KR970704435A - 헤테로시클릭 화합물의 도파민-D 리간드로서의 용도(Use of Heterocyclic Compounds as Dopamines-D Ligands) - Google Patents

헤테로시클릭 화합물의 도파민-D 리간드로서의 용도(Use of Heterocyclic Compounds as Dopamines-D Ligands) Download PDF

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KR970704435A
KR970704435A KR1019970700265A KR19970700265A KR970704435A KR 970704435 A KR970704435 A KR 970704435A KR 1019970700265 A KR1019970700265 A KR 1019970700265A KR 19970700265 A KR19970700265 A KR 19970700265A KR 970704435 A KR970704435 A KR 970704435A
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alkyl
formula
halogen
het
group
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KR1019970700265A
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비테 헬렌달
안네그레트 란스키
베아트리체 렌덴바흐-뮐러
알프레트 바흐
릴리안 웅거
한스-위르겐 테쉔도르프
카르스텐 빅케
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스타르크, 카르크
바스프 악티엔게젤샤프트
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Publication of KR970704435A publication Critical patent/KR970704435A/ko

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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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine

Abstract

본 발명은 Het, A, B및 Ar이 명세서에서 언급된 의미를 갖는 화학식 Het-A-B-Ar의 헤테로시클릭 화합물의 용도에 관한 것이다. 본 발명에 따른 화합물은 도파민 D3수용체에 대한 높은 친화도를 갖기 때문에 도파민D3리간드에 반응하는 질환의 치료에 사용될 수 있다.

Description

헤테로시클릭 화합물의 도파민-D3리간드로서의 용도(Use of Heterocyclic Compounds as Dopamines-D3Ligands)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 도파민 D3수용체 길항제 또는 작용제에 반응하는 질환의 치료를 위한 제약조성물을 제조하기 위한 하기 화학식(I)의 화합물 및 그의 생리학상 허용되는 산부가염의 용도.
    Het-A-B-Ar
    상기 식에서,A는 O,S,NR4,CONR4,NR4CO,COO,OCO 및 이중결합 또는 삼중결합 중에서 선택되는 하나 이상의 기를 포함할 수 있는 직쇄 또는 분지쇄 C1-C18-알킬렌기이고,B는 화학식또는의 기이고,Ar은 서로 독립적으로 OR4,C1-C8-알킬,C2-C8-알케닐,C2-C8-알키닐,할로겐,CN,CO2R4,NO2,SO2R4,SO3R4,NR4R5,SO2NR4R5,SR4,CF3,CHF2,5원 또는 6원 카르보시클릭,방향족 또는 비방향족 고리, 및O,S 및 N 중에서 선택되는 1내지 3개의 헤테로 원자를 갖는 5원 또는 6원 헤테로시클릭, 방향족 또는 비방향족 고리(여기서,카르보시클릭 또는 헤테로시클릭 고리는 비치환되거나 또는 C1-C8-알킬,할로겐,OC1-C8-알킬,OH,NO2또는 CF3에 의해 치환됨)중에서 선택되는 1내지 4개의 치환체를 가질 수 있는 페닐,피리딜,피리미딜 또는 트리아지닐이고, 또한 Ar은 상기 정의된 종류의 카르보시클릭 또는 헤테로시클릭 고리에 융합될 수 있고,Het는 하기 화학식의 기 중에서 선택되는 기이고,
    R1,R2및 R3은 서로 독립적으로 H,할로겐,OR5, NR4R5,SR4,CF3,CN,CO2R4또는 비치환되거나 OH,OC1-C8-알킬 또는 할로겐으로 치환된 C1-C8-알킬이고,R4는 H또는 비치환되거나 OH, OC1-C8-알킬 또는 할로겐으로 치환된 C1-C8-알킬이고, R5는 R4에 대해 정의된 의미를 갖거나 또는 COR4또는 CO2R4이고,R8은 R5에 대해 정의된 의미를 갖는다.
  2. 제1항에 있어서, Het가 하기 화학식의 기 중에서 선택되는 기인 화학식(I)의 화합물의 용도.
  3. 제2항에 있어서,Het가 하기 화학식의 기 중에서 선택되는 기인 화학식(I)의 화합물의 용도.
  4. 제 2항에 있어서, Het가 하기 화학식의 기 중에서 선택되는 기인 화학식(I)의 화합물의 용도.
  5. 제1항 내지 제4항 중 어느 한 항에 있어서, A가 O,S또는 CONR4를 포함할 수 있는C1-C8-알킬렌기이고,Ar이서로독립적으로 H,C1-C8-알킬, OC1-C8-알킬,CHF2,CF3,CN,할로겐, SO2OR4및 COR4(여기서,R4는 제1항에서 정의된 의미를 가짐)중에서 선택되는 1또는 2개의 치환체를 가질 수 있는 페닐 또는 피리딜인 화학식(I)의 화합물의 용도.
  6. 제5항에 있어서,A가 S,O 또는 CONR4를 포함할수 있는 C3-C6-알킬렌기이고, Ar이 서로 독립적으로 H,CF3,할로겐,C1-C8-알킬,OC1-C8-알킬 및 CN 중에서 선택되는 1또는 2개의 치환체를 가질 수 있고, B가인 화학식(I)의 화합물의 용도
  7. 제6항에 있어서,R1,R2및 R3이 각각 서로 독립적으로 H,NR4R5,OR5,C1-C8-알킬,CO2R4,CF3또는 할로겐이고,R4가 H또는 C1-C8-알킬이고,R5가 H,C1-C8-알킬인 또는 CO-C1-C8-알킬이고, R8이 H또는 C1-C8-알킬 화학식(I)의 화합물의 용도.
  8. 제1항 내지 제7항 중 어느 한 항에 있어서, A가 S,O 또는 CONH를 포함할 수 있는 C3-C6-알킬렌기이고,B가이고, 라디칼 Ar의 치환체 또는 치환체들은 서로 독립적으로 H,CHF2,C1-C4-알킬또는 CF3중에서 선택되는 것인 화학식(I)의 화합물의 용도.
  9. 제1항 내지 제 8항 중 어느 한 항에 있어서, Het및 A가 상기 청구항 중의 어느 한 항에서 정의된 의미를 갖고, X및 Y 가 라디칼 Ar의 치환체에 대해 정의된 바와 같은 하기 화학식(Ia) 의 화합물의 용도.
  10. 제 9항에 있어서, Het,A,X 및 Y 가 제 9항에서 정의된 의미를 갖는 하기 화학식(Ib)의 화합물의 용도.
  11. 제 9항또는 제 10항에 있어서, Y 가 H 또는 C1-C4-알킬이고 X가 CF3,CHF2,CN,C1-C4-알킬인 용도.
  12. 제1항 내지 제11항중 어느 한 항에 정의된 화합물의 치료 유효량을 도파민 D3수용체 길항제 또는 작용제에 반응하는 질환의 치료를 필요로 하는 사람에게 투여하는 것으로 이루어지는 상기 질환의 치료 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019970700265A 1994-07-15 1995-07-14 헤테로시클릭 화합물의 도파민-D 리간드로서의 용도(Use of Heterocyclic Compounds as Dopamines-D Ligands) KR970704435A (ko)

