CN101801979A - (r)-n-溴化甲基纳曲酮的晶体形式及其用途 - Google Patents
(r)-n-溴化甲基纳曲酮的晶体形式及其用途 Download PDFInfo
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
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- C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
- C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
- C07D489/04—Salts; Organic complexes
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- C07—ORGANIC CHEMISTRY
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- C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
- C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
- C07D489/08—Oxygen atom
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Abstract
Description
A形式(°2θ) |
11.56 |
13.44 |
13.98 |
15.52 |
16.4 |
17.3 |
19.42 |
20.06 |
20.82 |
21.9 |
A形式(°2θ) |
22.3 |
23.34 |
A形式(°2θ) |
24.42 |
24.84 |
26.38 |
27 |
27.64 |
28.62 |
29.16 |
29.7 |
峰号 | °2θ |
1 | 9.42 |
2 | 11.56 |
3 | 13.44 |
4 | 13.98 |
5 | 15.52 |
6 | 16.4 |
7 | 17.3 |
8 | 17.78 |
9 | 19.42 |
10 | 20.06 |
11 | 20.82 |
峰号 | °2θ |
12 | 21.9 |
13 | 22.3 |
14 | 23.34 |
15 | 24.42 |
16 | 24.84 |
17 | 25.82 |
18 | 26.38 |
峰号 | °2θ |
19 | 27 |
20 | 27.64 |
21 | 28.62 |
22 | 29.16 |
23 | 29.7 |
24 | 30.04 |
25 | 30.5 |
26 | 31.1 |
27 | 31.5 |
28 | 32.28 |
29 | 32.96 |
30 | 34.34 |
31 | 35.1 |
32 | 36 |
峰号 | °2θ |
33 | 36.88 |
34 | 38.16 |
35 | 39.04 |
36 | 39.48 |
峰号 | °2θ |
1 | 9.5 |
2 | 11.35 |
3 | 11.75 |
4 | 13.3 |
5 | 13.6 |
6 | 13.9 |
7 | 15.3 |
8 | 16.85 |
9 | 17.35 |
10 | 17.95 |
11 | 19.5 |
12 | 20.3 |
峰号 | °2θ |
13 | 20.65 |
峰号 | °2θ |
14 | 21.15 |
15 | 21.8 |
16 | 22.75 |
17 | 23 |
18 | 23.3 |
19 | 23.65 |
20 | 23.85 |
21 | 24.7 |
22 | 24.95 |
23 | 26.05 |
24 | 26.35 |
峰号 | °2θ |
25 | 26.75 |
26 | 27.2 |
27 | 28.35 |
28 | 29.25 |
29 | 29.65 |
30 | 30.1 |
31 | 31.1 |
峰号 | °2θ |
32 | 31.25 |
峰号 | °2θ |
33 | 31.8 |
34 | 32.05 |
35 | 32.55 |
36 | 33.4 |
37 | 34.3 |
38 | 34.75 |
B形式(°2θ) |
7.9 |
8.18 |
10.64 |
11.57 |
12.68 |
13.44 |
13.89 |
14.38 |
15.42 |
16.01 |
16.39 |
B形式(°2θ) |
17.18 |
B形式(°2θ) |
19.89 |
20.79 |
21.44 |
21.9 |
23.35 |
24.49 |
24.87 |
25.53 |
29.17 |
峰号 | °2θ |
1 | 7.9 |
2 | 8.18 |
3 | 10.64 |
4 | 11.57 |
5 | 12.68 |
6 | 13.44 |
7 | 13.89 |
8 | 14.38 |
9 | 15.42 |
10 | 16.01 |
峰号 | °2θ |
11 | 16.39 |
12 | 17.18 |
13 | 17.74 |
14 | 18.12 |
15 | 18.47 |
16 | 19.37 |
17 | 19.89 |
18 | 20.3 |
19 | 20.79 |
20 | 21.44 |
峰号 | °28 |
21 | 21.9 |
22 | 22.31 |
23 | 23.35 |
24 | 24.11 |
25 | 24.49 |
26 | 24.87 |
27 | 25.12 |
28 | 25.53 |
29 | 26.33 |
30 | 26.78 |
31 | 27.51 |
峰号 | °28 |
32 | 28.1 |
33 | 29.17 |
34 | 29.69 |
35 | 30.07 |
36 | 30.76 |
37 | 31.04 |
38 | 32.18 |
