JP4875205B2 - チアジアゾール誘導体の安定な製剤 - Google Patents
チアジアゾール誘導体の安定な製剤 Download PDFInfo
- Publication number
- JP4875205B2 JP4875205B2 JP2010516173A JP2010516173A JP4875205B2 JP 4875205 B2 JP4875205 B2 JP 4875205B2 JP 2010516173 A JP2010516173 A JP 2010516173A JP 2010516173 A JP2010516173 A JP 2010516173A JP 4875205 B2 JP4875205 B2 JP 4875205B2
- Authority
- JP
- Japan
- Prior art keywords
- dimethyl
- pharmaceutical composition
- less
- buffer
- tartrate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Description
以下の製剤実施例は例示であり、本発明の範囲を限定することを意図しない。
Claims (10)
- N−{4−(2,2−ジメチル−プロピオニル)−(5R)−5−[(2−エチルアミノ−エタンスルホニルアミノ)−メチル]−5−フェニル−4,5−ジヒドロ−[1,3,4]チアジアゾール−2−イル}−2,2−ジメチル−プロピオンアミド、以下からなる群:酒石酸塩、リン酸塩、クエン酸塩、メシラート、リン酸ナトリウム、および硫酸ナトリウムから選択される緩衝液および/または塩、ならびに水溶液中で薬理学的に許容できる担体、希釈剤または賦形剤を含む、医薬組成物であって、前記組成物のpHが5.4未満であり、かつ2.0より大きく、N−{4−(2,2−ジメチル−プロピオニル)−(5S)−5−[(2−エチルアミノ−エタンスルホニルアミノ)−メチル]−5−フェニル−4,5−ジヒドロ−[1,3,4]チアジアゾール−2−イル}−2,2−ジメチル−プロピオンアミドの含有量が2.0%を超えない、キラル変換に安定である、医薬組成物。
- 前記緩衝液および/または塩は、酒石酸塩、リン酸塩、クエン酸塩およびリン酸ナトリウムから選択される、請求項1に記載の医薬組成物。
- 前記緩衝液および/または塩は、酒石酸塩およびリン酸ナトリウムから選択される、請求項2に記載の医薬組成物。
- 前記緩衝液および/または塩は、酒石酸塩である、請求項3に記載の医薬組成物。
- 前記組成物のpHは、4.2未満であり、かつ2.0より大きい、請求項1〜4のいずれか1項に記載の医薬組成物。
- N−{4−(2,2−ジメチル−プロピオニル)−(5R)−5−[(2−エチルアミノ−エタンスルホニルアミノ)−メチル]−5−フェニル−4,5−ジヒドロ−[1,3,4]チアジアゾール−2−イル}−2,2−ジメチル−プロピオンアミド、以下からなる群:酒石酸塩、リン酸塩、クエン酸塩、メシラート、リン酸ナトリウム、および硫酸ナトリウムから選択される緩衝液および/または塩、ならびに薬理学的に許容できる担体、希釈剤または賦形剤を含む、凍結乾燥医薬組成物であって、水性希釈剤で希釈した場合、5.4未満かつ2.0より大きいpHを有し、N−{4−(2,2−ジメチル−プロピオニル)−(5S)−5−[(2−エチルアミノエタンスルホニルアミノ)−メチル]−5−フェニル−4,5−ジヒドロ−[1,3,4]チアジアゾール−2−イル}−2,2−ジメチル−プロピオンアミドの含有量が2.0%を超えない、溶液製剤が得られ、キラル変換に安定である、凍結乾燥医薬組成物。
- 前記緩衝液および/または塩は、酒石酸塩、リン酸塩、クエン酸塩およびリン酸ナトリウムから選択される、請求項6に記載の凍結乾燥医薬組成物。
- 前記緩衝液および/または塩は、酒石酸塩およびリン酸ナトリウムから選択される、請求項7に記載の凍結乾燥医薬組成物。
- 前記緩衝液および/または塩は、酒石酸塩である、請求項8に記載の凍結乾燥医薬組成物。
- 前記溶液製剤のpHは、4.2未満であり、かつ2.0より大きい、請求項6〜9のいずれか1項に記載の凍結乾燥医薬組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US94926807P | 2007-07-12 | 2007-07-12 | |
US60/949,268 | 2007-07-12 | ||
PCT/US2008/069301 WO2009009470A1 (en) | 2007-07-12 | 2008-07-07 | Stable formulations of thiadiazole derivatiive |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2010533190A JP2010533190A (ja) | 2010-10-21 |
JP2010533190A5 JP2010533190A5 (ja) | 2011-06-30 |
JP4875205B2 true JP4875205B2 (ja) | 2012-02-15 |
Family
ID=39735000
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2010516173A Expired - Fee Related JP4875205B2 (ja) | 2007-07-12 | 2008-07-07 | チアジアゾール誘導体の安定な製剤 |
Country Status (28)
Country | Link |
---|---|
US (1) | US8222284B2 (ja) |
EP (1) | EP2178508B1 (ja) |
JP (1) | JP4875205B2 (ja) |
KR (1) | KR101188036B1 (ja) |
CN (1) | CN101730525A (ja) |
AR (1) | AR067472A1 (ja) |
AU (1) | AU2008275258A1 (ja) |
BR (1) | BRPI0814039A2 (ja) |
CA (1) | CA2694277C (ja) |
CL (1) | CL2008001996A1 (ja) |
CO (1) | CO6270304A2 (ja) |
