JP2000501399A - ジアミノピリミジン、それらを含む医薬組成物及びそれらの抗菌剤としての用途 - Google Patents
ジアミノピリミジン、それらを含む医薬組成物及びそれらの抗菌剤としての用途Info
- Publication number
- JP2000501399A JP2000501399A JP9520925A JP52092597A JP2000501399A JP 2000501399 A JP2000501399 A JP 2000501399A JP 9520925 A JP9520925 A JP 9520925A JP 52092597 A JP52092597 A JP 52092597A JP 2000501399 A JP2000501399 A JP 2000501399A
- Authority
- JP
- Japan
- Prior art keywords
- formula
- dimethoxy
- benzopyran
- methyl
- compound
- 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
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
- C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
-
- 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
-
- 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
- A61P31/04—Antibacterial agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
- C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
- C07D311/64—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 with oxygen atoms directly attached in position 8
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Saccharide Compounds (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.一般式I (式中、R1が、直鎖C5-10−アルキル、分岐C3-5−アルキル、C3-6−シクロ アルキル又はC3-5−ω−カルボキシアルキルを表わし、そして、R2及びR3が C1-5−アルキルを表わすか、 又は、 R1が、水素を表わし、R2が、C3-5−ω−カルボキシアルキルを表わし、そし て、R3がC1-5−アルキルを表わすかのいずれかである) で示される化合物又はその薬学的に許容し得る酸付加塩。 2.R1が、直鎖C5-10−アルキル、分岐C3-5−アルキル、C3-6−シクロアル キル又はC3-5−ω−カルボキシアルキルを表わす、請求項1記載の化合物。 3.化合物、 (RS)−5−(2−シクロプロピル−7,8−ジメトキシ−2H−1−ベンゾ ピラン−5−イル−メチル)−ピリミジン−2,4−ジアミン、 (RS)−4−[5−(2,4−ジアミノ−ピリミジン−5−イル−メチル)− 7,8−ジメトキシ−2H−1−ベンゾピラン−2−イル]−酪酸、 (RS)−5−(7,8−ジメトキシ−2−ペンチル−2H−1−ベンゾピラン −5−イル−メチル)−ピリミジン−2,4−ジアミン、 (RS)−5−(2−イソプロピル−7,8−ジメトキシ−2H−1−ベンゾピ ラン−5−イル−メチル)−ピリミジン−2,4−ジアミン、又は 4−[5−(2,4−ジアミノ−ピリミジン−5−イル−メチル)−8−メトキ シ−2H−1−ベンゾピラン−7−イルオキシ]−酪酸。 4.式(式中、R1、R2及びR3は、請求項1で定義した意味を有する) で示される化合物。 5.式 (式中、R1、R2及びR3は、請求項1で定義した意味を有し、Xは、脱離基を 表わす) で示される化合物。 6.医薬用の、請求項1〜3のいずれか1項に記載の化合物。 7.請求項1〜3の化合物の製造方法であって、 a)式 (式中、R1、R2及びR3は、上記意味を有する) で示される化合物を環化する工程、又は、 b)式(式中、R1、R2及びR3は、上記意味を有し、Xは、脱離基を表わす) で示される化合物をグアニジンと反応させ、存在する保護基を開裂除去する工程 、及び、所望により、このようにして得られた式Iの化合物を薬学的に使用可能 な塩に変換する工程、 を含む方法。 8.請求項1〜3のいずれか1項に記載の化合物及び治療的に不活性な担体を含 んでいる医薬。 9.請求項1〜3のいずれか1項に記載の化合物の、特に感染性疾患における、 医薬としての用途。 10.請求項1〜3のいずれか1項に記載の化合物の、抗生物質的に活性な医薬 の製造における使用。 11.前記した発明。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CH3425/95 | 1995-12-04 | ||
CH342595 | 1995-12-04 | ||
PCT/EP1996/005151 WO1997020839A1 (en) | 1995-12-04 | 1996-11-22 | Diaminopyrimidines, pharmaceutical compositions containing them and their use as antibacterial |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2000501399A true JP2000501399A (ja) | 2000-02-08 |
