JP2001508400A - アセチルコリンエステラーゼ阻害剤および鎮痛剤としてのイサチン誘導体 - Google Patents
アセチルコリンエステラーゼ阻害剤および鎮痛剤としてのイサチン誘導体Info
- Publication number
- JP2001508400A JP2001508400A JP53708497A JP53708497A JP2001508400A JP 2001508400 A JP2001508400 A JP 2001508400A JP 53708497 A JP53708497 A JP 53708497A JP 53708497 A JP53708497 A JP 53708497A JP 2001508400 A JP2001508400 A JP 2001508400A
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- compound
- alkoxy
- hydroxy
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.式 [式中、 Rは、水素、(C1−C6)アルキルまたはヒドロキシ(C1−C6)アルキルであり; Xは、水素、ヒドロキシ、(C1−C6)アルコキシ、フェニル(C1−C6)アルコキシ 、または−O(C=O)NR1R2であり;そして Yは、水素またはハロゲンであり; ここでR1は、(C1−C6)アルキル、フェニル、またはフェニル(C1−C6)アルキル であって、このフェニル基は場合により(C1−C6)アルキル、(C1−C6)アルコキシ 、ハロゲンまたはトリフルオロメチルによって置換されていてもよく;R2は、水 素または(C1−C6)アルキルであるか;または、R1およびR2は一緒になって、これ らが結合している窒素とともにテトラヒドロイソキノリン基を形成する] の化合物およびその製薬上許容できる酸付加塩。 2.Rが、水素、(C1−C6)アルキルまたはヒドロキシ(C1−C6)アルキルであり; Xが、水素、ヒドロキシ、(C1−C6)アルコキシ、ベンジルオキシ、または−O(C =O)NR1R2であり;そしてYが、水素またはハロゲンであり;ここでR1は、(C1− C6)アルキル、フェネチル、またはベンジルであって、このフェニル基は場合に より(C1−C6)アルキル、(C1−C6)アルコキシ、ハロゲンまたはトリフルオロメチ ルによって置換 されていてもよく;そしてR2は、水素である、請求項1に記載の化合物およびそ の製薬上許容できる酸付加塩。 3.R1が水素であり、そしてR2が(C1−C6)アルキルである、請求項2に記載の化 合物。 4.Rが(C1−C6)アルキルである、請求項2に記載の化合物。 5.Xが水素であり、Yが水素であり、そしてRが水素、メチル、エチルまたは プロピルである、請求項4に記載の化合物。 6.1−(プロピル−ピリジン−4−イル−アミノ)−1H−インドール−2,3− ジオンである、請求項4に記載の化合物。 7.1−(ピリジン−4−イル−アミノ)−1H−インドール−2,3−ジオンであ る、請求項5に記載の化合物。 8.Rが、水素、(C1−C6)アルキルまたはヒドロキシ(C1−C6)アルキルであり; Xが、水素、ヒドロキシ、(C1−C6)アルコキシ、ベンジルオキシ、または−O(C =O)NR1R2であり;そしてYが、水素またはハロゲンであり;ここでR1およびR2 は一緒になって、これらが結合している窒素とともにテトラヒドロイソキノリン 基を形成している、請求項1に記載の化合物およびその製薬上許容できる酸付加 塩。 9.XがOC(=O)NR1R2であり、Yが水素である、請求項8に記載の化合物。 10.製薬上許容できる担体および製薬的に有効な量の請求項1に記載の化合物よ り成る医薬組成物。 11.患者に有効量の請求項1に記載の化合物を投与することより成る、低下した コリン作動性機能を特性とする記憶機能障害の軽減が必要な患者を治療する方法 。 12.患者に有効量の請求項1に記載の化合物を投与することより成る、 痛みの軽減が必要な患者を治療する方法。 13.活性医薬物質として使用するための請求項1に記載の化合物。 14.低下したコリン作動性機能を特性とする記憶機能障害の治療薬の製造のため の請求項1に記載の化合物の使用。 15.痛みの治療薬の製造のための請求項1に記載の化合物の使用。 16.式(式中、X、YおよびRは、下に定義する通りである)の化合物を、適当な有機 溶媒の存在において適当な酸化剤と反応させることより成る、式 [式中、 Rは、水素、(C1−C6)アルキルまたはヒドロキシ(C1−C6)アルキルであり; Xは、水素、ヒドロキシ、(C1−C6)アルコキシ、フェニル(C1−C6)アルコキシ 、または−O(C=O)NR1R2であり;そして Yは、水素またはハロゲンであり; ここでR1は、(C1−C6)アルキル、フェニル、またはフェニル(C1−C6)アルキル であって、このフェニル基は場合により(C1−C6)アルキ ル、(C1−C6)アルコキシ、ハロゲンまたはトリフルオロメチルで置換されていて もよく;R2は、水素または(C1−C6)アルキルであるか;または、R1およびR2は一 緒になって、これらが結合している窒素とともにテトラヒドロイソキノリン基を 形成する] の化合物およびその製薬上許容できるカチオン付加塩を製造する方法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US63187096A | 1996-04-12 | 1996-04-12 | |
US08/631,870 | 1996-04-12 | ||
PCT/US1997/003598 WO1997038993A1 (en) | 1996-04-12 | 1997-03-07 | Isatin derivatives as acetylcholinesterase inhibitors and analgesics |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2001508400A true JP2001508400A (ja) | 2001-06-26 |
JP2001508400A5 JP2001508400A5 (ja) | 2004-11-25 |
JP4109718B2 JP4109718B2 (ja) | 2008-07-02 |
Family
ID=24533114
