KR880002869A - 치환된 헥사하이드로 아릴퀴놀리진 - Google Patents
치환된 헥사하이드로 아릴퀴놀리진 Download PDFInfo
- Publication number
- KR880002869A KR880002869A KR870009444A KR870009444A KR880002869A KR 880002869 A KR880002869 A KR 880002869A KR 870009444 A KR870009444 A KR 870009444A KR 870009444 A KR870009444 A KR 870009444A KR 880002869 A KR880002869 A KR 880002869A
- Authority
- KR
- South Korea
- Prior art keywords
- benzo
- spiro
- compound
- lower alkyl
- hydrogen
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/12—Antihypertensives
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/20—Spiro-condensed systems
-
- 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
- C07D471/22—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 systems contains four or more hetero rings
-
- 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
- C07D491/22—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 four or more hetero rings
-
- 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
- C07D495/22—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 four or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Nutrition Science (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Saccharide Compounds (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (10)
- 다음 일반식(Ⅰ)의 헥사하이드로아릴퀴놀리진 화합물 또는 약제학적으로 허용되는 염.상기 식에서, Ar은 R1,R2-벤조 [b]푸로, R1,R2-벤조[b]티에노, R1,R2- 티에노, R1,R2- 푸로, R1,R2- 벤조, R1,R2- 인돌로, R1,R2- 피리디노, 티아졸로, 이미다조, 피라졸로, R1,R2- 나프토 및 R1,R2-피롤로로 이루어진 그룹 중에서 선택된 방향족한 시스템을 나타내고, 여기에서 R1및 R2는 각각 독립적으로 수소, 할로, 하이드록시, C1-C3알콕시, 저급알킬 또는 카복시를 나타내거나, R1, 및 R2가 함께는 메틸렌디옥시 또는 C3-C4알킬렌을 나타내고, Ar의 유리결합은 Ar의 양쪽 배위 모두에서 퀴놀리진 환에 결합될 수 있으며, R3는 질소 원자들중 한 질소원자의 유리 결합에 결합되고, 수소, 저급알킬, 벤질 또는 R을 나타내며, R4는 나머지 질소원자의 유리 결합에 결합되고, 알킬렌-OXR, 알킬렌 -NR'XP또는를 나타내며, R은 저급알킬, C1-C3알콕시, 페닐, 할로페닐, 저급알킬페닐, 저급알콕시페닐, 벤질, 트리폴루오로메틸, 아미노 또는 디(저급알킬)아미노를 나타내고, R'는 H 또는 저급알킬을 나타내며, X는 - CO-, -SO2-, P(O)(OR')2, -CSNH-, -CONH-, 또는 -(CNCN)-을 나타내고, n은 1 또는 2이다.
- 제 1 항에 있어서, Ar이 R1, R2-벤조 [b]푸로, R1,R2-벤조R1, R2-벤조[b]티에노 또는 R1, R2-나프토이고, R4는 -CH2CH2OXR 또는 -CH2CH2NHXR인 화합물,
- 제 2 항에 있어서, (2R, 12bs)-3'-(2-메탄설폰아미도에틸)-스피로[1,3,4,6,7, 12b - 헥사 하이드로벤조[b]푸로 [2,3-a]퀴놀리진]-2,4'-이미다졸리딘-2'-온, (2s, 12bR)-3'-(2-메탄설폰 아미도에틸)-스피로(1,3,4,6,7,12b-헥사하이드로벤조 [b]-푸로 [2,3-a]퀴놀리진)-2, 44'(이미다졸리딘-2'-온) 또는 이의 혼합물.
- 제 2 항에 있어서, (2R, 12bS)-9-메톡시-3'-(2-메탄설폰아미도에틸)-스피로 (1,3,4,6,7,11b-헥사하이드로벤조 [a] 퀴놀리진)-2,4'-(이미다졸리딘-2'-온)(2s,12bR)-9-메톡시-3'-(2-메탄설폰아미도에틸)스피로 (1,3,4,6,7,11b-헥사하이드로 벤조 [a] 퀴놀리진)-2,4'-(이미다졸리딘-2'-온), 또는 이외 혼합물.