JP3309340B2 JP3309340B2 (ja) | 2002-07-29 |
Family
ID=4255709
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP52092597A Expired - Fee Related JP3309340B2 (ja) | 1995-12-04 | 1996-11-22 | ジアミノピリミジン、それらを含む医薬組成物及びそれらの抗菌剤としての用途 |
Country Status (16)
Country | Link |
---|---|
US (1) | US5773446A (ja) |
EP (2) | EP1149834A1 (ja) |
JP (1) | JP3309340B2 (ja) |
KR (1) | KR100417207B1 (ja) |
CN (1) | CN1092194C (ja) |
AT (1) | ATE212629T1 (ja) |
AU (1) | AU708578B2 (ja) |
BR (1) | BR9611871B1 (ja) |
CA (1) | CA2238521C (ja) |
DE (1) | DE69618986T2 (ja) |
DK (1) | DK0866791T3 (ja) |
ES (1) | ES2169272T3 (ja) |
MX (1) | MX9804416A (ja) |
PT (1) | PT866791E (ja) |
TR (1) | TR199801014T2 (ja) |
WO (1) | WO1997020839A1 (ja) |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2004505077A (ja) * | 2000-07-29 | 2004-02-19 | アルパイダ アーゲー | ベンゾフラン誘導体 |
JP2007501771A (ja) * | 2003-08-08 | 2007-02-01 | アルパイダ アーゲー | 2h−クロメン類の新規製造方法 |
JP2009505943A (ja) * | 2005-02-18 | 2009-02-12 | アルパイダ アーゲー | 2h−クロメンの製造のための新規方法 |
JP2011516509A (ja) * | 2008-04-08 | 2011-05-26 | アシノ ファーマ アーゲー | 水性医薬製剤 |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW438796B (en) * | 1996-05-15 | 2001-06-07 | Hoffmann La Roche | 2,4-diaminopyrimidine derivatives, the manufacture process thereof, and the antibiotically-active pharmaceutical composition containing the same |
JP4033676B2 (ja) * | 2000-04-27 | 2008-01-16 | バジリア ファルマスーチカ アーゲー | 抗菌剤としてのクロメニルメチルピリミジンジアミン類 |
US20090069357A1 (en) * | 2007-09-09 | 2009-03-12 | Protia, Llc | Deuterium-enriched iclaprim |
US7947293B2 (en) | 2008-04-08 | 2011-05-24 | Arpida Ag | Aqueous pharmaceutical formulation |
EP3452042A1 (en) | 2016-05-04 | 2019-03-13 | Motif Biosciences, Inc. | Systems and methods for treating bacterial infection |
EP3538094A4 (en) * | 2016-11-11 | 2020-06-24 | Motif Biosciences, Inc. | FORMULATIONS, METHODS, KIT AND PHARMACEUTICAL FORMS FOR TREATING BACTERIAL INFECTIONS |
CN110498812B (zh) * | 2018-05-17 | 2021-08-24 | 上海医药工业研究院 | 一种艾拉普林的中间体化合物的制备方法 |
CN110606831A (zh) * | 2018-06-14 | 2019-12-24 | 上海度德医药科技有限公司 | 一种Iclaprim的新中间体及其制备方法和应用 |
CN110818693B (zh) * | 2018-08-07 | 2023-06-02 | 上海度德医药科技有限公司 | 一种艾拉普林甲磺酸盐晶型b及其制备方法 |
WO2020161284A1 (en) | 2019-02-07 | 2020-08-13 | Sandoz Ag | Crystalline form of iclaprim mesylate |
CN109988156B (zh) * | 2019-03-12 | 2021-12-28 | 广东中科药物研究有限公司 | 一种氨基嘧啶化合物 |
CN113493461A (zh) * | 2020-04-01 | 2021-10-12 | 上海医药工业研究院 | 一种七元杂环化合物或其盐、其制备方法及应用 |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4438267A (en) * | 1980-11-11 | 1984-03-20 | Daluge Susan M | Monoheteroring compounds and their use |
