KR890013013A - 뉴우트로픽 활성을 갖는 신규의 화합물, 이의 제조방법 및 이들 함유하는 치료제 - Google Patents
뉴우트로픽 활성을 갖는 신규의 화합물, 이의 제조방법 및 이들 함유하는 치료제 Download PDFInfo
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- KR890013013A KR890013013A KR1019890001446A KR890001446A KR890013013A KR 890013013 A KR890013013 A KR 890013013A KR 1019890001446 A KR1019890001446 A KR 1019890001446A KR 890001446 A KR890001446 A KR 890001446A KR 890013013 A KR890013013 A KR 890013013A
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Abstract
내용 없음.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (17)
- 하기식 (1)의 화합물.상기식에서, R1은 수소, C1-4알킬, CHR6CONHR7또는 CHR6COOR7이고; R6및 R7은 각각 수소 또는 C1-4알킬이고; R2는 수소, C1-5알킬 또는 아미노산 R2CH(NH)COOH의 잔기 R2이며; R3은 수 TH, C1-4알킬, CONH2또는 CO2R8이고; R8은 수소 또는 C1-4알킬이며; n은 2, 3 또는 4임.
- 제1항에 있어서, R1내지 R3은 각각 수소인 화합물.
- 제1항에 있어서, 하기 그룹으로부터 선택된 화합물. 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. 2,5-디옥소-7a-메틸헥사하이드로-1H-피롤로[1,2-a]이미다졸. (3S)-3,7a-디메틸-2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. (3R,S)-3,7a-디메틸-2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. (3S)-2,5-디옥소-3-메틸헥사하이드로-1H-피롤로[1,2-a]이미다졸. (3R,S)-2,5-디옥소-3-메틸헥사하이드로-1H-[1,2-a]이미다졸. (3S)-2,5-디옥소-3-이소부틸헥사하이드로-1H-피롤로[1,2-a]이미다졸. 2,5-디옥소-3-에틸헥사하이드로-1H-피롤로[1,2-a]이미다졸. 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. 에틸 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸-1-아세테이트. 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸-1-아세트이미드. (3S)-3-벤질-2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. (3S)-3-히드록시메틸-2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸-7a-카르복실 산. 에틸 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸-7a-카르복실레이트. 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸-7a-카르복실레이트. 2,5-디옥소-1H-옥타하이드로이미다졸[1,2-a]피리딘 또는 2,5-디옥소-1H-옥타하이드로이미다조[1,2-a]아제핀.
- 하기식 (4)의 화합물.상기식에서 R1내지 R3및 n은 제1항의 식(1)의 화합물에서 정의된 바와 동일하며, R4는 수소이고, R5는 수소, C1-4알킬 또는 벤질임.
- 제1항에 있어서, 정의된 바의 식(1)의 화합물과 약학적 허용 담체로 구성되는 약학적 조성물.
- 제5항에 있어서, 식(1)의 화합물은 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸인 약학적 조성물.
- 제1항에 있어서, 식 (1)의 화합물은 치료제로서 사용되는 것을 특징으로 하는 화합물.
- 제1항에 있어서, 식(1)의 화합물은 뉴우트로픽제(nootropicagent)로서 사용되는 것을 특징으로 하는 화합물.
- 제1항에 있어서, a) 식(2)의 화합물을 식(3)의 화합물과 반응시키거나 b) 식(4)의 화합물을 고리화하는 반응을 포함하는 것을 특징으로 하는 식(1)의 화합물의 제조방법.상기식에서, R1은 수소, C1-4알킬, CHR6CONHR7또는 CHR6COOR7이고; R6및 R7은 각각 수소 또는 C1-4알킬이고; R2는 수소, C1-4알킬 또는 아미노산 R2CH(NH)COOH의 잔기 R2이며; R3은 수소, C1-4알킬, CONH2또는 CO2R7은 수소 또는 C1-4알킬이며; n은 2,3 또는 4이고; R4는 수소이고; R5는 수소, C1-4알킬 또는 벤질임.
- 제9항에 있어서, a) 단계의 반응이 염기의 존재하에서 실시되는 방법.
- 제10항에 있어서, 염기가 수산화나트륨 또는 탄산나트륨으로부터 선택된 방법.
- 제9항에 있어서, b)단계의 고리화 반응이 수산화암모늄의 존재하에 실시되는 방법.
- 제9항 내지 제12항중 어느 한 항에 있어서, 식(1)의 화합물에서 R1내지 R3이 각각 수소인 방법.