- 약제학적으로 허용되는 담체 및 α2- 아드레날린 수용체 길항유효량의 일반식 (Ⅰ)의 헥사하이드로아리뤼놀리진 화합물 또는 그의 약제학적으로허용되는 염을 함유하며, 말초 α2-아드레날린 수용체 길항 활성을 갖는 약학적 조성물.상기 식에서 Ar은 R1, R2- 벤조 [b] 푸로, R1, R2-벤조 [b] 티에노, R1,R2-티에노, R1, R2- 푸로, R1, R2-벤조, R1, R2-인돌로, R1, R2-피리디노, 티아졸로, 이미다조, 피라졸로, R1, R2- 나프토, 및 R1, R2-피롤로로 이루어진 그룹 중에서 선택된 방향족 환 시스템을 나타내고, 여기에서 R1및 R2는 각각 독립적으로 수소, 할로, 하이드록시, C1- C3알콕시, 저급알킬, 또는 카복시를 나타내거나, R1및 R2가 함께는 메틸렌디옥시 또는 C1- C3알킬렌을 나타내고, Ar의 유리 결합은 Ar의 유리 겹합은 Ar의 양쪽 배워 모두에서 퀴놀리진 환에 결합될 수 있으며, R3는 질소원자들 중에 어느 한 질소의 유리 결합에 결합되고, 수소, 저급알킬, 벤질 또는 R을 나타내며, R3는 나머지 질소의 유리 결합에 결합되고, 알킬렌-OXR, 알킬렌-NR'XR 또는-알킬렌를 나타내며, R은 저급알킬, C1- C3알콕시, 페닐, 할로페닐, 저급알킬페닐, 저급알콕시페닐, 벤질, 트리플루오로메틸, 아미노 또는 디(저급알킬)아미노를 나타내고, R'는 H 또는 저급알킬을 나타내며, X는 -CO-, -SO2-, -P(O)(OR), - CSNH-, -CONH, 또는 -C(NCN)을 나타내고, N은 1 또는 2이다.
- 제 1 항에 따른 헥사하이드로아릴퀴놀리진 화합물 또는 이의 약제학적으로 허용되는 산부가염을 함유하는 조성물의 치료적 유효량을 투여함을 특징으로 하여, 원치 않는 중추신경계 부작용은 피하면서 원치 않는 α-아드레날린 수용체 작용에 의한 질환을 치료하는 방법.
- 제 6 항에 있어서, 헥사하이드로아릴퀴놀리진 화합물이 Ar은 R1, R2-벤조 [b] 푸로이고, 이때, R1및 R2는 수소이며, R3가 수소이고, R4가메탄설폰아미도 에틸이며, n이 1인 화합물, 즉(2R,12bS)-3'-(2-메탄설폰아미도에틸)-스피로-(1,3,4,5,6,12b-헥사하이드로벤조 [b]푸로 [2,3-a]-퀴놀리진)-2,4'-(이미다졸리딘-2'-온)으로 명명되는 화합물, 또는 Ar이 R1, R2벤조이고, 이 때R1은9-메톡시이며, R2는 수소이고, R3는 수소이며, R4는 메탄설폰아미도에틸이고, n이 1인 화합물, 즉(2R, 12bS)-9-메톡시-3'-(2-메탄설폰아미도에틸)-스피로-(1,3,4,6,7,11b - 헥사하이드로벤조 [a]퀴놀리진)-2, 4'-(이미다졸린딘-2'-온)으로 명명되는 화합물인 방법,
- 제 1 항에 있어서, 퀴놀리진 환의 2번 탄소에 결합된 스피로-4'-이미다졸리디논-2-온 또는 스피로-4'(5,6-디하이드로-1H- 피리미딘-2[3H]-온)의 헤테로 원자와 퀴놀리진 환의 12b에 존재하는 수소가 트랜스 위치로 배열되도록 하는 입체 배위를 가지며, 라세미체, 에난티오머 도는 에난티오머의 혼합물인 화합물.
- 제 1 항에 있어서, Ar이 R1, R2-벤조푸로, R1,R2-벤조 R1, R2-벤조[b]티에노, 또는 R1, R2-나프토이고, R3은 수소이며, R4은 -CH2CH2NHXR이고 n은 2인 화합물.