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP53708497A Expired - Fee Related JP4109718B2 (ja) | 1996-04-12 | 1997-03-07 | アセチルコリンエステラーゼ阻害剤および鎮痛剤としてのイサチン誘導体 |
Country Status (19)
Country | Link |
---|---|
EP (1) | EP0892796B1 (ja) |
JP (1) | JP4109718B2 (ja) |
KR (1) | KR20000005379A (ja) |
CN (1) | CN1215399A (ja) |
AR (1) | AR006606A1 (ja) |
AT (1) | ATE207483T1 (ja) |
BR (1) | BR9708655A (ja) |
CA (1) | CA2252039C (ja) |
DE (1) | DE69707659T2 (ja) |
DK (1) | DK0892796T3 (ja) |
ES (1) | ES2165586T3 (ja) |
GR (1) | GR3037006T3 (ja) |
HU (1) | HUP9903473A3 (ja) |
IL (1) | IL126308A0 (ja) |
NO (1) | NO984740L (ja) |
PT (1) | PT892796E (ja) |
TW (1) | TW426678B (ja) |
WO (1) | WO1997038993A1 (ja) |
ZA (1) | ZA972990B (ja) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6218383B1 (en) | 1998-08-07 | 2001-04-17 | Targacept, Inc. | Pharmaceutical compositions for the prevention and treatment of central nervous system disorders |
WO2008055945A1 (en) | 2006-11-09 | 2008-05-15 | Probiodrug Ag | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
EP2091948B1 (en) | 2006-11-30 | 2012-04-18 | Probiodrug AG | Novel inhibitors of glutaminyl cyclase |
MX2009009234A (es) | 2007-03-01 | 2009-12-01 | Probiodrug Ag | Uso nuevo de inhibidores de ciclasa de glutaminilo. |
EP2865670B1 (en) | 2007-04-18 | 2017-01-11 | Probiodrug AG | Thiourea derivatives as glutaminyl cyclase inhibitors |
ES2548913T3 (es) | 2009-09-11 | 2015-10-21 | Probiodrug Ag | Derivados heterocíclicos como inhibidores de glutaminil ciclasa |
CN102905532A (zh) | 2010-02-09 | 2013-01-30 | 约翰斯.霍普金斯大学 | 用于改善认知功能的方法和组合物 |
IN2012DN06631A (ja) | 2010-02-16 | 2015-10-23 | Pfizer | |
ES2586231T3 (es) | 2010-03-03 | 2016-10-13 | Probiodrug Ag | Inhibidores de glutaminil ciclasa |
AU2011226074B2 (en) | 2010-03-10 | 2015-01-22 | Vivoryon Therapeutics N.V. | Heterocyclic inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5) |
EP2560953B1 (en) | 2010-04-21 | 2016-01-06 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
US8530670B2 (en) | 2011-03-16 | 2013-09-10 | Probiodrug Ag | Inhibitors |
CA2891122C (en) | 2012-11-14 | 2021-07-20 | The Johns Hopkins University | Methods and compositions for treating schizophrenia |
BR112015013675B1 (pt) | 2012-12-13 | 2022-04-26 | H. Lundbeck A/S | Composição compreendendo vortioxetina e donepezil e usos dos mesmos |
WO2014144663A1 (en) | 2013-03-15 | 2014-09-18 | The Johns Hopkins University | Methods and compositions for improving cognitive function |
WO2014144801A1 (en) | 2013-03-15 | 2014-09-18 | Agenebio Inc. | Methods and compositions for improving cognitive function |
US10537552B2 (en) | 2015-05-05 | 2020-01-21 | Carafe Drug Innovation, Llc | Substituted 5-hydroxyoxindoles and their use as analgesics and fever reducers |
EA034167B8 (ru) | 2015-05-22 | 2021-04-27 | Эйджинбайо, Инк. | Фармацевтические композиции леветирацетама пролонгированного высвобождения |