- 제9항에 내지 제12항중 어느 한 항에 있어서, 제조된 식 (1)의 화합물이 하기 그룹으로부터 선택되는 방법.2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. 2,5-디옥소-7a-메틸헥사하이드로-1H-피롤로[1,2-a]이미다졸. (3S)-3,7a-디메틸-2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. (3R,S)-3,7a-디메틸-2,5-디옥소헥사하이드로-1H-피롤 로[1,2-a]이미다졸. (3S)-2,5-디옥소-3-메틸헥사하이드로-1H-피롤로[1,2-a]이미다졸. (3R,S)-2,5-디옥소-3-메틸헥사하이드로-1H-[1,2-a]이미다졸. (3S)-2,5-디옥소-3-이소부틸헥사하이드로-1H-피롤로[1,2-a]이미다졸. 2,5-디옥소-3-에틸헥사하이드로-1H-피롤로[1,2-a]이미다졸. 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. 에틸 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸-1-아세테이트. 2,5-디독소헥사하이드로-1H-피롤로[1,2-a]이미다졸-1-아세트이미드. (3S)-3-벤질-2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. (3S)-3-히드록시메틸-2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸-7a-카르복실 산. 에틸 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸-7a-카르복실레이트. 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸-7a-카르복실레이트. 2,5-디옥소-1H-옥타하이드로이미다졸[1,2-a]피리딘 또는 2,5-디옥소-1H-옥타하이드로이미다조[1,2-a]아제핀.
- 제1항에서 정의된 바의 식 (1)의 화합물과 약학적 허용담체를 조합시키는 것을 포함하는 약학적 조성물의 제조방법.
- 제15항에 있어서, 식(1)의 화합물이 하기 그룹으로부터 선택되는 방법.2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. 2,5-디옥소-7a-메틸헥사하이드로-1H-피롤로[1,2-a]이미다졸. (3S)-3,7a-디메틸-2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. (3R,S)-3,7a-디메틸-2,5-디옥소헥사하이드로-1H-피 롤로[1,2-a]이미다졸. (3S)-2,5-디옥소-3-메틸헥사하이드로-1H-피롤로[1,2-a]이미다졸. (3R,S)-2,5-디옥소-3-메틸헥사하이드로-1H-[1,2-a]이미다졸. (3S)-2,5-디옥소-3-이소부틸헥사하이드로-1H-피롤로[1,2-a]이미다졸. 2,5-디옥소-3-에틸헥사하이드로-1H-피롤로[1,2-a]이미다졸. 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. 에틸 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸-1-아세테이트. 2,5-디독소헥사하이드로-1H-피롤로[1,2-a]이미다졸-1-아세트이미드. (3S)-3-벤질-2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. (3S)-3-히드록시메틸-2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸. 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸-7a-카르복실산. 에틸 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸-7a-카르복실레이트. 2,5-디옥소헥사하이드로-1H-피롤로[1,2-a]이미다졸-7a-카르복실레이트. 2,5-디옥소-1H-옥타하이드로이미다졸[1,2-a]피리딘 또는 2,5-디옥소-1H-옥타하이드로이미다조[1,2-a]아제핀.
- 하기식(A)의 화합물을 환원하는 것으로 구성되는 R3은 수소이고, R5가 이소부틸인 제9항에서 정의된 바의 식 (3)의 화합물의 제조방법.HCOCH=CHCO2iBU (A)※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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IT19336A/88 | 1988-02-08 | ||
IT8819336A IT1233860B (it) | 1988-02-08 | 1988-02-08 | Derivati del peridroazacicloalca (1,2-a) imidazolo ad attivita' nootropa |
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US (2) | US5053422A (ko) |
EP (1) | EP0335483A3 (ko) |
JP (1) | JPH01246281A (ko) |
KR (1) | KR890013013A (ko) |
CN (1) | CN1036204A (ko) |
AU (2) | AU616240B2 (ko) |
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DK (1) | DK55089A (ko) |
FI (1) | FI890438A (ko) |
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TW304167B (ko) * | 1995-01-30 | 1997-05-01 | Lilly Co Eli | |
PE17897A1 (es) * | 1995-02-17 | 1997-06-12 | Lilly Co Eli | Formulacion transdermica en parche del 3-(4-butiltio)-1,2,5-tiadiazol-3-il)-1-azabiciclo (2,2,2) octano |
IL118323A (en) * | 1995-06-02 | 1999-11-30 | Akzo Nobel Nv | 3,8-Diamino-8- hydroxyimidazo (1,5-a) pyridine -1(5H)-one derived serine protease inhibitors and pharmaceutical compositions containing them |
JP3905409B2 (ja) | 2002-04-10 | 2007-04-18 | タレックス光学工業株式会社 | 光学レンズ成型用ポリウレタン樹脂組成物および耐衝撃性合成樹脂レンズ |
ITMI20030573A1 (it) * | 2003-03-24 | 2004-09-25 | Nikem Research Srl | Composti ad azione nootropica, loro preparazione, |