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DEP4425146.7 1994-07-15
DE4425146A DE4425146A1 (de) 1994-07-15 1994-07-15 Verwendung heterocyclischer Verbindungen
PCT/EP1995/002782 WO1996002246A1 (de) 1994-07-15 1995-07-14 Verwendung heterocyclischer verbindungen als dopamin-d3 liganden

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FI970148A0 (fi) 1997-01-14
NO311683B1 (no) 2002-01-07
DE59510635D1 (de) 2003-05-15
CN1152870A (zh) 1997-06-25
PT771197E (pt) 2003-08-29
US6090807A (en) 2000-07-18
AU3111495A (en) 1996-02-16
SI9520084A (en) 1997-08-31
FI970148A (fi) 1997-01-14
DE4425146A1 (de) 1996-01-18
AU704839B2 (en) 1999-05-06
KR20040000412A (ko) 2004-01-03
ATE236629T1 (de) 2003-04-15
HUT77608A (hu) 1998-06-29
CN1534023A (zh) 2004-10-06
BG101112A (en) 1998-04-30
KR100443850B1 (ko) 2004-08-11
EP0771197B1 (de) 2003-04-09
SI9520084B (sl) 2005-02-28
MX9700430A (es) 1998-05-31
HU9700111D0 (en) 1997-02-28
BR9508296A (pt) 1998-05-19
NO970163D0 (no) 1997-01-14
NO970163L (no) 1997-03-14
ES2196072T3 (es) 2003-12-16
BG63487B1 (bg) 2002-03-29
EP0771197A1 (de) 1997-05-07
CZ9697A3 (en) 1997-08-13
CA2195242A1 (en) 1996-02-01
CZ293126B6 (cs) 2004-02-18
JPH10502658A (ja) 1998-03-10
DK0771197T3 (da) 2003-06-23
NZ290388A (en) 2001-04-27
WO1996002246A1 (de) 1996-02-01

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