KR920701122A - 신규 이환식 아미노-치환 화합물 - Google Patents

신규 이환식 아미노-치환 화합물

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KR920701122A
KR920701122A KR1019910700844A KR910700844A KR920701122A KR 920701122 A KR920701122 A KR 920701122A KR 1019910700844 A KR1019910700844 A KR 1019910700844A KR 910700844 A KR910700844 A KR 910700844A KR 920701122 A KR920701122 A KR 920701122A
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compound
alkyl
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율리 핵셀
스벤-에릭 힐버
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클래스 빌헬름슨
악티에볼라게트 아스트라
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Publication of KR920701122A publication Critical patent/KR920701122A/ko

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    • C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C215/64—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/54—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C217/74—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/51—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by pyrolysis, rearrangement or decomposition
    • C07C45/511—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by pyrolysis, rearrangement or decomposition involving transformation of singly bound oxygen functional groups to >C = O groups
    • C07C45/515—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by pyrolysis, rearrangement or decomposition involving transformation of singly bound oxygen functional groups to >C = O groups the singly bound functional group being an acetalised, ketalised hemi-acetalised, or hemi-ketalised hydroxyl group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/51—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by pyrolysis, rearrangement or decomposition
    • C07C45/54—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by pyrolysis, rearrangement or decomposition of compounds containing doubly bound oxygen atoms, e.g. esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C07C45/70—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form
    • C07C45/71—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline

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  • Nitrogen Condensed Heterocyclic Rings (AREA)
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Abstract

내용 없음

Description

신규 이환식 아미노-치환 화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (32)

  1. 하기 일반식의 화합물.
    상기식에서, X는 O, CH2, S, SO 또는 SO2이고, R은 F또는 C1 이고, R1은 H, C1-C6알킬 또는 C2-C6알케닐이고, R2는 H, C1-C6알킬 또는 C2-C6알케닐이고, R3은 H C1-C6알킬이고, 여기서, C1-C6알킬은 탄소 원자수 1내지 6의 직쇄, 분지쇄 및 환식 알킬기이고, C2-C6알케닐은 1개 또는 2개의 이중 결합을 포함하는 직쇄 또는 분지 탄소쇄이고, R1및 R2는 합께 결합하여 N, O및 S로 부터 선택된 1종 또는 2종의 헤테로 원자를 포함하는 5원-또는 6원환을 형성할 수 있다.
  2. 제1항에 있어서, R이 불소임을 특징으로 하는 화합물.
  3. 제1항 또는 제2항에 있어서, R1,R2및 R3은 독립적으로 메틸 에틸, n-프로필 및 n-부틸로부터 선택되는 알킬임을 특징으로 하는 화합물.
  4. 제1항 또는 제2항에 있어서, R1및 R2가 탄소 원자수가 2내지 4이고 1개의 이중 결합을 갖는 알케닐임을 특징으로 하는 화합물.
  5. 제4항에 있어서, R3이 메틸, 에틸, n-프로필 및 n-부틸로부터 선택됨을 특징으로 하는 화합물.
  6. 제2항에 있어서, R1및 R2는 n-프로필이고 R3은 H임을 특징으로 하는 화합물.
  7. 제1항 내지 제6항 중 어느 한 항에 있어서, 아미노기에 인접 한 비대칭 탄소 원자가(S)-배열임을 특징으로 하는 화합물.
  8. 제1항 내지 제7항 중 어느 한 항에 따른 화합물의 제약상 허용되는 염.
  9. 제1항 내지 제7항 중 어느 한 항에 따른 화합물의 거울상 이성질체.
  10. 제9항에 따른 거울상 이성질체의 제약상 허용되는 염.
  11. 치료용 제1항 내지 제7항 중 어느 한 항에 따른 화합물.
  12. 치료용 제9항에 따른 거울상 이성질체의 제약상 허용되는 염.
  13. 치료용 제9항에 따른 거울상 이성질체.
  14. 하기 일반식의 화합물, 그의 거울상 이성질체 또는 그의 제약상 허용되는 염 또는 이러한 거울상 이성질체의 제약상 허용되는 염을 활성 성분으로서 함유하는 제약 제제.
    상기 식에서, X는 O, CH2, S, SO 또는 SO2이고, R은 F 또는 C1이고, R1은 H, C1-C6알킬 또는 C2-C6알케닐이고, R2은 H, C1-C6알킬 또는 C2-C6알케닐이고, R3은 H, C1-C6알킬이고, 여기서, C1-C6알킬은 탄소 원자수 1내지 6의 직쇄, 분지쇄 및 환식 알킬기 이고, C2-C6알케닐은 1개 또는 2개의 이중 결합을 포함하는 직쇄 또는 분지 탄소쇄이고, R1및 R2는 함께 결합하여 N,O 및 S로 부터 선택된 1종 또는 2종의 헤테로 원자를 포함하는 5원-또는 6원환을 형성할 수 있다.
  15. 제14항에 있어서, R,R1,R2및 R3이 제2항 내지 제6항 중 어느 한 항에서 정의한 바와 같은 제약 제제.
  16. 제14항에 있어서, 화합물이 거울상 이성질체임을 특징으로 하는 제약제제.
  17. 제16항에 있어서, 거울상 이성질체가(S)-배열임을 특징으로 하는 제약 제제.
  18. 우울증, 불안증, 식욕불량증, 노인성 치매, 알쯔하이머병, 편두통, 체온 조절 장애 및 성기능 장애 치료용 제2항 내지 제7항 중 어느 한 항에 따른 화합물.
  19. 통증 치료용 제2항 내지 제7항 중 어느 한 항에 따른 화합물.
  20. 심장 혈관계 장애의 치료용 제2항 내지 제7항 중 어느 한 항에 따른 화합물.
  21. 제2항 내지 제7항 중 어느 한 항에 따른 화합물의 중추 신경계 질환, 특히 5-히드록시트립타민 관련질환 치료를 위한 의약 제조용 용도.
  22. 제21항에 있어서, 우울증, 불안증, 식욕불량증, 노인성 치매, 편두통, 알쯔하이머병, 체온 조절 장애 또는 성기능 장애 치료를 위한 의약 제조용 용도.
  23. 제21항에 있어서, 통증 치료를 위한 의약 제조용 용도.
  24. 제21항에 있어서, 심장혈관계 기능 장애 치료를 위한 의약 제조용 용도.
  25. 포유 동물 및 인간에게 제2항 내지 제7항 중 어느 한 항에 따른 화합물, 그의 거울상 이성질체 또는 그의 생리학상 허용되는 염 또는 그의 거울상 이성질체의 생리학상 허용되는 염을 투여하는 것으로 이루어진 중추 신경계 질환, 특히, 5-히드록시트립타민 관련 질환의 치료 방법.
  26. 제25항에 있어서, 우울증, 불안증, 식욕불량증, 노인성 치매, 편두통, 알쯔하이머병, 체온 조절 장애 또는 성기능 장애의 치료방법.
  27. 제25항에 있어서, 통증의 치료 방법.
  28. 제25항에 있어서, 심장혈관계 기능 장애의 치료 방법.
  29. R, R1, R2, 및 X가 제1항의 일반식(Ⅰ)에서 정의한 바와 같고 R3이 C1-C6알킬인 일반식(Ⅰ)의 화합물을 브롬화수소 수용액과 반응시킴으로써 R3이 H인 제1항에 따른 일반식(Ⅰ)의 화합물의 제조 방법.
  30. 제29항에 있어서, 일반식(Ⅱ)에 따른 화합물을 2급 아민 또는 1급 아민의 N-알킬화에 의해 얻음을 특징으로 하는 방법.
  31. 제30항에 있어서, 2급 아민 또는 1급 아민은 벤질기를 포함하는 3급 아민으로부터 수소 첨가 반응시켜 얻음을 특징으로 하는 방법.
  32. 상기 항 중 어느 한 항에서 청구되며 실질적으로 설명된 화합물, 그의 제조 방법, 그의 제약상 제제 및 치료 용도 및 치료 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910700844A 1989-12-07 1990-12-05 신규 이환식 아미노-치환 화합물 KR920701122A (ko)

