JPH05509082A - 新規なα―グルコシダーゼ抑制剤 - Google Patents
新規なα―グルコシダーゼ抑制剤Info
- Publication number
- JPH05509082A JPH05509082A JP3511186A JP51118691A JPH05509082A JP H05509082 A JPH05509082 A JP H05509082A JP 3511186 A JP3511186 A JP 3511186A JP 51118691 A JP51118691 A JP 51118691A JP H05509082 A JPH05509082 A JP H05509082A
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound according
- compound
- tables
- glucobylanosyl
- 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
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 title 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 claims description 5
- 150000001875 compounds Chemical class 0.000 claims 16
- 239000000126 substance Substances 0.000 claims 7
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000006239 protecting group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 125000003147 glycosyl group Chemical group 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 150000002402 hexoses Chemical class 0.000 claims 2
- 201000001421 hyperglycemia Diseases 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 150000003863 ammonium salts Chemical class 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000000625 hexosyl group Chemical group 0.000 claims 1
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 1
- 150000002736 metal compounds Chemical class 0.000 claims 1
- 125000001805 pentosyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000376 reactant Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P31/14—Antivirals for RNA viruses
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Virology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Saccharide Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
(57)【要約】本公報は電子出願前の出願データであるため要約のデータは記録されません。
Description
【発明の詳細な説明】
本発明は新規な１−デすキンノジリマイシンのポリグリコンジル誘導体、その製
造方法及び最終用途特にｍ膿病の処置におけるそれらの用達に間する。
補正書の写しく翻訳文）提出書（特許法第１８４条の８）平成０４年１２月０８
日
Claims (12)
- １．式 ▲数式、化学式、表等があります▼Ｉ ［式中ｎは０、１又は２であり、 Ｒは、１−３個のヘキソース又はベントース単位を含有しているグリコシル部分 であり、該単位は、任意付加的に末端ヘキソーズ又はベントース単位のアノマー 炭素原子上のエーテル又はアシル基を有することもあり得、Ｒ１とＲ２の一つは Ｈであり、他方はα−Ｄ−グルコビラノシルである］の化合物及び製薬上受け入 れられるその塩。
- ２．Ｒ１がα−Ｄ−グルコビラノシルでありＲ２がＨである、請求項１に記載の 化合物。
- ３．Ｒ２かα−Ｄ−グルコビラノシルでＲ１がＨである、請求項１に記載の化合 物。
- ４．ｎが１である請求項１に記載の化合物。
- ５．該化合物が１，５−ジテオキシ−４−Ｏ−（α，Ｄ−グルコビラノシル）− １，５−［（６−デオキシ−１−Ｏ−メチル−６−α，Ｄ−グルコビラノシル） イミノ］−Ｄ−ケリシトールである請求項１に記載の化合物。
- ６．請求項１−５の何れか一に記載の化合物及び製薬上受け入れられる担体を含 む製剤組成物。
- ７．医薬としての用途のための請求項１−５の何れか一に記載の化合物。
- ８．糖尿病を処置する薬剤を製造するための請求項１−５の何れか一に記載の化 合物の用途。
- ９．肥満を処置ずる薬剤を製造するための請求項１−５の何れか一に記載の化合 物の用途。
- １０．請求項１に記載の化合物の治療上有効量を過血糖症にかかっている患者に 投与することを含む過血糖症を処置する方法。
- １１．請求項１に記載の化合物の治療上有効量を肥満にかかった患者に投与する ことからなる肥満を処置する方法。
- １２．式 ▲数式、化学式、表等があります▼ＩＩ［ｎは０、１又は２であり、 Ｒは１−３個のヘキソース又はペントース単位を含有するグリコシル部分であっ て、該単位は任意付加的に末端ヘキソースマはペンソース単位のアノマー炭素原 子とにエーテル又はアシル基を有ずることもあり得、Ｒ１とＲ２の１つはＨであ り他方はα−Ｄ−グリコピラノシルである］の化合物及び製薬上受け入れられろ その塩を製造する方法において （ａ）式 ▲数式、化学式、表等があります▼ＩＩＩ［式中ｎは０、１又は２であり、 Ｒ′は式ＩＩでＲに対して定義したグリコシル部分でありここでそのＯＨ基はヒ ドロキシ保護基を有しており、Ｐｇはヒドロキシ保護基であり、Ｒ３とＲ４の１ つはヒドロキシ保護基であり他方はＨである］の化合物を式▲数式、化学式、表 等があります▼ＩＶの化合物と縮合させて、式 ▲数式、化学式、表等があります▼Ｖ ▲数式、化学式、表等があります▼ＶＩの化合物を製造し、続いて任意のヒドロ キシ保護基を除去しそして必要ならば任意のアンモニウム塩を中和させ、そして （ｂ）式 ▲数式、化学式、表等があります▼ＶＩＩ［式中Ｒ１とＲ２の１つはＨであり他 方は、α−Ｄ−グルコビラノシル部分である］の化合物を式Ｘ−（ＣＨ２）ｎＲ 、［式中Ｘはブロモであり、ｎは０、１又は２であり、Ｒは式ＩＩに対して定義 した通りである］の化合物と縮合させることからなり、該反応体（ａ）及び（ｂ ）が式▲数式、化学式、表等があります▼Ｉ ［式中Ｒ、Ｒ１、Ｒ２及ひｎは式ＩＩにおいて定義した通りである］の化合物を つくり、そして任意付加的に該化金物を製薬上受け人れられる塩に変化すること もあり得ることからなる方法。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP90401582 | 1990-06-08 | ||
