KR950704284A - 칼슘 채널 길항제로서의 피페리딘 유도체(Piperidine Derivatives as Calcium Channel Antagonists) - Google Patents
칼슘 채널 길항제로서의 피페리딘 유도체(Piperidine Derivatives as Calcium Channel Antagonists)Info
- Publication number
- KR950704284A KR950704284A KR1019950702552A KR19950702552A KR950704284A KR 950704284 A KR950704284 A KR 950704284A KR 1019950702552 A KR1019950702552 A KR 1019950702552A KR 19950702552 A KR19950702552 A KR 19950702552A KR 950704284 A KR950704284 A KR 950704284A
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- South Korea
- Prior art keywords
- compound
- formula
- piperidine
- hydroxy
- pharmaceutically acceptable
- Prior art date
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- 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
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- 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
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
- C07D295/104—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/108—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
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- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Rheumatology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
본 발명은 칼슘 길항제, 예컨대 뇌 세포에서 칼슘의 축적과 관련된 상태의 치료에 유용한 하기 일반식(I)의 화합무 또는 그의 염에 관한 것이다.
상기 식중에서 R1은 C1―6알킬, 할로겐 또는 페닐을 나타내고, R2는 수소 원자, C1―6알킬, 할로겐 또는 페닐을 나타내고 R3는 히드록실 또는 생체내에서 히드록실기로 전환될 수 있는 기이고, R4는 C1―6알킬을 나타내고, p는 0,1 또는 2이고, X는 ―CH2―, ―C〓O, O 또는 S이고, n은 4내지 10의 정수이고, m은 3내지 8의 정수이다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (12)
- 하기 일반식(I)의 화합물 또는 그의 염.(I)상기 식중에서 R1은 C1―6알킬, 할로겐 또는 페닐을 나타내고, R2는 수소 원자, C1―6알킬, 할로겐 또는 페닐을 나타내고 R3는 히드록실 또는 생체내에서 히드록실기로 전환될 수 있는 기이고, R4는 C1―6알킬을 나타내고, p는 0,1 또는 2이고, X는 ―CH2―, ―C〓O, O 또는 S이고, n은 4내지 10의 정수이고, m은 3내지 8의 정수이다.
- 제1항에 있어서, R1및 R2중 어느 하나 또는 모두가 분지쇄 C1―6알킬기인 화합물.
- 제1항 또는 2항에 있어서, p가 0인 화합물.
- 제1항 내지 3항 중 어느 한 항에 있어서, n이 5 내지 8의 정수인 화합물.
- 제1항 내지 4항 중 어느 한 항에 있어서, m이 4 내지 6의 정수인 화합물.
- 하기 일반식(I)의 화합물 및 이들의 염.1―〔6―옥소―6―(4―히드록시―3,5―디―t―부틸페닐)헥실〕피페리딘, 1―〔8―옥소―8―(4―히드록시―3,5―디―t―부틸페닐)옥틸〕피페리딘, 1―〔6―(4―히드록시―3,5―디―t―부틸페닐)헥실〕피페리딘, 1―〔8―(4―히드록시―3,5―디―t―부틸페닐)옥틸〕피페리딘, 1―〔7―(4―히드록시―3,5―디―t―부틸)티오페녹시―헵틸〕피페리딘, 1―〔7―(4―히드록시―3,5―디―t―부틸)페녹시헵틸〕피페리딘, 1―〔7―(4―옥소―7―(4―히드록시 3,5―디―t―부틸)헵틸〕피페리딘.
- (a)X가 O 또는 S인 화합물(I)을 제조 하기 위하여, 하기 일반식(II)의 화합물과 하기 일반식(III)의 화합물을 반응시키거나(상기 식 중, X1은 O 또는 S이고, m, n, p, R1, R2, R3및 R4는 일반식(I)에 정의된 바와 같고, L1은 친핵제와 치환가능한 기임), (b)하기 일반식(IV)의 화합물과 하기 일반식(V)의 화합물을 반응시키거나(상기 식 중, X, m, n, p, R1, R2, R3및 R4는 일반식(I)에 정의된 바와 같고, L2은 이탈기임), (c)하기 일반식(VI)의 화합물과 R1및 (또는) R2기를 도입시키는데 기여하는 화합물을 반응시키거나(상기 식 중, R1a및 R2a중 하나는 수소 원자이고, 다른 하나는 수소 원자, 할로겐, C1―6알킬 또는 페닐 중에서 선택되고, X, m, n, p, R1, R2, R3및 R4는 일반식(I)에 정의된 바와 같음), (d)X가 ―CH2―, S 또는 O인 화합물을 제조하기 위하여, 하기 일반식(VII) 또는 (VIII)의 아미드를 환원시키거나, 또는(e)일반식(I)의 화합물을 일반식(I)의 다른 화합물로 전환시키고, 계속하여 필요한 경우 염을 형성시키는 것을 포함하는, 상기 일반식(I)의 화합물을 제조 방법.
