JP2000508297A - 抗高血圧活性を有する新規キナゾリン―4―アミノ―2―(ピペリジン―1―イル―4―置換)誘導体並びにその製造法および医薬用途 - Google Patents
抗高血圧活性を有する新規キナゾリン―4―アミノ―2―(ピペリジン―1―イル―4―置換)誘導体並びにその製造法および医薬用途Info
- Publication number
- JP2000508297A JP2000508297A JP09535770A JP53577097A JP2000508297A JP 2000508297 A JP2000508297 A JP 2000508297A JP 09535770 A JP09535770 A JP 09535770A JP 53577097 A JP53577097 A JP 53577097A JP 2000508297 A JP2000508297 A JP 2000508297A
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- compound
- pharmaceutically acceptable
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- Granted
Links
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
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Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.一般式: 〔式中、Arは非置換ピリジル基(2−,3−もしくは4−イル)もしくはメ トキシあるいはメチル基でモノ置換されたピリジル基; 非置換フリル基(2−もしくは3−イル)もしくはメトキシあるいはメチル基 で置換されたフリル基;または ベンゾフリル基(2−もしくは3−イル); である〕 で示される化合物、または医薬的に許容しうる無機もしくは有機酸から得られる その塩。 2.一般式(I)において、Arが非置換ピリジル基(2−,3−もしくは4 −イル)もしくはメトキシあるいはメチル基でモノ置換されたピリジル基である 請求の範囲1に記載の化合物、またはその医薬的に許容しうる塩。 3.Arが2−ピリジル基である請求の範囲2に記載の化合物、またはその医 薬的に許容しうる塩。 4.一般式(I)において、Arが非置換フリル基(2−もしくは3−イル) もしくはメトキシあるいはメチル基で置換されたフリル基である請求の範囲1に 記載の化合物、またはその医薬的に許容しうる塩。 5.Arが2−フリル基である請求の範囲4に記載の化合物、またはその医薬 的に許容しうる塩。 6.活性成分として、請求の範囲1に記載の化合物またはその医薬的に許容し うる塩の少なくとも1種を含有する医薬製剤。 7.異なる病因を持つ動脈高血圧症の治療に用いる請求の範囲6に記載の医薬 製剤。 8.単独または利尿薬もしくは心臓作用性グリコシド類と併用して、うっ血性 心不全の治療に用いる請求の範囲6に記載の医薬製剤。 9.前立腺肥大、各種尿路障害および一般のノルアドレナリン作用性神経系の 機能亢進または機能不全によって起る病的症状の治療に用いる請求の範囲6に記 載の医薬製剤。 10.ビヒクル、結合剤、芳香剤、分散剤、保存剤、湿潤剤およびこれらの混 合物からなる群から選ばれる医薬的に許容しうる不活性成分、または経皮吸収を 促進する成分、または時間経過にわたって活性成分の制御放出を可能ならしめる 成分をさらに含有する請求の範囲6に記載の医薬製剤。 11.一般式(I)(ここで、Arは請求の範囲1に記載と同意義)の化合物 の製造法であって、式: (式中、Arは前記と同意義である) のピペリジン誘導体(II)を高沸点溶媒、好ましくはイソアミルアルコール中 、プロトン受容体として第4級塩基の存在または非存在下、2−Cl−4−アミ ノ−6,7−ジメトキシキナゾリンと、70〜150℃の温度にて1〜48時間 反応させ、次いで反応媒体から濾過により、化合物(I)をそのまま、あるいは 、好ましくは医薬的に許容しうる塩の形状で単離し、通常の方法で精製すること から成る製造法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IT96A000275 | 1996-04-10 | ||
IT96TO000275A IT1286302B1 (it) | 1996-04-10 | 1996-04-10 | Chinazoline-4-amino-2-(piperidino-1-il-4-sostituite) ad attivita' anti-ipertensiva, procedimento per la loro preparazione e loro uso |
PCT/EP1996/003370 WO1997037979A1 (en) | 1996-04-10 | 1996-07-31 | New quinazoline-4-amino-2-(piperidine-1-yl-4-substituted) derivatives having anti-hypertensive activity, a method for their preparation and their pharmaceutical use |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2000508297A true JP2000508297A (ja) | 2000-07-04 |
JP3987113B2 JP3987113B2 (ja) | 2007-10-03 |
Family
ID=11414541
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP53577097A Expired - Lifetime JP3987113B2 (ja) | 1996-04-10 | 1996-07-31 | 抗高血圧活性を有する新規キナゾリン―4―アミノ―2―(ピペリジン―1―イル―4―置換)誘導体並びにその製造法および医薬用途 |
Country Status (11)
Country | Link |
---|---|
US (1) | US5985885A (ja) |
EP (1) | EP0892790B1 (ja) |
JP (1) | JP3987113B2 (ja) |
AT (1) | ATE264312T1 (ja) |
AU (1) | AU6788596A (ja) |
CA (1) | CA2251308A1 (ja) |
DE (1) | DE69632206T2 (ja) |
ES (1) | ES2216057T3 (ja) |
IT (1) | IT1286302B1 (ja) |
PT (1) | PT892790E (ja) |
