KR960037680A - 크로몬 유도체 - Google Patents
크로몬 유도체 Download PDFInfo
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- KR960037680A KR960037680A KR1019960012355A KR19960012355A KR960037680A KR 960037680 A KR960037680 A KR 960037680A KR 1019960012355 A KR1019960012355 A KR 1019960012355A KR 19960012355 A KR19960012355 A KR 19960012355A KR 960037680 A KR960037680 A KR 960037680A
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- compound
- ring
- unsubstituted
- salt
- pharmaceutically acceptable
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- 150000004777 chromones Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 18
- 150000003839 salts Chemical class 0.000 claims 13
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000001309 chloro group Chemical group Cl* 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 1
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 claims 1
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 claims 1
- 230000008485 antagonism Effects 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- QBTSRLXRTFDCQH-XZOQPEGZSA-N n-[(2r,4s)-1-[3,5-bis(trifluoromethyl)benzoyl]-2-[(4-chlorophenyl)methyl]piperidin-4-yl]-6-fluoro-4-oxochromene-2-carboxamide Chemical compound C([C@H]1N(CC[C@@H](C1)NC(=O)C=1OC2=CC=C(C=C2C(=O)C=1)F)C(=O)C=1C=C(C=C(C=1)C(F)(F)F)C(F)(F)F)C1=CC=C(Cl)C=C1 QBTSRLXRTFDCQH-XZOQPEGZSA-N 0.000 claims 1
- MNLDOIFGGVZJHR-XZOQPEGZSA-N n-[(2r,4s)-2-benzyl-1-[3,5-bis(trifluoromethyl)benzoyl]piperidin-4-yl]-4-oxochromene-2-carboxamide Chemical compound FC(F)(F)C1=CC(C(F)(F)F)=CC(C(=O)N2[C@@H](C[C@H](CC2)NC(=O)C=2OC3=CC=CC=C3C(=O)C=2)CC=2C=CC=CC=2)=C1 MNLDOIFGGVZJHR-XZOQPEGZSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 239000003890 substance P antagonist Substances 0.000 abstract 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/08—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing alicyclic 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
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- A—HUMAN NECESSITIES
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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- A61P11/06—Antiasthmatics
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- A61P11/08—Bronchodilators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
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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
- A61P25/08—Antiepileptics; Anticonvulsants
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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
- A61P25/20—Hypnotics; Sedatives
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
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- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P9/12—Antihypertensives
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- Pain & Pain Management (AREA)
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- Cardiology (AREA)
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- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
하기 일반식(Ⅰ)의 화합물은 약리학상 가치있는 특성을 지니며, 특히 NK1 길항제 및 물질 P 길항제로서 유용하다.
상기 식에서, 고리 A 및 고리 B는 각각 명세서에서 정의한 바와 같다. 상기 화합물은 그 자체 공지의 방식으로 제조된다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (11)
- 하기 일반식(Ⅰ)의 화합물 또는 그의 염.상기 식에서, 고리 A는 비치환되거나 또는 저급 알킬, 저급 알콕시, 할로겐, 니트로 또는 트리플루오로메틸에 의해 일치환되며 ; 고리 B는 비치환되거나 또는 저급 알킬, 히드록시, 저급 알콕시, 저급 알킬티오, 할로겐, 니트로, 시아노 및 트리플루오로메틸로 이루어진 군 중에서 선택된 1 내지 4개의 치환체에 의해 치환된다.
- 제1항에 있어서, 고리 A가 비치환되거나 또는 할로겐에 의해 일치환되고 고리 B는 비치환되거나 또는 저급 알킬, 히드록시, 저급 알콕시, 저급 알킬티오, 할로겐, 니트로 및 시아노로 이루어진 군 중에서 선택된 1 또는 2개의 치환체에 의해 치환된 일반식(Ⅰ)의 화합물 또는 제약학상 허용되는 그의 염.
- 제1항에 있어서, 고리 A가 비치환되거나 또는 클로로에 의해 일치환되며 고리 B는 비치환되거나 또는 히드록시, 저급 알콕시, 클로로 및 브로모로 이루어진 군 중에서 선택된 1 또는 2개의 치환체에 의해 치환된 일반식(Ⅰ)의 화합물 또는 제약학상 허용되는 그의 염.
- 제1항에 있어서, 고리 A가 비치환되거나 또는 클로로에 의해 일치환되며 고리 B는 비치환되거나 또는 클로로 또는 플루오로에 의해 일치환된 일반식(Ⅰ)의 화합물 또는 제약학상 허용되는 그의 염.
- 제1항에 있어서, 일반식(Ⅰ)의 화합물이 하기 일반식(Ⅰa)로 표시되는 디아스테레오이소머 형태인 것인 화합물.