- 상기 일반식(I)의 화합물 또는 그의 제약상 허용되는 염의 유효량을 이를 필요로 하는 환자에게 투여하는 것을 포함하는, 자유 라디칼 관련 질환의 치료 방법.
- 상기 일반식(II)의 화합물 또는 그의 제약상 허용되는 염의 유효량을 이를 필요로 하는 환자에게 투여하는 것을 포함하는, 포유 동물의 뇌 세포에서 칼슘의 축적에 의해 발명되거나 또는 악화되는 상태 또는 질병의 치료방법.
- 유리 라디칼 관련 질환의 치료용 의약의 제조에 있어서의 상기 일반식(I)의 화합물 또는 그의 제약상 허용되는 염의 용도.
- 포유 동물의 뇌 세포에서 칼슘의 축적에 의해 발병되거나 또는 악화되는 상태 또는 질병의 치료용 의약의 제조에 있어서의 상기 일반식(I)의 화합물 또는 그의 제약상 허용되는 염의 용도.
- 상기 일반식(I)의 화합물 또는 그의 제약상 허용되는 염과 제약상 허용되는 담체 또는 부형제를 함유하는 제약 조성물.※ 참고사항:최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB929226718A GB9226718D0 (en) | 1992-12-22 | 1992-12-22 | Compounds |
GB939321808A GB9321808D0 (en) | 1993-10-22 | 1993-10-22 | Compounds |
GB9226718.6 | 1993-10-22 | ||
GB9321808.9 | 1993-10-22 | ||
PCT/EP1993/003629 WO1994014786A1 (en) | 1992-12-22 | 1993-12-16 | Piperidine derivatives as calcium channel antagonists |
Publications (1)
Publication Number | Publication Date |
---|---|
KR950704284A true KR950704284A (ko) | 1995-11-17 |
Family
ID=26302202
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019950702552A KR950704284A (ko) | 1992-12-22 | 1993-12-16 | 칼슘 채널 길항제로서의 피페리딘 유도체(Piperidine Derivatives as Calcium Channel Antagonists) |
Country Status (8)
Country | Link |
---|---|
EP (1) | EP0675883A1 (ko) |
JP (1) | JPH08504792A (ko) |
KR (1) | KR950704284A (ko) |
CN (1) | CN1092415A (ko) |
AU (1) | AU5833494A (ko) |
CA (1) | CA2152394A1 (ko) |
MX (1) | MX9400070A (ko) |
WO (1) | WO1994014786A1 (ko) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5677291A (en) * | 1993-12-10 | 1997-10-14 | Hoechst Marion Roussel, Inc. | Method of lowering serum cholesterol levels with 2,6-di-alkyl-4-silyl-phenols |
US5795876A (en) * | 1996-04-30 | 1998-08-18 | Hoechst Marion Rousssel, Inc. | Method of inhibiting vascular cell adhesion molecule-1 and treating chronic inflammatory diseases with 2, 6-di-alkyl-4-silyl-phenols |
US5608095A (en) * | 1996-04-30 | 1997-03-04 | Hoechst Marion Roussel, Inc. | Alkyl-4-silyl-phenols and esters thereof as antiatherosclerotic agents |
JP3588734B2 (ja) * | 1996-07-26 | 2004-11-17 | コニカミノルタホールディングス株式会社 | 電子写真感光体 |
US6114572A (en) * | 1996-11-20 | 2000-09-05 | Hoechst Marion Roussel, Inc. | Substituted phenols and thiophenols useful as antioxidant agents |
US6121463A (en) * | 1997-06-24 | 2000-09-19 | Hoechst Marion Roussel, Inc. | Alkyl-4-silylheterocyclic phenols and thiophenols useful as antioxidant agents |
US6133467A (en) * | 1997-06-25 | 2000-10-17 | Hoechst Marion Roussel, Inc. | 2,6-di-t-butyl-4-[(dimethyl-4-methoxyphenylsilyl)-methyl-oxy]phenol and 2,6-di-t-butyl-4-[(dimethyl-2-methoxy-phenylsilyl)methyloxy]phenol |
WO1999043658A1 (en) | 1998-02-27 | 1999-09-02 | Warner-Lambert Company | Heterocyclic substituted aniline calcium channel blockers |