39 | 32.88 |
40 | 34.33 |
D形式(°2θ) |
7.66 |
D形式(°2θ) |
8.42 |
12.85 |
13.48 |
16.11 |
17.53 |
18.67 |
19.61 |
21.06 |
21.79 |
22.07 |
23.25 |
24.53 |
26.23 |
峰号 | °2θ |
1 | 7.66 |
2 | 8.42 |
3 | 9.43 |
4 | 10.6 |
5 | 11.57 |
6 | 12.85 |
峰号 | °2θ |
7 | 13.48 |
8 | 13.89 |
9 | 14.17 |
10 | 14.38 |
11 | 14.79 |
12 | 15.38 |
13 | 16.11 |
14 | 17.22 |
15 | 17.53 |
16 | 18.67 |
17 | 19.61 |
18 | 20.79 |
19 | 21.06 |
20 | 21.79 |
21 | 22.07 |
22 | 23.25 |
峰号 | °2θ |
23 | 24.53 |
24 | 25.43 |
25 | 25.91 |
26 | 26.23 |
27 | 27.2 |
峰号 | °2θ |
28 | 27.71 |
29 | 28.06 |
30 | 28.55 |
31 | 29.03 |
32 | 29.86 |
33 | 30.56 |
34 | 31.11 |
35 | 32.22 |
36 | 32.7 |
37 | 34.12 |
38 | 34.89 |
39 | 35.82 |
40 | 37 |
41 | 37.86 |
42 | 38.11 |
43 | 38.63 |
44 | 39.46 |
峰号 | °2θ |
1 | 9.1 |
2 | 10.8 |
3 | 11.4 |
4 | 11.6 |
5 | 12.8 |
6 | 14.35 |
7 | 14.8 |
8 | 15.5 |
峰号 | °2θ |
9 | 15.9 |
10 | 16.25 |
11 | 18.25 |
12 | 18.5 |
峰号 | °2θ |
13 | 18.85 |
14 | 19.15 |
15 | 19.7 |
16 | 20.85 |
峰号 | °2θ |
17 | 21.2 |
18 | 21.65 |
19 | 21.85 |
20 | 22 |
21 | 22.65 |
22 | 22.95 |
23 | 23.3 |
24 | 23.6 |
25 | 24.25 |
26 | 25.05 |
27 | 25.3 |
28 | 25.7 |
峰号 | °2θ |
29 | 26 |
30 | 27.05 |
31 | 27.5 |
峰号 | °2θ |
32 | 28.1 |
33 | 28.9 |
34 | 29.5 |
35 | 29.9 |
36 | 30.45 |
37 | 30.75 |
38 | 31.5 |
39 | 31.75 |
40 | 32.15 |
峰号 | °2θ |
1 | 10.58 |
2 | 11.56 |
3 | 13.44 |
4 | 13.88 |
5 | 15.42 |
峰号 | °2θ |
6 | 16.4 |
7 | 18.88 |
8 | 19.34 |
9 | 19.9 |
峰号 | °2θ |
10 | 20.82 |
11 | 21.86 |
12 | 22.22 |
13 | 22.74 |
14 | 23.2 |
15 | 23.84 |
16 | 24.74 |
17 | 25.7 |
18 | 26.96 |
峰号 | °2θ |
19 | 28.7 |
20 | 29.14 |
21 | 29.64 |
22 | 34.02 |
23 | 34.66 |
峰号 | °2θ |
24 | 35.08 |
25 | 35.98 |
26 | 37.14 |
27 | 38.32 |
28 | 39.24 |
溶剂 | 习性/描述 | XRPD结果 |
丙酮 | 白色,形态未知,非双折射 | A |
乙腈 | 白色,形态未知,非双折射 | A |
2-丁酮(MEK) | 白色,形态未知,非双折射 | A |
叔丁基甲醚(MTBE) | 白色,形态未知,非双折射 | A |
乙醇 | 白色,形态未知,非双折射 | A |
乙酸乙酯 | 白色,形态未知,非双折射 | A |
异丙醇 | 白色,形态未知,非双折射 | A |
甲醇 | 类白色,形态未知,非双折射 | B |
甲苯 | 白色,形态未知,非双折射 | A |
溶剂 | 习性/描述 | XRPD结果 |
95%RH | 白色,形态未知,非双折射 | A |
Claims (51)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US92111107P | 2007-03-29 | 2007-03-29 | |
US60/921,111 | 2007-03-29 | ||
PCT/US2008/004116 WO2008121352A2 (en) | 2007-03-29 | 2008-03-28 | Crystal forms of (r) -n-methylnaltrexone bromide and uses thereof |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
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CN2012103612119A Division CN102942572A (zh) | 2007-03-29 | 2008-03-28 | (r)-n-溴化甲基纳曲酮的晶体形式及其用途 |
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Publication Number | Publication Date |