-
1996
- 1996-11-22 DK DK96939890T patent/DK0866791T3/da active
- 1996-11-22 TR TR1998/01014T patent/TR199801014T2/xx unknown
- 1996-11-22 PT PT96939890T patent/PT866791E/pt unknown
- 1996-11-22 JP JP52092597A patent/JP3309340B2/ja not_active Expired - Fee Related
- 1996-11-22 EP EP01117420A patent/EP1149834A1/en not_active Withdrawn
- 1996-11-22 DE DE69618986T patent/DE69618986T2/de not_active Expired - Lifetime
- 1996-11-22 BR BRPI9611871-7A patent/BR9611871B1/pt not_active IP Right Cessation
- 1996-11-22 CA CA002238521A patent/CA2238521C/en not_active Expired - Fee Related
- 1996-11-22 WO PCT/EP1996/005151 patent/WO1997020839A1/en active IP Right Grant
- 1996-11-22 AU AU76963/96A patent/AU708578B2/en not_active Ceased
- 1996-11-22 KR KR10-1998-0704199A patent/KR100417207B1/ko not_active IP Right Cessation
- 1996-11-22 ES ES96939890T patent/ES2169272T3/es not_active Expired - Lifetime
- 1996-11-22 EP EP96939890A patent/EP0866791B1/en not_active Expired - Lifetime
- 1996-11-22 AT AT96939890T patent/ATE212629T1/de active
- 1996-11-22 CN CN96198783A patent/CN1092194C/zh not_active Expired - Fee Related
- 1996-12-02 US US08/758,993 patent/US5773446A/en not_active Expired - Lifetime
-
1998
- 1998-06-03 MX MX9804416A patent/MX9804416A/es unknown
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2004505077A (ja) * | 2000-07-29 | 2004-02-19 | アルパイダ アーゲー | ベンゾフラン誘導体 |
JP2007501771A (ja) * | 2003-08-08 | 2007-02-01 | アルパイダ アーゲー | 2h−クロメン類の新規製造方法 |
JP2009505943A (ja) * | 2005-02-18 | 2009-02-12 | アルパイダ アーゲー | 2h−クロメンの製造のための新規方法 |
JP2011516509A (ja) * | 2008-04-08 | 2011-05-26 | アシノ ファーマ アーゲー | 水性医薬製剤 |
Also Published As
Publication number | Publication date |
---|---|
EP0866791B1 (en) | 2002-01-30 |
ATE212629T1 (de) | 2002-02-15 |
ES2169272T3 (es) | 2002-07-01 |
AU7696396A (en) | 1997-06-27 |
DE69618986D1 (de) | 2002-03-14 |
CN1203600A (zh) | 1998-12-30 |
KR19990071912A (ko) | 1999-09-27 |
BR9611871B1 (pt) | 2010-11-03 |
CA2238521A1 (en) | 1997-06-12 |
PT866791E (pt) | 2002-05-31 |
DK0866791T3 (da) | 2002-04-22 |
EP1149834A1 (en) | 2001-10-31 |
EP0866791A1 (en) | 1998-09-30 |
CN1092194C (zh) | 2002-10-09 |
AU708578B2 (en) | 1999-08-05 |
DE69618986T2 (de) | 2002-06-20 |
MX9804416A (es) | 1998-09-30 |
TR199801014T2 (xx) | 1998-09-21 |
WO1997020839A1 (en) | 1997-06-12 |
US5773446A (en) | 1998-06-30 |
CA2238521C (en) | 2005-08-16 |
KR100417207B1 (ko) | 2004-04-17 |
BR9611871A (pt) | 1999-02-17 |
JP3309340B2 (ja) | 2002-07-29 |
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