- 제 2 항에 있어서, (2R, 11bS)-9-메톡시-1,3,4,5',6,6',7,11b-옥타하이드로-3'-(2-메탄설폰아미도에틸)-스피로(벤조 [a]퀴놀리진)-2,4'-(1'H - 피리미딘-2'-(3'H)-온) 또는 (2s, 11bR)-9-메톡시-1,3,4,5',6,6',7,11b-옥타하이드로-3'-(2-메탄설폰아미도에틸)스피로(벤조 [a]퀴놀리진)-2,4'-(1'H- 피리미딘-2'-(3'H)-온), 또는 이의 혼합물.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US90148586A | 1986-08-28 | 1986-08-28 | |
US901485 | 1992-06-25 |
Publications (1)
Publication Number | Publication Date |
---|---|
KR880002869A true KR880002869A (ko) | 1988-05-12 |
Family
ID=25414273
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR870009444A KR880002869A (ko) | 1986-08-28 | 1987-08-28 | 치환된 헥사하이드로 아릴퀴놀리진 |
Country Status (14)
Country | Link |
---|---|
EP (1) | EP0259092B1 (ko) |
JP (1) | JP2582799B2 (ko) |
KR (1) | KR880002869A (ko) |
AT (1) | ATE78482T1 (ko) |
AU (1) | AU597412B2 (ko) |
CA (1) | CA1288435C (ko) |
DE (1) | DE3780542T2 (ko) |
DK (1) | DK447387A (ko) |
ES (1) | ES2044944T3 (ko) |
GR (1) | GR3005537T3 (ko) |
IL (1) | IL83586A (ko) |
NZ (1) | NZ221485A (ko) |
PT (1) | PT85593B (ko) |
ZA (1) | ZA876400B (ko) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4942235A (en) * | 1989-03-16 | 1990-07-17 | Merck & Co., Inc. | Process for certain (2R-trans)hexahydroaroquinolizines |
US5229387A (en) * | 1991-09-20 | 1993-07-20 | Syntex (U.S.A.) Inc. | Decahydro-8H-isoquino[2,1-g][1,6]naphthyridine and decahydrobenzo[a]pyrrolo [2,3-e]quinolizine derivatives |
FR2744451B1 (fr) * | 1996-02-01 | 1998-04-24 | Pf Medicament | Nouvelles imidazolidinones, pyrimidinones, et 1,3-diazepin-2 -ones, leur preparation et leurs applications en therapeutique |
US6141745A (en) * | 1998-04-30 | 2000-10-31 | Advanced Micro Devices, Inc. | Functional bit identifying a prefix byte via a particular state regardless of type of instruction |
FI126838B (en) | 2014-12-16 | 2017-06-15 | Vetcare Oy | Process for the preparation of spirocyclic substituted benzofuroquinolizines |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1435573A (en) * | 1973-05-25 | 1976-05-12 | Wyeth John & Brother Ltd | Indoloquinolizines |
GB2106909B (en) * | 1981-10-07 | 1984-09-19 | Wyeth John & Brother Ltd | Benzoquinolizines |
IE57014B1 (en) * | 1983-03-25 | 1992-03-11 | Wyeth John & Brother Ltd | Benzoquinolizines |
IL74147A (en) * | 1984-02-02 | 1988-08-31 | Merck & Co Inc | 2-acylamino-hexahydro-arylquinolizines and salts thereof and pharmaceutical compositions containing them |
NZ216283A (en) * | 1985-06-03 | 1989-10-27 | Merck & Co Inc | Hexahydro arylquinolizine derivatives and pharmaceutical compositions |
-
1987
- 1987-08-18 NZ NZ221485A patent/NZ221485A/en unknown
- 1987-08-19 AU AU77205/87A patent/AU597412B2/en not_active Ceased
- 1987-08-19 IL IL83586A patent/IL83586A/xx not_active IP Right Cessation
- 1987-08-26 PT PT85593A patent/PT85593B/pt not_active IP Right Cessation
- 1987-08-26 DE DE8787307541T patent/DE3780542T2/de not_active Expired - Fee Related
- 1987-08-26 AT AT87307541T patent/ATE78482T1/de active
- 1987-08-26 CA CA000545453A patent/CA1288435C/en not_active Expired - Fee Related
- 1987-08-26 ES ES87307541T patent/ES2044944T3/es not_active Expired - Lifetime
- 1987-08-26 EP EP87307541A patent/EP0259092B1/en not_active Expired - Lifetime
- 1987-08-27 ZA ZA876400A patent/ZA876400B/xx unknown
- 1987-08-27 DK DK447387A patent/DK447387A/da not_active Application Discontinuation
- 1987-08-28 KR KR870009444A patent/KR880002869A/ko not_active Application Discontinuation
- 1987-08-28 JP JP62214979A patent/JP2582799B2/ja not_active Expired - Lifetime
-
1992
