JP2002536333A5 - - Google Patents
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- JP2002536333A5 JP2002536333A5 JP2000596939A JP2000596939A JP2002536333A5 JP 2002536333 A5 JP2002536333 A5 JP 2002536333A5 JP 2000596939 A JP2000596939 A JP 2000596939A JP 2000596939 A JP2000596939 A JP 2000596939A JP 2002536333 A5 JP2002536333 A5 JP 2002536333A5
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- JP
- Japan
- Prior art keywords
- compound
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- pharmaceutically acceptable
- need
- oral formulation
- 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.)
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- 150000001875 compounds Chemical class 0.000 description 19
- 150000003839 salts Chemical class 0.000 description 10
- 238000009472 formulation Methods 0.000 description 8
- 239000000203 mixture Substances 0.000 description 8
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 6
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 description 4
- 239000003085 diluting agent Substances 0.000 description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 4
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 description 4
- 239000008194 pharmaceutical composition Substances 0.000 description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 4
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 description 4
- 102000006991 Apolipoprotein B-100 Human genes 0.000 description 3
- 108010008150 Apolipoprotein B-100 Proteins 0.000 description 3
- 108010023302 HDL Cholesterol Proteins 0.000 description 3
- 108010028554 LDL Cholesterol Proteins 0.000 description 3
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 3
- VDXAJPMEBTVBFW-UHFFFAOYSA-N 5,5-dihydroxyhept-6-enoic acid Chemical compound OC(=O)CCCC(O)(O)C=C VDXAJPMEBTVBFW-UHFFFAOYSA-N 0.000 description 1
- SFFYOOJRHFHVCM-LDCPCGJSSA-L calcium (3R,5S)-3,5-dihydroxyhept-6-enoate Chemical compound [Ca+2].O[C@@H](CC(=O)[O-])C[C@@H](C=C)O.O[C@@H](CC(=O)[O-])C[C@@H](C=C)O SFFYOOJRHFHVCM-LDCPCGJSSA-L 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
Description
【特許請求の範囲】
【請求項１】 化合物（Ｅ）−７−［４−（４−フルオロフェニル）−６−イソプロピル−２−［メチル（メチルスルホニル）アミノ］ピリミジン−５−イル］−（３Ｒ，５Ｓ）−３，５−ジヒドロキシヘプツ−６−エン酸またはその医薬的に許容できる塩の、経口製剤の製造のための使用であって、
経口製剤が、化合物５〜８０ｍｇを含み、その必要があるヒト患者において、ＬＤＬ−Ｃレベルを４０％以上低下させ、および／または総コレステロールレベルを３０％以上低下させ、および／またはトリグリセリドレベルを１０％以上低下させ、および／またはアポリポタンパク質Ｂ−１００レベルを３０％以上低下させ、および／またはＨＤＬ−Ｃレベルを５％以上高めるのに用いられ、その際化合物が１日５〜８０ｍｇ投与される。
【請求項２】 経口製剤が、化合物５〜１０ｍｇを含み、その必要があるヒト患者において、ＬＤＬ−Ｃレベルを４０％以上低下させ、および／または総コレステロールレベルを３０％以上低下させ、および／またはトリグリセリドレベルを１０％以上低下させ、および／またはアポリポタンパク質Ｂ−１００レベルを３０％以上低下させ、および／またはＨＤＬ−Ｃレベルを５％以上高めるのに用いられ、その際化合物が１日５〜１０ｍｇ投与される、請求項１に記載の化合物またはその医薬的に許容できる塩の使用。