- 제1항에 따른 (2R,4S)-N-〔1-(3,5-비스트리플루오로메틸벤조일)-2-(4-클로로벤질)피페리딘-4-일〕-4-옥소-4H-1-벤조피란-2-카르복소아미드 또는 제약학상 허용되는 그의 염.
- 제1항에 따른 (2R,4S)-N-〔1-(3,5-비스트리플루오로메틸벤조일)-2-벤질피페리딘-4-일〕-옥소-4H-1-벤조피란-2-카르복소아미드 또는 제약학상 허용되는 그의 염.
- 제1항에 따른 (2R,4S)-N-〔1-(3,5-비스트리플루오로메틸벤조일)-2-(4-클로로벤질)피페리딘-4-일〕-6-플루오로-4-옥소-4H-1-벤조피란-2-카르복소아미드 또는 제약학상 허용되는 그의 염.
- 제1항에 따른 화합물 치료 유효량 및 하나 이상의 제약학상 허용되는 담체를 포함하는 제약 조성물.
- 제1항에 따른 화합물 또는 제약학상 허용되는 그의 염 치료 유효량을 이를 필요로 하는 포유류에게 투여하는 단계를 포함하는 NK1 수용체의 길항작용에 반응하는 질환의 치료 방법.
- (a) 하기 일반식(Ⅱa)의 화합물을 하기 일반식(Ⅱb)의 화합물, 또는 하기 구조시(Ⅱb')의 라디칼 또는 그의 염과 반응시키는 공정, 또는 (b) 하기 일반식(Ⅲa)의 화합물을 하기 일반식(Ⅲb)의 화합물, 또는 하기 구조식(Ⅲb')의 라디칼 또는 그의 염과 반응시키는 공정, 및 필요에 따라서, 일반식(Ⅰ)의 화합물을 다른 일반식(Ⅰ)의 화합물로 전환시키고(시키거나), 필요에 따라서, 얻어진 염을 유리 화합물 또는 다른 염으로 전환시키고(시키거나), 필요에 따라서, 염 형성 특성을 갖는 얻어진 일반식(Ⅰ)의 유리 화합물을 염으로 전환시키고(시키거나), 필요에 따라서, 얻어진 스테레오이소머 또는 디아스테레오이소머의 혼합물을 개개 스테레오이소머 또는 디아스테레오이소머로 분리시키는 공정을 포함하는 제1항에 따른 일반식(Ⅰ)의 화합물의 제조 방법.상기 식에서, 고리 A 및 고리 B는 각각 제1항에 따른 일반식(Ⅰ)에서 정의한 바와 같고, Q1은 에테르화될 수 있는 히드록시, 예를 들면 히드록시, 저급 알콕시 또는 비치환 또는 치환 페녹시, 또는 반응성 에스테르화 히드록시, 예를 들면 할로겐, 바람직하게는 클로로이다.※ 참고사항 : 최초출원 내용에 의하여 공개되는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CH1157/95-3 | 1995-04-24 | ||
CH115795 | 1995-04-24 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR960037680A true KR960037680A (ko) | 1996-11-19 |
KR100416674B1 KR100416674B1 (ko) | 2004-06-11 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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KR1019960012355A KR100416674B1 (ko) | 1995-04-24 | 1996-04-23 | 크로몬유도체 |
Country Status (21)
Country | Link |
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US (1) | US5604247A (ko) |
EP (1) | EP0739892B1 (ko) |
JP (1) | JP3068458B2 (ko) |
KR (1) | KR100416674B1 (ko) |
CN (1) | CN1063176C (ko) |
AR (1) | AR001813A1 (ko) |
AT (1) | ATE224891T1 (ko) |
AU (1) | AU714523B2 (ko) |
BR (1) | BR9602025A (ko) |
CA (1) | CA2174707C (ko) |
DE (1) | DE59609707D1 (ko) |
DK (1) | DK0739892T3 (ko) |
ES (1) | ES2183923T3 (ko) |
HU (1) | HUP9601062A3 (ko) |
IL (1) | IL117989A (ko) |
NO (1) | NO309813B1 (ko) |
NZ (1) | NZ286422A (ko) |
PT (1) | PT739892E (ko) |
RU (1) | RU2156250C2 (ko) |
TW (1) | TW475930B (ko) |
ZA (1) | ZA963211B (ko) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2255910A1 (en) * | 1996-05-24 | 1997-11-27 | Mitchell Irvin Steinberg | Methods of treating hypertension |
TW426667B (en) * | 1997-11-19 | 2001-03-21 | Pfizer | Piperidinylaminomethyl trifluoromethyl cyclic ether compounds as substance P antagonists |
CN1216598C (zh) * | 1998-08-25 | 2005-08-31 | 诺瓦提斯公司 | 药物用途 |
WO2000071538A2 (en) * | 1999-05-21 | 2000-11-30 | Pfizer Products Inc. | 1-trifluoromethyl-4-hydroxy-7-piperidinyl-aminomethylchroman derivatives |
GB0220953D0 (en) | 2002-09-10 | 2002-10-23 | Novartis Ag | Organic compounds |
GB2394417A (en) * | 2002-10-24 | 2004-04-28 | Novartis Ag | Solid dispersion comprising a piperidine substance P antagonist and a carrier |
DE10256182A1 (de) * | 2002-12-02 | 2004-06-24 | Merck Patent Gmbh | 2-Oxadiazolchromonderivate |
