JPH11502532A - 末端カルボキシまたはテトラゾール基を含有するジアルキルエーテル - Google Patents
末端カルボキシまたはテトラゾール基を含有するジアルキルエーテルInfo
- Publication number
- JPH11502532A JPH11502532A JP8529342A JP52934296A JPH11502532A JP H11502532 A JPH11502532 A JP H11502532A JP 8529342 A JP8529342 A JP 8529342A JP 52934296 A JP52934296 A JP 52934296A JP H11502532 A JPH11502532 A JP H11502532A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- compound according
- administering
- cholesterol
- mammal
- 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.)
- Granted
Links
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- 238000000034 method Methods 0.000 claims description 26
- 235000012000 cholesterol Nutrition 0.000 claims description 21
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- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 239000011775 sodium fluoride Substances 0.000 description 1
- 235000013024 sodium fluoride Nutrition 0.000 description 1
- KKCBUQHMOMHUOY-UHFFFAOYSA-N sodium oxide Chemical compound [O-2].[Na+].[Na+] KKCBUQHMOMHUOY-UHFFFAOYSA-N 0.000 description 1
- 229910001948 sodium oxide Inorganic materials 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000012289 standard assay Methods 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 125000005017 substituted alkenyl group Chemical group 0.000 description 1
- 125000004426 substituted alkynyl group Chemical group 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 description 1
- 150000003462 sulfoxides Chemical class 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000037317 transdermal delivery Effects 0.000 description 1
- 238000005809 transesterification reaction Methods 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 230000006492 vascular dysfunction Effects 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 239000008096 xylene Substances 0.000 description 1
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- C07D257/04—Five-membered rings
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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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Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.式 [式中、nおよびmは独立して2〜9の整数であり、 R1、R2、R3およびR4は独立して(C1〜C6)アルキル、(C2〜C6)アルケニル、 (C2〜C6)アルキニルであり、R1とR2はそれらが結合している炭素と一緒になり 、そしてR3とR4はそれらが結合している炭素と一緒になって、独立して3〜6個 の炭素を有する炭素環式環を完成することができ、 Y1およびY2は独立してCOOH、CHO、テトラゾールおよびCOOR5{ここでR5は(C1 〜C6)アルキル、(C2〜C6)アルケニルまたは(C2〜C6)アルキニルである}で あり、 そしてここでアルキル、アルケニルおよびアルキニル基はハロ、ヒドロキシ、 (C1〜C6)アルコキシおよびフェニルから選択される1個または2個の基で置換 されてもよい] で表される化合物およびその医薬的に許容し得る塩。 2.R1、R2、R3およびR4がそれぞれ(C1〜C6)アルキルである請求項1記載の化 合物。 3.Y1およびY2が独立してCOOHまたはCOOR5である請求項1記載の化合物。 4.Y1およびY2が独立してCOOHまたはCOOR5であり、R5が(C1〜C6)アルキルで ある請求項3記載の化合物。 5.R1、R2、R3およびR4がそれぞれ同じアルキルであり、そしてY1およ びY2が両方ともCOOHである請求項4記載の化合物。 6.R1、R2、R3およびR4がそれぞれメチルである請求項5記載の化合物。 7.nおよびmが同じ整数である請求項6記載の化合物。 8.nおよびmが両方とも4である請求項7記載の化合物。 9.6,6′−オキシビス(2,2−ジメチルヘキサン酸)である請求項8記載の化合 物。 10.nおよびmの両方が2、3、5または6である請求項7記載の化合物。 11.4,4′−オキシビス(2,2−ジメチルブタン酸); 5,5′−オキシビス(2,2−ジメチルペンタン酸); 7,7′−オキシビス(2,2−ジメチルヘプタン酸);または 8,8′−オキシビス(2,2−ジメチルオクタン酸)である請求項10記載の化合物 。 