JPWO2005073218A1 - バイパス術に伴う血管攣縮治療剤 - Google Patents
バイパス術に伴う血管攣縮治療剤 Download PDFInfo
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- JPWO2005073218A1 JPWO2005073218A1 JP2005517484A JP2005517484A JPWO2005073218A1 JP WO2005073218 A1 JPWO2005073218 A1 JP WO2005073218A1 JP 2005517484 A JP2005517484 A JP 2005517484A JP 2005517484 A JP2005517484 A JP 2005517484A JP WO2005073218 A1 JPWO2005073218 A1 JP WO2005073218A1
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- 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
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
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- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- Life Sciences & Earth Sciences (AREA)
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- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Surgery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Description
一方、一般式(I)で示される化合物は、Rhoキナーゼ、ミオシン軽鎖リン酸化酵素、プロテインキナーゼCといったキナーゼ阻害活性を有し、血管平滑筋弛緩作用、血流増加作用、血圧低下作用、脳、心臓保護作用等を示し、血管拡張剤(特に、狭心症治療剤)、高血圧治療剤、脳、心臓保護剤、動脈硬化症治療剤等において有効な物質であることは既に公知である(例えば、特許文献1〜9及び非特許文献2〜5)。
(1)下記一般式(I)
(2)当該バイパス術が、冠動脈バイパス術である(1)記載のバイパス術に伴う血管攣縮の予防及び/または治療剤、
(3)攣縮が、カルシウム拮抗剤及び/又はニトロ化合物に不応の攣縮である(1)あるいは(2)に記載のバイパス術に伴う血管攣縮の予防及び/または治療剤、(4)攣縮が、吻合部位と異なる部位で発生したものである(1)〜(3)のいずれかに記載のバイパス術に伴う血管攣縮の予防及び/または治療剤、である。
Pharam. Bull., 40, (3) 770-773 (1992)、特開昭61-152658号公報等に記載されている方法に従って合成することができる。また、本発明の一般式(I)で示される化合物の酸付加塩は、薬学上許容される非毒性の塩が好ましく、例えば塩酸、臭化水素酸、リン酸、硫酸等の無機酸、および酢酸、クエン酸、酒石酸、乳酸、コハク酸、フマル酸、マレイン酸、メタンスルホン酸等の有機酸の塩を挙げることができる。また、本発明の一般式(I)で示される化合物の水和物としては、例えば1/2水和物、1水和物、3水和物が例示される。
非経口的に筋肉内注射、静脈内注射、皮下注射で投与する場合、一般式(I)で示される化合物またはその酸付加塩もしくは水和物を等張にするために、食塩または、グルコース等の他の溶質を添加した無菌溶液として投与される。
併用薬剤を併用し、バイパス術に伴う血管攣縮を予防あるいは治療する場合の用量としては、一般式(I)で示される化合物またはその酸付加塩もしくは水和物の用量を1とした場合、他剤(例えばカルシウム拮抗剤やニトロ化合物)の用量として、1/500から1が例示される。
下記表2の成分を注射用蒸留水に溶解し、その後、注射用蒸留水を添加し、必要な最終重量とし、この溶液2mlをアンプルに密封し、加熱滅菌した。
下記表3の成分を含む錠剤を常法により調製した。
Claims (4)
- 下記一般式(I)
(ただし、式中R1は水素原子または水酸基を表す)で示される化合物またはその酸付加塩、もしくは水和物を有効成分とするバイパス術に伴う血管攣縮の予防及び/または治療剤。 - 当該バイパス術が、冠動脈バイパス術である請求項1記載のバイパス術に伴う血管攣縮の予防及び/または治療剤。
- 攣縮が、カルシウム拮抗剤及び/又はニトロ化合物に不応の攣縮である請求項1あるいは2に記載のバイパス術に伴う血管攣縮の予防及び/または治療剤。
- 攣縮が、吻合部位と異なる部位で発生したものである請求項1〜3のいずれかに記載のバイパス術に伴う血管攣縮の予防及び/または治療剤。
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2005517484A JP4854070B2 (ja) | 2004-01-29 | 2005-01-27 | バイパス術に伴う血管攣縮治療剤 |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2004020882 | 2004-01-29 | ||
JP2004020882 | 2004-01-29 | ||
JP2005517484A JP4854070B2 (ja) | 2004-01-29 | 2005-01-27 | バイパス術に伴う血管攣縮治療剤 |
PCT/JP2005/001102 WO2005073218A1 (ja) | 2004-01-29 | 2005-01-27 | バイパス術に伴う血管攣縮治療剤 |
Publications (2)
Publication Number | Publication Date |
---|---|
JPWO2005073218A1 true JPWO2005073218A1 (ja) | 2007-09-06 |
JP4854070B2 JP4854070B2 (ja) | 2012-01-11 |