CR (1) | CR11210A (ja) |
DO (1) | DOP2010000004A (ja) |
EA (1) | EA016861B1 (ja) |
EC (1) | ECSP109864A (ja) |
ES (1) | ES2401477T3 (ja) |
GT (1) | GT201000003A (ja) |
HK (1) | HK1141238A1 (ja) |
IL (1) | IL202382A0 (ja) |
MA (1) | MA31880B1 (ja) |
MX (1) | MX2010000468A (ja) |
NZ (1) | NZ581791A (ja) |
PE (1) | PE20090438A1 (ja) |
SV (1) | SV2010003449A (ja) |
TN (1) | TN2010000015A1 (ja) |
TW (1) | TW200918050A (ja) |
UA (1) | UA97672C2 (ja) |
WO (1) | WO2009009470A1 (ja) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8753098B2 (en) | 2009-06-26 | 2014-06-17 | Mitsubishi Electric Corporation | Refrigerant compressor |
Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2004092147A1 (ja) * | 2003-04-18 | 2004-10-28 | Kyowa Hakko Kogyo Co., Ltd. | M期キネシン阻害剤 |
WO2006101105A1 (ja) * | 2005-03-22 | 2006-09-28 | Kyowa Hakko Kogyo Co., Ltd. | 乾癬治療剤 |
WO2006101104A1 (ja) * | 2005-03-22 | 2006-09-28 | Kyowa Hakko Kogyo Co., Ltd. | 関節炎治療剤 |
WO2006101102A1 (ja) * | 2005-03-22 | 2006-09-28 | Kyowa Hakko Kogyo Co., Ltd. | 固形腫瘍治療剤 |
WO2006101103A1 (ja) * | 2005-03-22 | 2006-09-28 | Kyowa Hakko Kogyo Co., Ltd. | 造血器腫瘍治療剤 |
JP2006265107A (ja) * | 2005-03-22 | 2006-10-05 | Kyowa Hakko Kogyo Co Ltd | 緑内障治療剤 |
WO2006137490A1 (ja) * | 2005-06-24 | 2006-12-28 | Kyowa Hakko Kogyo Co., Ltd. | 再狭窄治療剤 |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PT1847534E (pt) | 2001-12-11 | 2011-08-01 | Kyowa Hakko Kirin Co Ltd | Derivado de tiadiozolina para o tratamento do cancro |
-
2008
- 2008-07-07 CA CA2694277A patent/CA2694277C/en not_active Expired - Fee Related
- 2008-07-07 CL CL2008001996A patent/CL2008001996A1/es unknown
- 2008-07-07 CN CN200880023900A patent/CN101730525A/zh active Pending
- 2008-07-07 PE PE2008001141A patent/PE20090438A1/es not_active Application Discontinuation
- 2008-07-07 AU AU2008275258A patent/AU2008275258A1/en not_active Abandoned
- 2008-07-07 MX MX2010000468A patent/MX2010000468A/es active IP Right Grant
- 2008-07-07 KR KR1020107000452A patent/KR101188036B1/ko not_active IP Right Cessation
- 2008-07-07 NZ NZ581791A patent/NZ581791A/en not_active IP Right Cessation
- 2008-07-07 BR BRPI0814039A patent/BRPI0814039A2/pt not_active IP Right Cessation
- 2008-07-07 TW TW097125572A patent/TW200918050A/zh unknown
- 2008-07-07 UA UAA201000209A patent/UA97672C2/ru unknown
- 2008-07-07 AR ARP080102933A patent/AR067472A1/es not_active Application Discontinuation
- 2008-07-07 US US12/665,740 patent/US8222284B2/en not_active Expired - Fee Related
- 2008-07-07 JP JP2010516173A patent/JP4875205B2/ja not_active Expired - Fee Related
- 2008-07-07 EA EA201070136A patent/EA016861B1/ru not_active IP Right Cessation
- 2008-07-07 EP EP08781425A patent/EP2178508B1/en active Active
- 2008-07-07 ES ES08781425T patent/ES2401477T3/es active Active