【請求項３】 経口製剤が、化合物５〜１０ｍｇを含み、その必要があるヒト患者において、ＬＤＬ−Ｃレベルを４５％以上低下させるのに用いられる、請求項２に記載の化合物またはその医薬的に許容できる塩の使用。
【請求項４】 経口製剤が、化合物５〜１０ｍｇを含み、その必要があるヒト患者において、総コレステロールレベルを３５％以上低下させるのに用いられる、請求項２に記載の化合物またはその医薬的に許容できる塩の使用。
【請求項５】 経口製剤が、化合物５〜１０ｍｇを含み、その必要があるヒト患者において、トリグリセリドレベルを１０％以上低下させるのに用いられる、請求項２に記載の化合物またはその医薬的に許容できる塩の使用。
【請求項６】 経口製剤が、化合物５〜１０ｍｇを含み、その必要があるヒト患者において、アポリポタンパク質Ｂ−１００レベルを３５％以上低下させるのに用いられる、請求項２に記載の化合物またはその医薬的に許容できる塩の使用。
【請求項７】 経口製剤が、化合物５〜１０ｍｇを含み、その必要があるヒト患者において、ＨＤＬ−Ｃレベルを８％以上高めるのに用いられる、請求項２に記載の化合物またはその医薬的に許容できる塩の使用。
【請求項８】 経口製剤を１日１回、単一用量として投与する、請求項１〜７のいずれか１項に記載の使用。
【請求項９】 ５〜８０ｍｇの（Ｅ）−７−［４−（４−フルオロフェニル）−６−イソプロピル−２−［メチル（メチルスルホニル）アミノ］ピリミジン−５−イル］−（３Ｒ，５Ｓ）−３，５−ジヒドロキシヘプツ−６−エン酸またはその医薬的に許容できる塩を医薬的に許容できる希釈剤またはキャリヤーと共に含む、経口投与に適する医薬組成物。
【請求項１０】 ５〜１０ｍｇの（Ｅ）−７−［４−（４−フルオロフェニル）−６−イソプロピル−２−［メチル（メチルスルホニル）アミノ］ピリミジン−５−イル］−（３Ｒ，５Ｓ）−３，５−ジヒドロキシヘプツ−６−エン酸またはその医薬的に許容できる塩を医薬的に許容できる希釈剤またはキャリヤーと共に含む、経口投与に適する医薬組成物。
【請求項１１】 ５．２〜１０．４ｍｇの（Ｅ）−７−［４−（４−フルオロフェニル）−６−イソプロピル−２−［メチル（メチルスルホニル）アミノ］ピリミジン−５−イル］−（３Ｒ，５Ｓ）−３，５−ジヒドロキシヘプツ−６−エン酸カルシウム塩を医薬的に許容できる希釈剤またはキャリヤーと共に含む、請求項９または１０に記載の医薬組成物。
【請求項１２】 化合物またはその医薬的に許容できる塩を医薬的に許容できる希釈剤またはキャリヤーと混合することを含む、請求項９、１０または１１に記載の医薬組成物の製造方法。
[Claims]
1. Compound (E) -7- [4- (4-fluorophenyl) -6-isopropyl-2- [methyl (methylsulfonyl) amino] pyrimidin-5-yl]-(3R, 5S) -3 Use of 5,5-dihydroxyhept-6-enoic acid or a pharmaceutically acceptable salt thereof for the manufacture of an oral preparation, comprising:
The oral formulation comprises 5-80 mg of the compound, which reduces LDL-C levels by more than 40% and / or reduces total cholesterol levels by more than 30% and / or lowers triglyceride levels by 10% in human patients in need thereof. % And / or reduce apolipoprotein B-100 levels by 30% or more and / or increase HDL-C levels by 5% or more, wherein the compound is administered at 5-80 mg daily. .
2. An oral formulation comprising 5-10 mg of the compound, which reduces LDL-C levels by more than 40% and / or lowers total cholesterol levels by more than 30% in a human patient in need thereof, and / or Alternatively, it is used to reduce triglyceride levels by 10% or more and / or reduce apolipoprotein B-100 levels by 30% or more and / or increase HDL-C levels by 5% or more, wherein the compound is used for 5 days per day. Use of a compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein the compound is administered at a dose of from 10 to 10 mg.
3. The compound of claim 2, wherein the oral formulation comprises 5-10 mg of the compound and is used to reduce LDL-C levels by more than 45% in a human patient in need thereof. Use of acceptable salts.
4. The compound of claim 2, wherein the oral formulation comprises 5-10 mg of the compound and is used to reduce total cholesterol levels by more than 35% in a human patient in need thereof. Use of acceptable salts.