Family
ID=34823769
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2005517484A Active JP4854070B2 (ja) | 2004-01-29 | 2005-01-27 | バイパス術に伴う血管攣縮治療剤 |
Country Status (6)
Country | Link |
---|---|
US (1) | US20080242660A1 (ja) |
EP (1) | EP1710243A4 (ja) |
JP (1) | JP4854070B2 (ja) |
CN (1) | CN1914194B (ja) |
CA (1) | CA2555763A1 (ja) |
WO (1) | WO2005073218A1 (ja) |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS61152658A (ja) * | 1984-12-27 | 1986-07-11 | Asahi Chem Ind Co Ltd | 置換されたイソキノリンスルホンアミド誘導体 |
JPS61227581A (ja) * | 1985-04-02 | 1986-10-09 | Asahi Chem Ind Co Ltd | 血管拡張剤 |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4678783B1 (en) * | 1983-11-04 | 1995-04-04 | Asahi Chemical Ind | Substituted isoquinolinesulfonyl compounds |
JP2893029B2 (ja) * | 1992-08-10 | 1999-05-17 | 旭化成工業株式会社 | 心臓保護剤 |
EP0870767B1 (en) * | 1995-07-03 | 2000-02-16 | Asahi Kasei Kogyo Kabushiki Kaisha | 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride hydrates |
KR19990082174A (ko) * | 1996-02-02 | 1999-11-25 | 니뽄 신야쿠 가부시키가이샤 | 이소퀴놀린 유도체 및 의약 |
ATE401082T1 (de) * | 2001-09-11 | 2008-08-15 | Asahi Kasei Pharma Corp | Medizinische zusammensetzung zur prävention oder behandlung von zerebrovaskulären störungen |
US20030162824A1 (en) * | 2001-11-12 | 2003-08-28 | Krul Elaine S. | Methods of treating or preventing a cardiovascular condition using a cyclooxygenase-1 inhibitor |
US20040162824A1 (en) * | 2003-02-13 | 2004-08-19 | Burns Roland John | Method and apparatus for classifying a document with respect to reference corpus |
WO2006058202A2 (en) * | 2004-11-24 | 2006-06-01 | The Regents Of The University Of Colorado | Mer diagnostic and therapeutic agents |
-
2005
- 2005-01-27 WO PCT/JP2005/001102 patent/WO2005073218A1/ja not_active Application Discontinuation
- 2005-01-27 JP JP2005517484A patent/JP4854070B2/ja active Active
- 2005-01-27 US US10/597,357 patent/US20080242660A1/en not_active Abandoned
- 2005-01-27 CN CN2005800034806A patent/CN1914194B/zh active Active
- 2005-01-27 CA CA002555763A patent/CA2555763A1/en not_active Abandoned
- 2005-01-27 EP EP05709376A patent/EP1710243A4/en not_active Withdrawn
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS61152658A (ja) * | 1984-12-27 | 1986-07-11 | Asahi Chem Ind Co Ltd | 置換されたイソキノリンスルホンアミド誘導体 |
JPS61227581A (ja) * | 1985-04-02 | 1986-10-09 | Asahi Chem Ind Co Ltd | 血管拡張剤 |
Also Published As
Publication number | Publication date |
---|---|
US20080242660A1 (en) | 2008-10-02 |
CN1914194A (zh) | 2007-02-14 |
WO2005073218A1 (ja) | 2005-08-11 |
EP1710243A1 (en) | 2006-10-11 |
EP1710243A4 (en) | 2009-09-23 |
CN1914194B (zh) | 2011-08-31 |
JP4854070B2 (ja) | 2012-01-11 |
CA2555763A1 (en) | 2005-08-11 |
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