ITMI20070770A1 (it) | 2007-04-16 | 2008-10-17 | Brane Discovery S R L | Impiego di dimiracetam nel trattamento del dolore cronico |
US9593209B2 (en) | 2009-10-22 | 2017-03-14 | Dow Corning Corporation | Process for preparing clustered functional polyorganosiloxanes, and methods for their use |
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US9862867B2 (en) | 2013-02-11 | 2018-01-09 | Dow Corning Corporation | Alkoxy-functional organopolysiloxane resin and polymer and related methods for forming same |
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US3334099A (en) * | 1965-03-31 | 1967-08-01 | Sandoz Ag | Novel pyrrolo-diazepines, pyrrolo-imidazolidines, and pyrrolo-pyrimidines |
CA1067079A (en) * | 1976-07-22 | 1979-11-27 | Yamanouchi Pharmaceutical Co. | Nitrogen-containing heterobicyclic compounds |
US4372966A (en) * | 1980-09-15 | 1983-02-08 | Warner-Lambert Company | Use of dihydro-1H-pyrrolizine-3,5(2H,6H)-dione as a cognition activator |
US4582838A (en) * | 1984-08-24 | 1986-04-15 | Warner-Lambert Company | Derivatives of dihydro-1H-pyrrolo[1,2-c]imidazol-3,5-dione as cognition activators |
US4677098A (en) * | 1985-11-22 | 1987-06-30 | Warner-Lambert Company | Substituted dihydro-1H-pyrolizine-3,5(2H,6H)-diones |
JPS62289581A (ja) * | 1986-06-09 | 1987-12-16 | Idemitsu Kosan Co Ltd | イミダゾピロリンジオン誘導体,その製造方法およびそれを有効成分とする除草剤 |
JPS62292783A (ja) * | 1986-06-12 | 1987-12-19 | Idemitsu Kosan Co Ltd | イミダゾピロリンジオン誘導体,その製造方法およびそれを有効成分として含有する除草剤 |
-
1988
- 1988-02-08 IT IT8819336A patent/IT1233860B/it active
-
1989
- 1989-01-30 FI FI890438A patent/FI890438A/fi not_active Application Discontinuation
- 1989-02-02 NZ NZ227833A patent/NZ227833A/xx unknown
- 1989-02-03 ZW ZW14/89A patent/ZW1489A1/xx unknown
- 1989-02-03 BR BR898900541A patent/BR8900541A/pt unknown
- 1989-02-04 CN CN89101740A patent/CN1036204A/zh active Pending
- 1989-02-06 EP EP19890301123 patent/EP0335483A3/en not_active Ceased
- 1989-02-06 ZA ZA89894A patent/ZA89894B/xx unknown
- 1989-02-06 CA CA000590213A patent/CA1324378C/en not_active Expired - Lifetime
- 1989-02-06 US US07/307,012 patent/US5053422A/en not_active Expired - Lifetime
- 1989-02-06 DD DD89325551A patent/DD283393A5/de not_active IP Right Cessation
- 1989-02-06 DD DD89337916A patent/DD291996A5/de not_active IP Right Cessation
- 1989-02-07 HU HU904864A patent/HU204794B/hu not_active IP Right Cessation
- 1989-02-07 PL PL1989277610A patent/PL158198B1/pl unknown
- 1989-02-07 AU AU29692/89A patent/AU616240B2/en not_active Ceased
- 1989-02-07 HU HU89574A patent/HU203104B/hu not_active IP Right Cessation
- 1989-02-07 RU SU894613489A patent/RU1799383C/ru active
- 1989-02-07 NO NO890515A patent/NO168424C/no unknown
- 1989-02-07 DK DK055089A patent/DK55089A/da not_active Application Discontinuation
- 1989-02-08 KR KR1019890001446A patent/KR890013013A/ko not_active Application Discontinuation
- 1989-02-08 RO RO138146A patent/RO104070B1/ro unknown
- 1989-02-08 JP JP1029571A patent/JPH01246281A/ja active Pending
- 1989-02-08 RO RO145765A patent/RO105965B1/ro unknown
- 1989-02-08 RO RO145764A patent/RO105964B1/ro unknown
- 1989-02-08 PT PT89657A patent/PT89657B/pt active IP Right Grant
- 1989-02-08 RO RO145763A patent/RO105963B1/ro unknown
-
1991
- 1991-03-15 US US07/669,806 patent/US5130319A/en not_active Expired - Lifetime
- 1991-07-01 AU AU79479/91A patent/AU7947991A/en not_active Abandoned
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