5. The compound of claim 2, wherein the oral formulation comprises 5-10 mg of the compound and is used to reduce triglyceride levels by 10% or more in a human patient in need thereof, or a pharmaceutically acceptable compound thereof. Use of salt that can.
6. The compound of claim 2, wherein the oral formulation comprises 5-10 mg of the compound and is used to reduce apolipoprotein B-100 levels by 35% or more in a human patient in need thereof. Use of a pharmaceutically acceptable salt.
7. The compound of claim 2, wherein the oral formulation comprises 5-10 mg of the compound and is used to increase HDL-C levels by 8% or more in a human patient in need thereof. Use of acceptable salts.
8. Use according to any one of the preceding claims, wherein the oral formulation is administered once a day as a single dose.
9. 5-80 mg of (E) -7- [4- (4-fluorophenyl) -6-isopropyl-2- [methyl (methylsulfonyl) amino] pyrimidin-5-yl]-(3R, 5S A) Pharmaceutical composition suitable for oral administration, comprising -3,5-dihydroxyhept-6-enoic acid or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable diluent or carrier.
10. 10 mg of (E) -7- [4- (4-fluorophenyl) -6-isopropyl-2- [methyl (methylsulfonyl) amino] pyrimidin-5-yl]-(3R, 5S A) Pharmaceutical composition suitable for oral administration, comprising -3,5-dihydroxyhept-6-enoic acid or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable diluent or carrier.
11. 5.2 to 10.4 mg of (E) -7- [4- (4-fluorophenyl) -6-isopropyl-2- [methyl (methylsulfonyl) amino] pyrimidin-5-yl]- The pharmaceutical composition according to claim 9 or 10, comprising (3R, 5S) -3,5-dihydroxyhept-6-enoic acid calcium salt together with a pharmaceutically acceptable diluent or carrier.
12. The method of producing a pharmaceutical composition according to claim 9, 10 or 11, comprising mixing the compound or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable diluent or carrier.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9902590.0 | 1999-02-06 | ||
| GBGB9902590.0A GB9902590D0 (en) | 1999-02-06 | 1999-02-06 | Use of cholesterol-lowering agent |
| GBGB9921062.7A GB9921062D0 (en) | 1999-09-08 | 1999-09-08 | Use of cholestrol-lowering agent |
| GB9921062.7 | 1999-09-08 | ||
| PCT/GB2000/000285 WO2000045819A1 (en) | 1999-02-06 | 2000-02-01 | Use of cholesterol-lowering agent |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011035406A Division JP2011137023A (en) | 1999-02-06 | 2011-02-22 | Use of cholesterol-lowering agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2002536333A JP2002536333A (en) | 2002-10-29 |
| JP2002536333A5 true JP2002536333A5 (en) | 2007-03-08 |
Family
ID=26315084
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000596939A Withdrawn JP2002536333A (en) | 1999-02-06 | 2000-02-01 | Use of cholesterol-lowering drugs |
| JP2011035406A Pending JP2011137023A (en) | 1999-02-06 | 2011-02-22 | Use of cholesterol-lowering agent |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011035406A Pending JP2011137023A (en) | 1999-02-06 | 2011-02-22 | Use of cholesterol-lowering agent |
Country Status (22)
| Country | Link |
|---|---|
| EP (1) | EP1150679A1 (en) |
| JP (2) | JP2002536333A (en) |
| KR (1) | KR100699287B1 (en) |
| CN (1) | CN1347320A (en) |
| AR (1) | AR022462A1 (en) |
| AU (1) | AU769897B2 (en) |
| BR (1) | BR0007991A (en) |
| CA (1) | CA2358641A1 (en) |