US6166052A (en) | 1998-03-11 | 2000-12-26 | Warner-Lambert Company | Heteroaryl alkyl alpha substituted peptidylamine calcium channel blockers |
US7186726B2 (en) | 1998-06-30 | 2007-03-06 | Neuromed Pharmaceuticals Ltd. | Preferentially substituted calcium channel blockers |
US6943168B2 (en) | 1998-06-30 | 2005-09-13 | Neuromed Technologies Inc. | Calcium channel inhibitors comprising benzhydril spaced from piperazine |
US6951862B2 (en) | 1998-06-30 | 2005-10-04 | Neuromed Technologies, Inc. | Calcium channel blockers comprising two benzhydril moieties |
US6387897B1 (en) * | 1998-06-30 | 2002-05-14 | Neuromed Technologies, Inc. | Preferentially substituted calcium channel blockers |
KR100740477B1 (ko) * | 1999-12-21 | 2007-07-19 | 미쯔비시 웰 파마 가부시키가이샤 | 신경계 장애의 치료 및/또는 예방약 |
AU2006263564A1 (en) * | 2005-06-29 | 2007-01-04 | Merck Sharp & Dohme Corp. | 4-fluoro-piperidine T-type calcium channel antagonists |
CN113226468A (zh) | 2018-06-27 | 2021-08-06 | 康奈尔大学 | 作为hcn1拮抗剂的经取代的烷基苯酚 |
Family Cites Families (4)
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DE3233828A1 (de) * | 1982-09-11 | 1984-03-15 | Basf Ag, 6700 Ludwigshafen | Aryloxyalkylamine, verfahren zu ihrer herstellung und ihre verwendung zur bekaempfung unerwuenschten pflanzenwuchses |
DE3421810A1 (de) * | 1984-06-12 | 1985-12-12 | Basf Ag, 6700 Ludwigshafen | Phenylalkylamine - bioregulatoren |
DE3706585A1 (de) * | 1987-02-25 | 1988-09-08 | Schering Ag | Aryl- und aryloxy-substituierte tert.-alkylenamine, verfahren zu ihrer herstellung und ihre pharmazeutische verwendung |
PT100639A (pt) * | 1991-06-27 | 1993-09-30 | Univ Virginia Commonwealth | Metodo para o tratamento terapeutico com compostos que sao ligandos ao receptor sigma e compostos ai utilizados, nomeadamente derivados fenilalquil-amina, aminotetralina,piperazina e piperidina |
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1993
- 1993-12-16 EP EP94904162A patent/EP0675883A1/en not_active Withdrawn
- 1993-12-16 AU AU58334/94A patent/AU5833494A/en not_active Abandoned
- 1993-12-16 CA CA002152394A patent/CA2152394A1/en not_active Abandoned
- 1993-12-16 JP JP6514808A patent/JPH08504792A/ja active Pending
- 1993-12-16 KR KR1019950702552A patent/KR950704284A/ko not_active Application Discontinuation
- 1993-12-16 WO PCT/EP1993/003629 patent/WO1994014786A1/en not_active Application Discontinuation
- 1993-12-21 CN CN93112958A patent/CN1092415A/zh active Pending
-
1994
- 1994-01-03 MX MX9400070A patent/MX9400070A/es unknown
Also Published As
Publication number | Publication date |
---|---|
EP0675883A1 (en) | 1995-10-11 |
WO1994014786A1 (en) | 1994-07-07 |
CA2152394A1 (en) | 1994-07-07 |
CN1092415A (zh) | 1994-09-21 |
JPH08504792A (ja) | 1996-05-21 |
MX9400070A (es) | 1994-07-29 |
AU5833494A (en) | 1994-07-19 |
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