- 2008-07-07 WO PCT/US2008/069301 patent/WO2009009470A1/en active Application Filing
-
2009
- 2009-11-26 IL IL202382A patent/IL202382A0/en unknown
-
2010
- 2010-01-07 DO DO2010000004A patent/DOP2010000004A/es unknown
- 2010-01-07 GT GT201000003A patent/GT201000003A/es unknown
- 2010-01-08 SV SV2010003449A patent/SV2010003449A/es not_active Application Discontinuation
- 2010-01-08 EC EC2010009864A patent/ECSP109864A/es unknown
- 2010-01-08 CO CO10001885A patent/CO6270304A2/es active IP Right Grant
- 2010-01-08 TN TNP2010000015A patent/TN2010000015A1/fr unknown
- 2010-01-12 CR CR11210A patent/CR11210A/es not_active Application Discontinuation
- 2010-02-11 MA MA32616A patent/MA31880B1/fr unknown
- 2010-08-13 HK HK10107726.4A patent/HK1141238A1/xx not_active IP Right Cessation
Patent Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2004092147A1 (ja) * | 2003-04-18 | 2004-10-28 | Kyowa Hakko Kogyo Co., Ltd. | M期キネシン阻害剤 |
WO2006101105A1 (ja) * | 2005-03-22 | 2006-09-28 | Kyowa Hakko Kogyo Co., Ltd. | 乾癬治療剤 |
WO2006101104A1 (ja) * | 2005-03-22 | 2006-09-28 | Kyowa Hakko Kogyo Co., Ltd. | 関節炎治療剤 |
WO2006101102A1 (ja) * | 2005-03-22 | 2006-09-28 | Kyowa Hakko Kogyo Co., Ltd. | 固形腫瘍治療剤 |
WO2006101103A1 (ja) * | 2005-03-22 | 2006-09-28 | Kyowa Hakko Kogyo Co., Ltd. | 造血器腫瘍治療剤 |
JP2006265107A (ja) * | 2005-03-22 | 2006-10-05 | Kyowa Hakko Kogyo Co Ltd | 緑内障治療剤 |
WO2006137490A1 (ja) * | 2005-06-24 | 2006-12-28 | Kyowa Hakko Kogyo Co., Ltd. | 再狭窄治療剤 |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8753098B2 (en) | 2009-06-26 | 2014-06-17 | Mitsubishi Electric Corporation | Refrigerant compressor |
Also Published As
Publication number | Publication date |
---|---|
US8222284B2 (en) | 2012-07-17 |
EA201070136A1 (ru) | 2010-06-30 |
UA97672C2 (ru) | 2012-03-12 |
KR20100029827A (ko) | 2010-03-17 |
SV2010003449A (es) | 2010-08-10 |
CO6270304A2 (es) | 2011-04-20 |
CR11210A (es) | 2010-06-23 |
BRPI0814039A2 (pt) | 2017-10-03 |
HK1141238A1 (en) | 2010-11-05 |
TW200918050A (en) | 2009-05-01 |
US20110009458A1 (en) | 2011-01-13 |
EA016861B1 (ru) | 2012-08-30 |
AR067472A1 (es) | 2009-10-14 |
ES2401477T3 (es) | 2013-04-19 |
TN2010000015A1 (en) | 2011-09-26 |
CA2694277A1 (en) | 2009-01-15 |
PE20090438A1 (es) | 2009-04-18 |
CN101730525A (zh) | 2010-06-09 |
DOP2010000004A (es) | 2010-03-15 |
AU2008275258A1 (en) | 2009-01-15 |
MA31880B1 (fr) | 2010-12-01 |
EP2178508B1 (en) | 2013-02-06 |
MX2010000468A (es) | 2010-04-09 |
ECSP109864A (es) | 2010-03-31 |
CA2694277C (en) | 2013-04-09 |
JP2010533190A (ja) | 2010-10-21 |
GT201000003A (es) | 2012-03-13 |
CL2008001996A1 (es) | 2009-05-22 |
KR101188036B1 (ko) | 2012-10-05 |
IL202382A0 (en) | 2010-06-30 |
NZ581791A (en) | 2012-03-30 |
WO2009009470A1 (en) | 2009-01-15 |
EP2178508A1 (en) | 2010-04-28 |
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