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CN101801979A true CN101801979A (zh) | 2010-08-11 |
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CN2012103612119A Pending CN102942572A (zh) | 2007-03-29 | 2008-03-28 | (r)-n-溴化甲基纳曲酮的晶体形式及其用途 |
CN200880017624A Pending CN101801979A (zh) | 2007-03-29 | 2008-03-28 | (r)-n-溴化甲基纳曲酮的晶体形式及其用途 |
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CN2012103612119A Pending CN102942572A (zh) | 2007-03-29 | 2008-03-28 | (r)-n-溴化甲基纳曲酮的晶体形式及其用途 |
Country Status (10)
Country | Link |
---|---|
US (3) | US20100305323A1 (zh) |
EP (2) | EP3263571B2 (zh) |
JP (5) | JP2010522756A (zh) |
CN (2) | CN102942572A (zh) |
AU (1) | AU2008233133B2 (zh) |
BR (1) | BRPI0809579B8 (zh) |
CA (3) | CA2865389A1 (zh) |
ES (1) | ES2765811T5 (zh) |
MX (2) | MX2009010550A (zh) |
WO (1) | WO2008121352A2 (zh) |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102558190A (zh) * | 2010-12-30 | 2012-07-11 | 天津康鸿医药科技发展有限公司 | (r)-n-溴甲基纳曲酮晶型化合物、其制备方法、组合物及应用 |
CN105753876A (zh) * | 2014-12-15 | 2016-07-13 | 北大方正集团有限公司 | 一种Delta-7溴甲纳曲酮的制备方法 |
CN105753874A (zh) * | 2014-12-15 | 2016-07-13 | 北大方正集团有限公司 | 一种Delta-7甲基纳曲酮甲酸盐及其制备方法 |
CN105777766A (zh) * | 2014-12-15 | 2016-07-20 | 北大方正集团有限公司 | Delta-7溴甲纳曲酮的制备方法 |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
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SI1615646T2 (sl) | 2003-04-08 | 2022-11-30 | Progenics Pharmaceuticals, Inc. | Farmacevtske formulacije vsebujoče metilnatrekson |
AR057035A1 (es) | 2005-05-25 | 2007-11-14 | Progenics Pharm Inc | SíNTESIS DE (R)-N-METILNALTREXONA, COMPOSICIONES FARMACÉUTICAS Y USOS |
AR065877A1 (es) | 2007-03-29 | 2009-07-08 | Progenics Pharm Inc | Antagonoistas del receptor opioide periferico y usos de los mismos |
MX2009010550A (es) | 2007-03-29 | 2009-12-14 | Progenics Pharm Inc | Formas de cristal de bromuro de (r)-n-metilnaltrexona y uso de las mismas. |
WO2009009292A2 (en) * | 2007-07-11 | 2009-01-15 | Mallinckrodt Inc. | Crystalline forms of naltrexone methobromide |
EP2240489A1 (en) | 2008-02-06 | 2010-10-20 | Progenics Pharmaceuticals, Inc. | Preparation and use of (r),(r)-2,2'-bis-methylnaltrexone |
BR112012022873B1 (pt) * | 2010-03-11 | 2021-09-14 | Wyeth Llc | Composição farmacêutica para administração oral compreendendo brometo de metilnaltrexona e dodecil sulfato de sódio |
AU2013203559B2 (en) * | 2010-03-11 | 2015-12-03 | Wyeth Llc | Oral formulations and lipophilic salts of methylnaltrexone |
US10485798B2 (en) | 2012-08-22 | 2019-11-26 | Aptapharma Inc. | Methylnaltrexone nasal formulations, methods of making, and use thereof |