- 1992-08-27 GR GR920401865T patent/GR3005537T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
DE3780542T2 (de) | 1993-01-07 |
AU7720587A (en) | 1988-03-03 |
CA1288435C (en) | 1991-09-03 |
ATE78482T1 (de) | 1992-08-15 |
JP2582799B2 (ja) | 1997-02-19 |
PT85593A (en) | 1987-09-01 |
DK447387D0 (da) | 1987-08-27 |
IL83586A0 (en) | 1988-01-31 |
GR3005537T3 (ko) | 1993-06-07 |
DE3780542D1 (en) | 1992-08-27 |
NZ221485A (en) | 1991-04-26 |
DK447387A (da) | 1988-02-29 |
ES2044944T3 (es) | 1994-01-16 |
JPS63139183A (ja) | 1988-06-10 |
EP0259092A1 (en) | 1988-03-09 |
EP0259092B1 (en) | 1992-07-22 |
AU597412B2 (en) | 1990-05-31 |
ZA876400B (en) | 1988-02-25 |
PT85593B (pt) | 1990-05-31 |
IL83586A (en) | 1991-12-15 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
PE20030848A1 (es) | Compuestos de espiropiperidina n-sustituidos como ligandos para el receptor orl-1 | |
KR860000299A (ko) | 치환된 바이시클릭 화합물의 제조방법 | |
PE20030415A1 (es) | Derivados policiclicos de guanina como inhibidores de fosfodiesterasa v | |
RU98101135A (ru) | Новые аналоги камптотецина, способы получения, их применение в качестве лекарственных средств и содержащие их фармацевтические композиции | |
AR055321A1 (es) | Compuestos de imidazopiridina uso para a fabricacion de un medicamento para el tratamiento o profilaxis de enfermedades o trastornos en los que se requiere un antagonista de una bomba de acido y composicion farmaceutica que lo comprende | |
AR037680A1 (es) | Antagonistas del receptor de adenosina a2a de 5-amino-pirazolo-[4,3-e]-1,2,4-triazolo[1,5-c]-pirimidinas sustituidas, composiciones farmaceuticas que los comprenden, el uso de dichos compuestos, solos o en combinacion para la elaboracion de un medicamento utiles para el tratamiento de enfermedades d | |
FI893634A0 (fi) | Menetelmä valmistaa terapeuttisesti aktiivisia mono- tai disubstituoituja (imidatsol-4-yyli)metyylipyrido/4,3-b/indol- ja atsepino/4,3-b/indol-1-oneja | |
RU2018140732A (ru) | Новые замещенные соединения имидазопиридина в качестве ингибиторов индоламин-2,3-диоксигеназы и/или триптофан-2,3-диоксигеназы | |
WO2013042035A4 (en) | Heterocyclic compounds as inhibitors of fatty acid biosynthesis for bacterial infections | |
KR880002869A (ko) | 치환된 헥사하이드로 아릴퀴놀리진 | |
EP0655451A1 (en) | Tetracyclic condensed heterocyclic compounds for the treatment of senile dementia | |
ES2892624T3 (es) | Compuestos tricíclicos y composiciones como inhibidores de cinasas | |
PE20000548A1 (es) | Derivados de diaza-espiro[3.5]nonano | |
IE831696L (en) | TRICYCLIC AND TETRACYCLIC IMIDAZO £1,5-b| £1,4|¹BENZODIAZEPINE-1 CARBOXYLATE DERIVATES | |
DE69129165T2 (de) | Prozess zur Darstellung von Lactamderivaten | |
JP2005533018A5 (ko) | ||
KR900003168A (ko) | 이미다조[4,5-b]피리딘 유도체 | |
KR930021202A (ko) | 다찌키닌 수용체 길항제, 이소퀴놀론 및 이의 제조방법 | |
OA07450A (fr) | Nouveaux dérivés du thioformamide, leur préparation et les médicaments qui les contiennent. | |
ATE48999T1 (de) | Piperazin-1-yl-ergolinderivate, verfahren zu ihrer herstellung und sie enthaltende pharmazeutische zusammensetzungen. | |
PT98893A (pt) | Processo de preparacao de compostos de fenantridina e de composicoes farmaceuticas que os contem | |
NZ212669A (en) | Pyrazolo(3,4-d)pyridin-3-one derivatives,and pharmaceutical compositions containing such | |
EP0254527A3 (en) | New tetracyclic indole derivatives | |
JPH07309835A (ja) | 四環式縮合複素環誘導体、その製造法および用途 | |
KR910020018A (ko) | 피리도[3, 4-b] 피롤로[1, 2-e][1, 4, 5]옥사디아제핀 및 이의 관련 동족체 이의 제조방법 및 약제로서의 이의 용도 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
WITN | Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid |