KR860009008A - 항정신병의 융합-고리의 피리디닐 피페라진 유도체 - Google Patents
항정신병의 융합-고리의 피리디닐 피페라진 유도체 Download PDFInfo
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- KR860009008A KR860009008A KR1019860003445A KR860003445A KR860009008A KR 860009008 A KR860009008 A KR 860009008A KR 1019860003445 A KR1019860003445 A KR 1019860003445A KR 860003445 A KR860003445 A KR 860003445A KR 860009008 A KR860009008 A KR 860009008A
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- 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
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- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
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Abstract
Description
Claims (42)
- 일반식(Ⅰ)의 화합물과 이 화합물의 제약상 허용 가능한 산부가염.이식에서, Z는 다음의 기들; R3와 R4가 수소, 저급알킬에서 독립적으로 선택되거나, C3-C6알킬렌 사슬로서 함께 존재할 수 있는R5와 R6가 수소, 저급알킬 및 A가 수소나 할로겐인 A-치환된 페닐로부터 독립적으로 선택되거나, R5와 R6가 부틸렌 사슬로서 함께 존재하고 W가 S이거나 CH2인V가 O이거나 S인G가 수소, 저급알킬, 저급알콕시, 또는 할로겐에서 선택되고, m이 1-4 정수이며, U는 C=O이거나 SO2인중에서 선택되고, n은 Z가(e)일때, n이 3인 것을 조건으로 정수 2-4이며; X나 Y중의 하나는 또 다른 X나 Y가 항상 =CH-이어야 하는 것을 조건으로 CH2, O, S 혹은 NR7에서 독립적으로 선택되며; R1과 R7은 수소나 저급알킬로부터 독립적으로 선택되며; R2는 수소, 저급알킬, 저급알콕시, 저급알킬티오, 할로겐 또는 수산기로부터 선택된다.
- Z가 기(a)인 청구범위 제1항에 화합물.
- Z가 기(b)인 청구범위 제1항에 화합물.
- Z가 기(c)인 청구범위 제1항에 화합물.
- Z가 기(d)인 청구범위 제1항에 화합물.
- Z가 기(e)인 청구범위 제1항에 화합물.
- Y가 산소원자인 청구범위 제1항의 화합물.
- Y가 유황원소인 청구범위 제1항의 화합물.
- R5와 R6가 부틸렌사슬로서 동시에 존재하고, W가 황인 청구범위 제3항의 화합물.
- V가 산소원자인 제4항의 화합물.
- Z가 기 (a), (c) 또는 (e)인 청구범위 제7항의 화합물.
- Z가 기 (a), (c) 또는 (e)인 청구범위 제8항의 화합물.
- 청구범위 제2항의 화합물, 1-[4-[4-(푸로- 3,2-c) 피리딘-4-일]-1-피페라지닐]부틸]-4,4-디메틸-2,6-피페리딘디온.
- 청구범위 제2항의 화합물, 4,4-디메틸-1-[4-[4-(2-메틸푸로-[3,2-c] 피리딘-4-일]-1-피페라지닐]부틸]-2,6-피페리딘디온.
- 청구범위 제2항의 화합물, 4,4-디메틸-1-[4-[4-(티에노[3,2-c] 피리딘-4-일]-1-피페라지닐]부틸]-2,6-피페리딘디온.
- 청구범위 제2항의 화합물, 4,4-디메틸-1-[4-[4-(1-메틸-1H-피롤로[3,2-c] 피리딘-4-일]-1-피페라지닐]부틸]-2,6-피페리딘디온.
- 청구범위 제2항의 화합물, 4,4-디메틸-1-[4-[4-(2-브로모티에노 3,2-c] 피리딘-4-일)-1-피페라지닐]부틸]-2,6-피페리딘디온.
- 청구범위 제2항의 화합물, 1-[4-[4-(티에노-[3,2-c) 피리딘-4-일)-1-피페라지닐]부틸]1,6-피페리딘디온.
- 청구범위 제2항의 화합물, 4-메틸-1-[4-[4-(티에노[3,2-c]-피리딘-4-일)-1-피페라지닐]부틸]-1,6-피페리딘디온.
- 청구범위 제3항의 화합물, 3-[4-[4-(푸로[3,2-c]- 피리딘-4-일)-1-피페라지닐]부틸]-1-티아-3-아자스피로[4,4]-논안-2,4-디온.
- 청구범위 제3항의 화합물, 3-[4-[4-(2-메틸-푸로[3,2-c]- 피리딘-4-일)-1-피페라지닐]부틸]-1-티아-3-아자-스피로[4,4]노난-2,4-디온.
- 청구범위 제3항의 화합물, 3-[4-[4-(티에노-[3,2-c]피리딘-4-일)-1-피페라지닐]부틸]-1-티아-3-아자스피로[4,4]노난-2,4-디온.
- 청구범위 제3항의 화합물, 3-[4-[4-(1-메틸-피롤로[3,2-c]피리딘-4-일)-1-피페라지닐]부틸]-1-티아-3-아자스피로[4,4]노난-2,4-디온.
- 청구범위 제3항의 화합물, 3-[4-[4-(2-브로모-티에노[3,2-c]피리딘-4-일)-2-피페라지닐]부틸]-1-티아-3-아자스피로[4,4]노난-2,4-디온.
- 청구범위 제3항의 화합물, 3-[4-[4-(2-메틸-티에노[3,2-c]피리딘-4-일)-1-피페라지닐]부틸]-1-티아-3-아자스피로[4,4]노난-2,4-디온.
- 청구범위 제1항의 화합물, 3-[4-[4-(티에노-[2,3-c]피리딘-7-일)-1-피페라지닐]부틸]-1-티아-3-아자스피로[4,4]노난-2,4-디온.
- 청구범위 제4항의 화합물, 4-[4-[4-(4-푸로-[3,2-c]피리디닐)-1-피페라지닐]부틸]-3,5-모르폴린디온.
- 청구범위 제4항의 화합물, 4-[4-[4-(1-메틸-1H-피롤로[3,2-c]피리딘-4-일-1-피페라지닐]부틸]3,5-모르폴린디온.
- 청구범위 제4항의 화합물, 4-[4-[4-(4-티에노[3,2-c]피리디닐)-1-피페라지닐]부틸]-3,5-티오모르폴린디온.
- 청구범위 제4항의 화합물, 4-[4-[4-(4-티에노[3,2-c]피리디닐)-1-피페라지닐]부틸]-3,5-모르폴린디온.
- 청구범위 제5항의 화합물, 2-[4-[4-(티에노-[3,2-c]피리딘-4-일-1-피페라지닐]부틸]-1H이소인돌-1,3-(2H)-디온.
- 청구범위 제5항의 화합물, 2-[4-[4-(티에노-[3,2-c]피리딘-4-일-1-피페라지닐]부틸]-1,2-벤즈이소티아졸-3(1H)은 1,1-디옥사이드.
- 청구범위 제6항의 화합물, α-(4-플루오로페닐)-4-(푸로[3,2-c]피리딘-4-일)-1-피페라지닐부탄올.
- 청구범위 제6항의 화합물, α-(4-플루오로페닐)-4(2-메틸푸로[3,2-c]피리딘-4-일)-1-피페라진부타놀.
- 청구범위 제6항의 화합물, α-(4-플루오로페닐)-4(티에노[3,2-c]피리딘-4-일)-1-피페라진부탄올.
- 청구범위 제1항에서 청구된 화합물을 항전신병적인 유효량으로 포유동물에 투여하는 것으로 구성되는 원치않는 정신병 상태를 개선하기 위한 방법.
- 청구범위 제15항에서 청구된 화합물을 투여하는 것으로 구성되는 청구범위 제28항의 방법.
- 청구범위 제23항에서 청구된 화합물을 투여하는 것으로 구성되는 청구범위 제28항의 방법.
- 제약용 담체와, 청구범위 제1항에서, 청구한 화합물들로부터 선택된 활성 화합물을 약1-500mg으로 구성되는 포유동물 숙주에 계통 투여하기에 적합한 투여단위 형태로된 제약조성물.
- 활성화합물이 청구범위 제15항에서 청구된 화합물인 청구범위 제31항의 제약조성물.
- 활성화합물이 청구범위 제23항에서 청구된 화합물인 청구범위 제31항의 제약조성물.
- 일반식(Ⅰ)의 화합물과 이 화합물의 제약상허용 가능한 산부가염을 제조하는 방법.이 식에서, Z는 다음의 기들; R3와 R4가 수소, 저급알킬에서 독립적으로 선택되거나, C3-C6알킬렌 사슬로서 함께 존재할 수 있는R5와 R6가 수소, 저급알킬 및 A가 수소나 할로겐인 치환된 페닐로부터 독립적으로 선택되거나, R5와 R6가 부틸렌 사슬로서 함께 존재하고 W가 S이거나 CH2인V가 O이거나 S인G가 수소, 저급알킬, 저급알콕시, 또는 할로겐에서 선택되고, m이 1-4정수니며,U는 C=O이거나 SO2인중에서 선택되고, n은 Z가 (e)일때, n이 3인 것을 조건으로 정수 2-4이며; X나 Y중의 하나는 또 다른 X나 Y가 항상 =CH-이어야 하는 것을 조건으로 CH2, O, S 혹은 NR7에서 독립적으로 선택되며; R1과 R7은 수소나 저급알킬로부터 독립적으로 선택되며; R2는 수소, 저급알킬, 저급알콕시, 저급알킬티오, 할로겐 또는 수산기로부터 선택며, 이 공정은 다음과 같이 구성되는 공정그룹으로부터 선책된 한가지 공정으로 이루어져 있다. (a) 기호 "D" 가 일반식 a'-d',의 2가 구조인 일반식 (Ⅱa)의 중간체를 R1, R2, n, X 와 Y가 앞서 정의한 바와 같은 일반식(Ⅲc)의 중간체와,반응시켜서 일반식(Ⅰ)의 생성물을 얻는 것과; (b) 일반식(Ⅱb)의 화합바물을,Q가 염화물, 취화물, 요오드화물, 황산염, 인산염, 토실레이트 또는 메실레이트이고, D, R1, R2, n, X 와 Y는 앞서 정의한 바와 같은 일반식(Ⅲb)의 중간체 화합물과 반응시켜서 일반식(Ⅰ)의 제품을 얻는 것;(c) 일반식(Ⅱb)의 화합물을 Q, R1, R2, n, X 및 Y가 앞서 정의한 바와 같은 일반식(Ⅱb')의 중간체 화합물과,반응시켜서 n이 정수 4로 고정된 일반식(Ⅰ)의 제품을 얻는것; (d) 일반식(Ⅱc)의 화합물,D, n, R1, R2, n, X 및 Y가 앞서 정의한 바와 같은 일반식(IIIc)의 중간체 화합물과 반응시켜서 일반식(Ⅰ) 제품을 얻는것; (e) 일반식(Ⅳ)의 화합물을,Z, N,1R2, Q, X와 Y가 앞서 정의한 바와 같은 일반식(Ⅴ)의 중간체 화합물과 반응시켜서 일반식(Ⅰ) 제품을 얻는것; (f) (1) 일반식(Ⅱd)의 화합물을,일반식(Ⅲ) 의 중간체 화합물과 반응시켜서 일반식(Ⅰc) 화합물을,을 얻고;(2) 산성 매질에서 Ⅰf를 가수분해시켜서 일반식(Ⅰg)의 화합물,을 얻으며;(3) 일반식(Ⅰg)의 화합물을 보란 나트륨과 반응시켜서 생성물(Ⅰe)을 얻는것.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73120185A | 1985-05-06 | 1985-05-06 | |
| US731,201 | 1985-05-06 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR860009008A true KR860009008A (ko) | 1986-12-19 |
| KR940000829B1 KR940000829B1 (ko) | 1994-02-02 |
Family
ID=24938510
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019860003445A Expired - Fee Related KR940000829B1 (ko) | 1985-05-06 | 1986-05-02 | 항정신병성 융합-환의 피리디닐 피페라진 유도체의 제조방법 |
Country Status (25)
| Country | Link |
|---|---|
| JP (1) | JPH0753728B2 (ko) |
| KR (1) | KR940000829B1 (ko) |
| CN (1) | CN1017901B (ko) |
| AT (1) | AT398572B (ko) |
| AU (1) | AU593244B2 (ko) |
| BE (1) | BE904724A (ko) |
| CA (1) | CA1278792C (ko) |
| CH (1) | CH672787A5 (ko) |
| DE (1) | DE3615180C2 (ko) |
| DK (1) | DK165745C (ko) |
| EG (1) | EG18206A (ko) |
| ES (6) | ES8801250A1 (ko) |
| FI (1) | FI85484C (ko) |
| FR (1) | FR2581385B1 (ko) |
| GB (1) | GB2174703B (ko) |
| GR (1) | GR861149B (ko) |
| HU (1) | HU195509B (ko) |
| IE (1) | IE59201B1 (ko) |
| IT (1) | IT1208607B (ko) |
| LU (1) | LU86421A1 (ko) |
| MY (1) | MY100777A (ko) |
| NL (1) | NL8601146A (ko) |
| PT (1) | PT82523B (ko) |
| SE (1) | SE465270B (ko) |
| ZA (1) | ZA862046B (ko) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100450317B1 (ko) * | 1999-08-27 | 2004-09-30 | 르 라보레또레 쎄르비에르 | 피리딘 화합물, 이들을 제조하는 방법 및 이들을 함유하는약제 조성물 |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5801186A (en) | 1987-11-20 | 1998-09-01 | Hoechst Marion Roussel, Inc. | 3- 4-(1-substituted-4-piperazinyl)butyl!-4-thiazolidinone and related compounds |
| US4880930A (en) * | 1987-11-30 | 1989-11-14 | New James S | Psychotropic acyclic amide derivatives |
| US4780466A (en) * | 1988-03-17 | 1988-10-25 | Hoechst-Roussel Pharmaceuticals, Inc. | Arylpiperazinylalkoxy derivatives of cyclic imides |
| IE903410A1 (en) * | 1989-10-09 | 1991-04-10 | Novo Nordisk As | Indole derivatives, their preparation and use |
| US5272148A (en) * | 1992-09-09 | 1993-12-21 | Hoechst-Roussel Pharmaceuticals Incorporated | Heteroarenylpiperazines |
| FR2738824B1 (fr) * | 1995-09-15 | 1997-10-31 | Synthelabo | Derives de 3-(omega(4-(thieno(3,2-c)pyridin-4-yl)piperazin-1 -yl)alkyl)-3,4-dihydroquinazolin-2(1h)-one,leur preparation et leur application en therapeutique |
| FR2738823B1 (fr) * | 1995-09-15 | 1997-10-31 | Synthelabo | Derives de 3-(omega-(4-(thieno(3,2-c)pyridin-4-yl)piperazin- 1-yl)alkyl)-3,4-dihydroquinolein-2(1h)-one,leur preparation et leur application en therapeutique |
| PL184808B1 (pl) * | 1995-09-15 | 2002-12-31 | Sanofi Synthelabo | Pochodne 2(1H)-chinolonu, sposób ich otrzymywania oraz ich zastosowanie terapeutyczne |
| FR2738822B1 (fr) * | 1995-09-15 | 1997-10-31 | Synthelabo | Derives de 4-(omega-(4-(thieno(3,2-c)pyridin-4-yl)piperazin- 1-yl)alkyl)quinolein-2(1h)-one, leur preparation et leur application en therapeutique |
| FR2761071B1 (fr) * | 1997-03-20 | 1999-12-03 | Synthelabo | Derives de quinolein-2(1h)-one et de dihydroquinolein-2(1h)- one, leur preparation et leur application en therapeutique |
| US20040077605A1 (en) | 2001-06-20 | 2004-04-22 | Salvati Mark E. | Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4367335A (en) * | 1981-08-03 | 1983-01-04 | Mead Johnson & Company | Thiazolidinylalkylene piperazine derivatives |
| US4452799A (en) * | 1981-12-23 | 1984-06-05 | Mead Johnson & Company | Benzisothiazole and benzisoxazole piperazine derivatives |
| US4361565A (en) * | 1981-12-28 | 1982-11-30 | Mead Johnson & Company | 2-[4-[(4,4-Dialkyl-2,6-piperidinedion-1-yl)butyl]-1-piperazinyl]pyridines |
-
1986
- 1986-03-11 CA CA000503794A patent/CA1278792C/en not_active Expired - Fee Related
- 1986-03-19 ZA ZA862046A patent/ZA862046B/xx unknown
- 1986-04-29 GR GR861149A patent/GR861149B/el unknown
- 1986-04-29 AU AU56795/86A patent/AU593244B2/en not_active Expired
- 1986-04-29 EG EG250/86A patent/EG18206A/xx active
- 1986-04-30 FI FI861820A patent/FI85484C/fi not_active IP Right Cessation
- 1986-05-02 GB GB08610810A patent/GB2174703B/en not_active Expired
- 1986-05-02 KR KR1019860003445A patent/KR940000829B1/ko not_active Expired - Fee Related
- 1986-05-05 DE DE3615180A patent/DE3615180C2/de not_active Expired - Lifetime
- 1986-05-05 BE BE0/216623A patent/BE904724A/fr not_active IP Right Cessation
- 1986-05-05 NL NL8601146A patent/NL8601146A/nl active Search and Examination
- 1986-05-05 ES ES554659A patent/ES8801250A1/es not_active Expired
- 1986-05-05 FR FR8606471A patent/FR2581385B1/fr not_active Expired - Lifetime
- 1986-05-05 LU LU86421A patent/LU86421A1/fr unknown
- 1986-05-05 IE IE119386A patent/IE59201B1/en not_active IP Right Cessation
- 1986-05-05 SE SE8602061A patent/SE465270B/sv not_active IP Right Cessation
- 1986-05-05 CN CN86103071A patent/CN1017901B/zh not_active Expired
- 1986-05-05 CH CH1830/86A patent/CH672787A5/de not_active IP Right Cessation
- 1986-05-05 DK DK207186A patent/DK165745C/da not_active IP Right Cessation
- 1986-05-06 AT AT0121486A patent/AT398572B/de not_active IP Right Cessation
- 1986-05-06 JP JP61103726A patent/JPH0753728B2/ja not_active Expired - Lifetime
- 1986-05-06 PT PT82523A patent/PT82523B/pt unknown
- 1986-05-06 IT IT8620313A patent/IT1208607B/it active
- 1986-05-06 HU HU861860A patent/HU195509B/hu unknown
-
1987
- 1987-09-25 ES ES557757A patent/ES8802149A1/es not_active Expired
- 1987-10-01 MY MYPI87002712A patent/MY100777A/en unknown
-
1988
- 1988-01-28 ES ES557809A patent/ES8802614A1/es not_active Expired
- 1988-05-26 ES ES557839A patent/ES8900138A1/es not_active Expired
- 1988-11-16 ES ES557855A patent/ES8900253A1/es not_active Expired
-
1989
- 1989-02-27 ES ES557865A patent/ES9000005A1/es not_active Expired
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100450317B1 (ko) * | 1999-08-27 | 2004-09-30 | 르 라보레또레 쎄르비에르 | 피리딘 화합물, 이들을 제조하는 방법 및 이들을 함유하는약제 조성물 |
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