RU2660156C1 (ru) * | 2014-11-04 | 2018-07-05 | Халлибертон Энерджи Сервисез, Инк. | Системы и способы с применением защелкиваемой обсадной трубы в процессе бурения |
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- 2008-03-28 CA CA2865389A patent/CA2865389A1/en not_active Abandoned
- 2008-03-28 ES ES17172002T patent/ES2765811T5/es active Active
- 2008-03-28 EP EP17172002.2A patent/EP3263571B2/en active Active
- 2008-03-28 CA CA002682129A patent/CA2682129A1/en not_active Abandoned
- 2008-03-28 CN CN2012103612119A patent/CN102942572A/zh active Pending
- 2008-03-28 CN CN200880017624A patent/CN101801979A/zh active Pending
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- 2008-03-28 AU AU2008233133A patent/AU2008233133B2/en active Active
- 2008-03-28 US US12/593,615 patent/US20100305323A1/en not_active Abandoned
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-
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Cited By (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102558190A (zh) * | 2010-12-30 | 2012-07-11 | 天津康鸿医药科技发展有限公司 | (r)-n-溴甲基纳曲酮晶型化合物、其制备方法、组合物及应用 |
CN102558190B (zh) * | 2010-12-30 | 2014-10-22 | 天津康鸿医药科技发展有限公司 | (r)-n-溴甲基纳曲酮晶型化合物、其制备方法、组合物及应用 |
CN105753876A (zh) * | 2014-12-15 | 2016-07-13 | 北大方正集团有限公司 | 一种Delta-7溴甲纳曲酮的制备方法 |
CN105753874A (zh) * | 2014-12-15 | 2016-07-13 | 北大方正集团有限公司 | 一种Delta-7甲基纳曲酮甲酸盐及其制备方法 |
CN105777766A (zh) * | 2014-12-15 | 2016-07-20 | 北大方正集团有限公司 | Delta-7溴甲纳曲酮的制备方法 |
CN105777766B (zh) * | 2014-12-15 | 2017-11-24 | 北大方正集团有限公司 | Delta‑7溴甲纳曲酮的制备方法 |
Also Published As
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CA2682129A1 (en) | 2008-10-09 |
US20140004188A1 (en) | 2014-01-02 |
EP2134718A2 (en) | 2009-12-23 |
BRPI0809579B8 (pt) | 2021-05-25 |
BRPI0809579A2 (pt) | 2014-09-23 |
ES2765811T5 (es) | 2024-02-27 |
JP2020079263A (ja) | 2020-05-28 |
JP2018123150A (ja) | 2018-08-09 |
EP3263571A1 (en) | 2018-01-03 |
AU2008233133A1 (en) | 2008-10-09 |
EP3263571B1 (en) | 2019-11-13 |
MX351611B (es) | 2017-10-20 |
JP2010522756A (ja) | 2010-07-08 |
US20160068540A1 (en) | 2016-03-10 |
US20100305323A1 (en) | 2010-12-02 |
EP3263571B2 (en) | 2023-08-23 |
US9879024B2 (en) | 2018-01-30 |
JP2014240400A (ja) | 2014-12-25 |
ES2765811T3 (es) | 2020-06-11 |
US9102680B2 (en) | 2015-08-11 |
WO2008121352A2 (en) | 2008-10-09 |
CA2945356C (en) | 2021-03-23 |
BRPI0809579B1 (pt) | 2020-09-08 |
CA2865389A1 (en) | 2008-10-09 |
CA2945356A1 (en) | 2008-10-09 |
AU2008233133B2 (en) | 2014-03-27 |
WO2008121352A3 (en) | 2009-01-15 |
MX2009010550A (es) | 2009-12-14 |
JP2016196490A (ja) | 2016-11-24 |
BRPI0809579A8 (pt) | 2019-07-02 |
CN102942572A (zh) | 2013-02-27 |
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