WO (1) | WO1997037979A1 (ja) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2015019365A1 (en) | 2013-08-07 | 2015-02-12 | Cadila Healthcare Limited | N-cyanomethylamides as inhibitors of janus kinase |
US9682955B2 (en) * | 2014-09-09 | 2017-06-20 | Janssen Pharmaceutica Nv | Quinazoline derivatives useful as CB-1 inverse agonists |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3511836A (en) * | 1967-12-13 | 1970-05-12 | Pfizer & Co C | 2,4,6,7-tetra substituted quinazolines |
GB1383409A (en) * | 1972-09-09 | 1974-02-12 | Pfizer Ltd | Derivatives of 2-amino- and 4-amino-quinazoline and pharmaceutical compositions containing them |
US4287341A (en) * | 1979-11-01 | 1981-09-01 | Pfizer Inc. | Alkoxy-substituted-6-chloro-quinazoline-2,4-diones |
US4351832A (en) * | 1980-04-18 | 1982-09-28 | American Home Products Corporation | 2-(Piperazinyl)-4-pyrimidinamines |
FI70411C (fi) * | 1980-12-29 | 1986-09-19 | Pfizer | Foerfarande foer framstaellning av nya antihypertensiva 4-amino-6,7-dimetoxi-2-piperazinokinazolin derivat |
DE3336409A1 (de) * | 1983-10-06 | 1985-04-18 | Ludwig Heumann & Co GmbH, 8500 Nürnberg | Chinazolinderivate, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
CA1307786C (en) * | 1984-12-14 | 1992-09-22 | Keiichi Yokoyama | Quinazoline derivatives and antihypertensive preparations containing same as effective components |
CA2077252C (en) * | 1992-08-31 | 2001-04-10 | Khashayar Karimian | Methods of making ureas and guanidines, and intermediates therefor |
IT1270993B (it) * | 1994-03-18 | 1997-05-26 | Recordati Chem Pharm | Derivati chinzolilamminici attivi come alfa-antagonisti |
-
1996
- 1996-04-10 IT IT96TO000275A patent/IT1286302B1/it active IP Right Grant
- 1996-07-31 JP JP53577097A patent/JP3987113B2/ja not_active Expired - Lifetime
- 1996-07-31 WO PCT/EP1996/003370 patent/WO1997037979A1/en active IP Right Grant
- 1996-07-31 ES ES96928398T patent/ES2216057T3/es not_active Expired - Lifetime
- 1996-07-31 US US09/155,993 patent/US5985885A/en not_active Expired - Lifetime
- 1996-07-31 DE DE69632206T patent/DE69632206T2/de not_active Expired - Fee Related
- 1996-07-31 PT PT96928398T patent/PT892790E/pt unknown
- 1996-07-31 AU AU67885/96A patent/AU6788596A/en not_active Abandoned
- 1996-07-31 CA CA002251308A patent/CA2251308A1/en not_active Abandoned
- 1996-07-31 EP EP96928398A patent/EP0892790B1/en not_active Expired - Lifetime
- 1996-07-31 AT AT96928398T patent/ATE264312T1/de not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
IT1286302B1 (it) | 1998-07-08 |
DE69632206T2 (de) | 2005-04-28 |
WO1997037979A1 (en) | 1997-10-16 |
US5985885A (en) | 1999-11-16 |
JP3987113B2 (ja) | 2007-10-03 |
PT892790E (pt) | 2004-06-30 |
CA2251308A1 (en) | 1997-10-16 |
DE69632206D1 (de) | 2004-05-19 |
AU6788596A (en) | 1997-10-29 |
ES2216057T3 (es) | 2004-10-16 |
ATE264312T1 (de) | 2004-04-15 |
EP0892790A1 (en) | 1999-01-27 |
EP0892790B1 (en) | 2004-04-14 |
ITTO960275A0 (ja) | 1996-04-10 |
ITTO960275A1 (it) | 1997-10-10 |
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