12.Y1およびY2が両方ともCOOR5である請求項7記載の化合物。 13.R5がメチルである請求項12記載の化合物。 14.メチル2,2−ジメチル−8−(7−メチル−7−メトキシカルボニルオクチル オキシ)オルタノエートである請求項13記載の化合物。 15.R5がエチルである請求項12記載の化合物。 16.エチル2,2−ジメチル−5−(4−メチル−4−エトキシカルボニルペンチル オキシ)ペンタノエートまたはエチル2,2−ジメチル−6−(5−メチル−5−エ トキシカルボニルヘキシルオキシ)ヘキサノエートある請求項15記載の化合物。 17.請求項1記載の化合物を医薬的に許容し得る希釈剤、担体または賦形剤とと もに含有する製剤。 18.Y1およびY2が独立してCOOHまたはCOOR5[ここでR5は(C1−C6)アルキルであ る]である化合物を用いる請求項17記載の製剤。 19.R1、R2、R3およびR4がそれぞれメチルである化合物を用いる請求項18記載の 製剤。 20.nおよびmが同一である化合物を用いる請求項19記載の製剤。 21.nおよびmの両方が4である化合物を用いる請求項20記載の製剤。 22.6,6′−オキシビス(2,2−ジメチルヘキサン酸)を用いる請求項20記載の製剤 。 23.Lp(a)を低下させる量の請求項1記載の化合物を哺乳動物に投与することか らなる血漿Lp(a)を低下させる方法。 24.有効量の請求項1記載の化合物を哺乳動物に投与することからなる血管性疾 患の予防または治療の方法。 25.有効量の請求項1記載の化合物を哺乳動物に投与することからなる血漿HDL −コレステロールを高める方法。 26.有効量の請求項1記載の化合物を哺乳動物に投与することからなる血漿トリ グリセリドを低下させる方法。 27.有効量の請求項1記載の化合物を哺乳動物に投与することからなる非インス リン依存性糖尿病の予防または治療の方法。 28.有効量の請求項1記載の化合物を哺乳動物に投与することからなるLDL−コ レステロールを低下させる方法。 29.VLDL−コレステロールを低下させる量の請求項1記載の化合物を哺乳動物に 投与することからなるVLDL−コレステロールを低下させる方法。 30.有効量の請求項1記載の化合物を哺乳動物に投与することからなるアポリポ タンパク質Bを低下させる方法。 31.有効量の請求項1記載の化合物を哺乳動物に投与することからなる血漿アポ リポタンパク質A-Iを高める方法。 32.有効量の請求項1記載の化合物を哺乳動物に投与することからなる血漿アポ リポタンパク質Eを高める方法。
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Application Number | Priority Date | Filing Date | Title |
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US08/409,780 | 1995-03-24 | ||
US08/409,780 US5648387A (en) | 1995-03-24 | 1995-03-24 | Carboxyalkylethers, formulations, and treatment of vascular diseases |
PCT/US1996/001639 WO1996030328A1 (en) | 1995-03-24 | 1996-02-05 | Terminal carboxy or tetrazole groups containing dialkyl ethers |
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JPH11502532A true JPH11502532A (ja) | 1999-03-02 |
JP3885115B2 JP3885115B2 (ja) | 2007-02-21 |
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US (4) | US5648387A (ja) |
EP (1) | EP0820428B1 (ja) |
JP (1) | JP3885115B2 (ja) |
KR (1) | KR100408612B1 (ja) |
CN (1) | CN1100747C (ja) |
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AU (1) | AU692359B2 (ja) |
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CA (1) | CA2215233C (ja) |
CZ (1) | CZ289556B6 (ja) |
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DK (1) | DK0820428T3 (ja) |
EE (1) | EE03520B1 (ja) |
ES (1) | ES2148733T3 (ja) |
FI (1) | FI973713A (ja) |
GR (1) | GR3034109T3 (ja) |
HK (1) | HK1009438A1 (ja) |
HU (1) | HUP9801825A3 (ja) |
NO (1) | NO307878B1 (ja) |
NZ (1) | NZ302170A (ja) |
PL (1) | PL181673B1 (ja) |
PT (1) | PT820428E (ja) |
RU (1) | RU2191772C2 (ja) |
SK (1) | SK282897B6 (ja) |
UA (1) | UA46020C2 (ja) |
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JP2017533973A (ja) * | 2014-11-14 | 2017-11-16 | ジェムフィアー セラピューティクス インコーポレイテッド | α,ω−ジカルボン酸末端ジアルカンエーテルを調製するためのプロセスおよび中間体 |
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JP2017533973A (ja) * | 2014-11-14 | 2017-11-16 | ジェムフィアー セラピューティクス インコーポレイテッド | α,ω−ジカルボン酸末端ジアルカンエーテルを調製するためのプロセスおよび中間体 |
JP2019048838A (ja) * | 2014-11-14 | 2019-03-28 | ジェムフィアー セラピューティクス インコーポレイテッド | α,ω−ジカルボン酸末端ジアルカンエーテルを調製するためのプロセスおよび中間体 |
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