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SE8904127A SE8904127D0 (sv) 1989-12-07 1989-12-07 New biocyclic amino-substituted compounds
SE8904127-1 1989-12-07
PCT/SE1990/000806 WO1991009006A1 (en) 1989-12-07 1990-12-05 New bicyclic amino-substituted compounds

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US (1) US5376687A (ko)
EP (1) EP0457883B1 (ko)
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AT (1) ATE137490T1 (ko)
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PH22522A (en) * 1985-09-03 1988-10-17 Ciba Geigy Ag 3-amino-dihydro-1-benzopyrans and benzothiopyrans, their pharmaceutical compositions and method of using said compounds
CA1331191C (en) * 1988-03-25 1994-08-02 Bengt Ronny Andersson Therapeutically useful tetralin derivatives
CA1335591C (en) * 1988-05-23 1995-05-16 James Arthur Nixon Ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes
CA2026775C (en) * 1989-01-09 1998-04-07 Per Arvid Emil Carlsson Halo substituted aminotetralins
US5225596A (en) * 1989-01-09 1993-07-06 The Upjohn Company Halo substituted aminotetralins
AU654653B2 (en) * 1989-05-31 1994-11-17 Pharmacia & Upjohn Company Therapeutically useful 2-aminotetralin derivatives

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GR3020122T3 (en) 1996-08-31
JPH04503819A (ja) 1992-07-09
FI913713A0 (fi) 1991-08-05
LV10607B (en) 1995-12-20
SE8904127D0 (sv) 1989-12-07
LV10607A (lv) 1995-04-20
DE69026816D1 (de) 1996-06-05
AU6958791A (en) 1991-07-18
AU639742B2 (en) 1993-08-05
WO1991009006A1 (en) 1991-06-27
DE69026816T2 (de) 1996-10-02
ES2086528T3 (es) 1996-07-01
LTIP1733A (en) 1995-08-25
ATE137490T1 (de) 1996-05-15
US5376687A (en) 1994-12-27
EP0457883B1 (en) 1996-05-01
NO913023D0 (no) 1991-08-02
CA2046292A1 (en) 1991-06-08
NO913023L (no) 1991-08-02
NO176018C (no) 1995-01-18
NO176018B (no) 1994-10-10
LT4035B (en) 1996-09-25
RU2086537C1 (ru) 1997-08-10
EP0457883A1 (en) 1991-11-27
DK0457883T3 (da) 1996-08-26

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