| FR90401582,3 | 1990-06-08 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH05509082A true JPH05509082A (ja) | 1993-12-16 |
| JP3136491B2 JP3136491B2 (ja) | 2001-02-19 |
Family
ID=8205720
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP03511186A Expired - Lifetime JP3136491B2 (ja) | 1990-06-08 | 1991-05-17 | 新規なα―グルコシダーゼ抑制剤 |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP0532668B1 (ja) |
| JP (1) | JP3136491B2 (ja) |
| AT (1) | ATE130304T1 (ja) |
| AU (1) | AU8069891A (ja) |
| DE (1) | DE69114707T2 (ja) |
| ES (1) | ES2082212T3 (ja) |
| WO (1) | WO1991018915A1 (ja) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5536732A (en) * | 1990-04-27 | 1996-07-16 | Merrell Pharmaceuticals Inc. | N-derivatives of 1-deoxy nojirimycin |
| US5252587A (en) * | 1990-04-27 | 1993-10-12 | Merrell Dow Pharmaceuticals, Inc. | N-derivatives of 1-deoxy nojirimycin |
| WO1995001361A1 (en) * | 1993-07-02 | 1995-01-12 | Nippon Shinyaku Co., Ltd. | Galactosylmoranoline derivative |
| AU7467394A (en) * | 1993-08-23 | 1995-03-21 | Nippon Shinyaku Co. Ltd. | Galactosylmoranoline derivative |
| US5633233A (en) * | 1995-06-07 | 1997-05-27 | Alberta Research Council | Modified kojibiosides analogues |
| WO2005092334A2 (en) * | 2004-03-25 | 2005-10-06 | David Priestman | Use of n-substituted imino sugars for appetite suppression |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6055078B2 (ja) * | 1980-12-01 | 1985-12-03 | 日本新薬株式会社 | モラノリンの誘導体 |
| GB2181729B (en) * | 1985-10-12 | 1990-04-04 | Nippon Shinyaku Co Ltd | Glucosylmoranoline derivatives and production thereof |
| JPS62242692A (ja) * | 1986-04-15 | 1987-10-23 | Nippon Shinyaku Co Ltd | モラノリン誘導体の製造法 |
| JP2504000B2 (ja) * | 1986-09-02 | 1996-06-05 | 日本新薬株式会社 | グルコシルモラノリン誘導体 |
-
1991
- 1991-05-17 ES ES91912140T patent/ES2082212T3/es not_active Expired - Lifetime
- 1991-05-17 AT AT91912140T patent/ATE130304T1/de not_active IP Right Cessation
- 1991-05-17 DE DE69114707T patent/DE69114707T2/de not_active Expired - Lifetime
- 1991-05-17 WO PCT/US1991/003474 patent/WO1991018915A1/en not_active Ceased
- 1991-05-17 JP JP03511186A patent/JP3136491B2/ja not_active Expired - Lifetime
- 1991-05-17 EP EP91912140A patent/EP0532668B1/en not_active Expired - Lifetime
- 1991-05-17 AU AU80698/91A patent/AU8069891A/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU8069891A (en) | 1991-12-31 |
| JP3136491B2 (ja) | 2001-02-19 |
| ES2082212T3 (es) | 1996-03-16 |
| EP0532668B1 (en) | 1995-11-15 |
| EP0532668A1 (en) | 1993-03-24 |
| ATE130304T1 (de) | 1995-12-15 |
| DE69114707T2 (de) | 1996-06-13 |
| DE69114707D1 (de) | 1995-12-21 |
| WO1991018915A1 (en) | 1991-12-12 |
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