| CZ (1) | CZ20012631A3 (en) |
| EE (1) | EE04659B1 (en) |
| HK (1) | HK1040924A1 (en) |
| HU (1) | HUP0105019A3 (en) |
| ID (1) | ID30131A (en) |
| IL (1) | IL144662A0 (en) |
| IS (1) | IS5996A (en) |
| MY (1) | MY136382A (en) |
| NO (1) | NO319827B1 (en) |
| NZ (1) | NZ512681A (en) |
| PL (1) | PL349137A1 (en) |
| SK (1) | SK11112001A3 (en) |
| TR (1) | TR200102236T2 (en) |
| WO (1) | WO2000045819A1 (en) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0001621D0 (en) * | 2000-01-26 | 2000-03-15 | Astrazeneca Ab | Pharmaceutical compositions |
| GB0003305D0 (en) | 2000-02-15 | 2000-04-05 | Zeneca Ltd | Pyrimidine derivatives |
| SE0103509D0 (en) * | 2001-10-19 | 2001-10-19 | Astrazeneca Ab | Rosuvastatin in pre-demented states |
| GB0322552D0 (en) | 2003-09-26 | 2003-10-29 | Astrazeneca Uk Ltd | Therapeutic treatment |
| WO2007142581A1 (en) * | 2006-06-07 | 2007-12-13 | Astrazeneca Ab | Combination product for the treatment or prevention of dyslipidaemia |
| WO2008156717A1 (en) * | 2007-06-20 | 2008-12-24 | Merck & Co., Inc. | Cetp inhibitors derived from benzoxazole arylamides |
| CA2689525A1 (en) * | 2007-06-20 | 2008-12-24 | Merck Sharp & Dohme Corp. | Cetp inhibitors derived from benzoxazole arylamides |
| WO2008156715A1 (en) | 2007-06-20 | 2008-12-24 | Merck & Co., Inc. | Cetp inhibitors derived from benzoxazole arylamides |
| EP2216095A1 (en) * | 2009-01-27 | 2010-08-11 | Koninklijke Philips Electronics N.V. | Microfluidic device for full blood count |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5260446A (en) * | 1989-12-22 | 1993-11-09 | Basf Aktiengesellschaft | Aminothiazoles |
| JP2648897B2 (en) * | 1991-07-01 | 1997-09-03 | 塩野義製薬株式会社 | Pyrimidine derivatives |
-
2000
- 2000-01-31 AR ARP000100408A patent/AR022462A1/en unknown
- 2000-02-01 CN CN00803519A patent/CN1347320A/en active Pending
- 2000-02-01 CA CA002358641A patent/CA2358641A1/en not_active Abandoned
- 2000-02-01 WO PCT/GB2000/000285 patent/WO2000045819A1/en active IP Right Grant
- 2000-02-01 ID IDW00200101666A patent/ID30131A/en unknown
- 2000-02-01 BR BR0007991-0A patent/BR0007991A/en not_active Application Discontinuation
- 2000-02-01 SK SK1111-2001A patent/SK11112001A3/en not_active Application Discontinuation
- 2000-02-01 KR KR1020017009822A patent/KR100699287B1/en not_active Ceased
- 2000-02-01 AU AU23051/00A patent/AU769897B2/en not_active Revoked
- 2000-02-01 CZ CZ20012631A patent/CZ20012631A3/en unknown
- 2000-02-01 EP EP00901748A patent/EP1150679A1/en not_active Withdrawn
- 2000-02-01 JP JP2000596939A patent/JP2002536333A/en not_active Withdrawn
- 2000-02-01 IL IL14466200A patent/IL144662A0/en unknown
- 2000-02-01 HK HK02102713.0A patent/HK1040924A1/en unknown
- 2000-02-01 PL PL00349137A patent/PL349137A1/en not_active Application Discontinuation
- 2000-02-01 TR TR2001/02236T patent/TR200102236T2/en unknown
- 2000-02-01 HU HU0105019A patent/HUP0105019A3/en unknown
- 2000-02-01 EE EEP200100404A patent/EE04659B1/en not_active IP Right Cessation
- 2000-02-01 NZ NZ512681A patent/NZ512681A/en not_active IP Right Cessation
- 2000-02-04 MY MYPI20000415A patent/MY136382A/en unknown
-
2001
- 2001-07-10 IS IS5996A patent/IS5996A/en unknown
- 2001-08-03 NO NO20013810A patent/NO319827B1/en active IP Right Review Request
-
2011
- 2011-02-22 JP JP2011035406A patent/JP2011137023A/en active Pending
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