DK3461819T3 (da) | 2017-09-29 | 2020-08-10 | Probiodrug Ag | Inhibitorer af glutaminylcyklase |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5296488A (en) * | 1989-08-02 | 1994-03-22 | Hoechst-Roussel Pharmaceuticals Inc. | Method of using 2,3-dihydro-1-(pyridinylamino)-indoles as anticonvulsants and for the enhancement of memory |
US4994472A (en) * | 1989-08-02 | 1991-02-19 | Hoechst-Roussel Pharmaceuticals Incorporated | 1-(pyridinylamino)-2-pyrrolidinones as pain relievers |
US5006537A (en) * | 1989-08-02 | 1991-04-09 | Hoechst-Roussel Pharmaceuticals, Inc. | 1,3-dihydro-1-(pyridinylamino)-2H-indol-2-ones |
-
1997
- 1997-03-07 WO PCT/US1997/003598 patent/WO1997038993A1/en active IP Right Grant
- 1997-03-07 JP JP53708497A patent/JP4109718B2/ja not_active Expired - Fee Related
- 1997-03-07 HU HU9903473A patent/HUP9903473A3/hu unknown
- 1997-03-07 IL IL12630897A patent/IL126308A0/xx unknown
- 1997-03-07 PT PT97908942T patent/PT892796E/pt unknown
- 1997-03-07 CN CN97193728A patent/CN1215399A/zh active Pending
- 1997-03-07 EP EP97908942A patent/EP0892796B1/en not_active Expired - Lifetime
- 1997-03-07 BR BR9708655A patent/BR9708655A/pt not_active Application Discontinuation
- 1997-03-07 DE DE69707659T patent/DE69707659T2/de not_active Expired - Fee Related
- 1997-03-07 AT AT97908942T patent/ATE207483T1/de not_active IP Right Cessation
- 1997-03-07 DK DK97908942T patent/DK0892796T3/da active
- 1997-03-07 CA CA002252039A patent/CA2252039C/en not_active Expired - Fee Related
- 1997-03-07 ES ES97908942T patent/ES2165586T3/es not_active Expired - Lifetime
- 1997-04-07 TW TW086104363A patent/TW426678B/zh active
- 1997-04-08 ZA ZA9702990A patent/ZA972990B/xx unknown
- 1997-04-11 AR ARP970101447A patent/AR006606A1/es unknown
-
1998
- 1998-10-09 NO NO984740A patent/NO984740L/no unknown
- 1998-10-12 KR KR1019980708105A patent/KR20000005379A/ko active IP Right Grant
-
2001
- 2001-10-25 GR GR20010401584T patent/GR3037006T3/el not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
CA2252039C (en) | 2002-12-24 |
EP0892796A1 (en) | 1999-01-27 |
ES2165586T3 (es) | 2002-03-16 |
HUP9903473A3 (en) | 2000-09-28 |
DK0892796T3 (da) | 2001-11-19 |
TW426678B (en) | 2001-03-21 |
EP0892796B1 (en) | 2001-10-24 |
DE69707659T2 (de) | 2002-05-08 |
KR20000005379A (en) | 2000-01-25 |
AU716997B2 (en) | 2000-03-16 |
JP4109718B2 (ja) | 2008-07-02 |
IL126308A0 (en) | 1999-05-09 |
CA2252039A1 (en) | 1997-10-23 |
CN1215399A (zh) | 1999-04-28 |
AU2072597A (en) | 1997-11-07 |
AR006606A1 (es) | 1999-09-08 |
BR9708655A (pt) | 1999-08-03 |
NO984740D0 (no) | 1998-10-09 |
NO984740L (no) | 1998-10-09 |
ATE207483T1 (de) | 2001-11-15 |
ZA972990B (en) | 1997-11-03 |
HUP9903473A2 (hu) | 2000-05-28 |
PT892796E (pt) | 2002-03-28 |
WO1997038993A1 (en) | 1997-10-23 |
DE69707659D1 (de) | 2001-11-29 |
GR3037006T3 (en) | 2002-01-31 |
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