19, 2
41, 4 11, 7
20, 1
44, 4 12, 5
21, 0
151, 9 42, 7
23, 5
159, 6 44, 9
24, 0
36, 4 10, 3
24, 9
221, 1 62, 2
26, 2
69, 6 19, 6
26, 9
32, 9 9, 3
27, 9
37, 3 10, 5
28, 4
26, 1 7, 3
18
imagen19
imagen20
Tabla 9 -Compuesto 125, sal demaleato FormaIII
imagen21
Posición (grado)
Intensidad (CPS) Intensidad relativa
5, 1
222, 0 9, 1
6, 0
441, 1 18, 1
8, 3
68, 2 2, 8
9, 3
43, 0 1, 8
10, 0
79, 3 3, 3
11, 2
246, 4 10, 1
11, 8
280, 8 11, 5
12, 3
373, 9 15, 3
13, 3
543, 8 22, 3
14, 3
414, 3 17, 0
14, 7
60, 2 2, 5
15, 9
204, 0 8, 4
16, 3
520, 7 21, 3
16, 9
126, 6 5, 2
17, 8
668, 4 27, 4
18, 2
173, 2 7, 1
19, 4
255, 3 10, 5
19, 8
250, 7 10, 3
20, 2
223, 7 9, 2
20, 8
773, 5 31, 7
21, 8
144, 8 5, 9
22, 8
2442, 6 100, 0
23, 7
271, 2 11, 1
24, 3
275, 9 11, 3
24, 7
81, 4 3, 3
24, 9
204, 9 8, 4
25, 9
115, 9 4, 7
26, 4
390, 9 16, 0
27, 6
333, 8 13, 7
28, 1
140, 8 5, 8
31, 1
85, 5 3, 5
32, 0
73, 8 3, 0
21
imagen22
imagen23
22
imagen24
imagen25
imagen26

Claims (1)

  1. imagen1
ES10715240.7T 2009-04-29 2010-04-23 Sales del inhibidor de cdk Active ES2660146T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09159030 2009-04-29
EP09159030 2009-04-29
PCT/EP2010/055463 WO2010125004A1 (en) 2009-04-29 2010-04-23 Cdk inhibitor salts

Publications (1)

Publication Number Publication Date
ES2660146T3 true ES2660146T3 (es) 2018-03-21

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US (1) US8586598B2 (es)
EP (1) EP2424868B1 (es)
JP (1) JP5801285B2 (es)
CN (1) CN102428086B (es)
AR (1) AR076433A1 (es)
ES (1) ES2660146T3 (es)
TW (1) TW201043631A (es)
WO (1) WO2010125004A1 (es)

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US8586598B2 (en) 2013-11-19
AR076433A1 (es) 2011-06-08
US20120041007A1 (en) 2012-02-16
JP5801285B2 (ja) 2015-10-28
HK1169408A1 (en) 2013-01-25
EP2424868A1 (en) 2012-03-07
WO2010125004A1 (en) 2010-11-04
TW201043631A (en) 2010-12-16
JP2012525345A (ja) 2012-10-22
CN102428086A (zh) 2012-04-25
EP2424868B1 (en) 2018-01-10

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