DE10256174A1 (de) * | 2002-12-02 | 2004-06-09 | Merck Patent Gmbh | 2-Benzoylchromonderivate |
US20050209274A1 (en) * | 2004-02-26 | 2005-09-22 | Lynch John K | Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor |
CN1300163C (zh) * | 2004-06-23 | 2007-02-14 | 南京大学 | 3-羟基色原酮糖苷及其制法和用途 |
MY144307A (en) * | 2006-04-18 | 2011-08-29 | Abbott Lab | Antagonists of the vanilloid receptor subtype 1 (vr1) and uses thereof |
GB0701365D0 (en) * | 2007-01-24 | 2007-03-07 | Glaxo Group Ltd | Novel pharmaceutical compositions |
UA105182C2 (ru) | 2008-07-03 | 2014-04-25 | Ньюрексон, Інк. | Бензоксазины, бензотиазины и родственные соединения, которые имеют ингибирующую nos активность |
Family Cites Families (5)
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DE3117389A1 (de) * | 1981-05-02 | 1982-11-18 | Boehringer Mannheim Gmbh, 6800 Mannheim | Benzopyranylether, verfahren zu deren herstellung sowie diese verbindungen enthaltende arzneimittel |
MY110227A (en) * | 1991-08-12 | 1998-03-31 | Ciba Geigy Ag | 1-acylpiperindine compounds. |
AU7856194A (en) * | 1993-10-26 | 1995-05-22 | Ciba-Geigy Ag | N-benzoyl-4-oxy/thio-2-substituted piperidines as substance-p receptor antagonists |
US5935951A (en) * | 1994-09-30 | 1999-08-10 | Novartis Finance Corporation | 1-acyl-4-aliphatylaminopiperidine compounds |
TW397825B (en) * | 1994-10-14 | 2000-07-11 | Novartis Ag | Aroyl-piperidine derivatives |
-
1996
- 1996-04-11 RU RU96107121/04A patent/RU2156250C2/ru not_active IP Right Cessation
- 1996-04-11 TW TW085104270A patent/TW475930B/zh not_active IP Right Cessation
- 1996-04-16 PT PT96810237T patent/PT739892E/pt unknown
- 1996-04-16 ES ES96810237T patent/ES2183923T3/es not_active Expired - Lifetime
- 1996-04-16 DE DE59609707T patent/DE59609707D1/de not_active Expired - Lifetime
- 1996-04-16 AT AT96810237T patent/ATE224891T1/de not_active IP Right Cessation
- 1996-04-16 EP EP96810237A patent/EP0739892B1/de not_active Expired - Lifetime
- 1996-04-16 US US08/632,971 patent/US5604247A/en not_active Expired - Lifetime
- 1996-04-16 DK DK96810237T patent/DK0739892T3/da active
- 1996-04-21 IL IL11798996A patent/IL117989A/xx active IP Right Grant
- 1996-04-22 CA CA002174707A patent/CA2174707C/en not_active Expired - Fee Related
- 1996-04-22 NZ NZ286422A patent/NZ286422A/en unknown
- 1996-04-22 AU AU50805/96A patent/AU714523B2/en not_active Ceased
- 1996-04-23 ZA ZA963211A patent/ZA963211B/xx unknown
- 1996-04-23 CN CN96106111A patent/CN1063176C/zh not_active Expired - Fee Related
- 1996-04-23 NO NO961616A patent/NO309813B1/no unknown
- 1996-04-23 JP JP8101568A patent/JP3068458B2/ja not_active Expired - Fee Related
- 1996-04-23 HU HU9601062A patent/HUP9601062A3/hu unknown
- 1996-04-23 KR KR1019960012355A patent/KR100416674B1/ko not_active IP Right Cessation
- 1996-04-24 AR AR33626596A patent/AR001813A1/es unknown
- 1996-04-24 BR BR9602025A patent/BR9602025A/pt not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
JPH093066A (ja) | 1997-01-07 |
HUP9601062A2 (en) | 1997-10-28 |
EP0739892A3 (de) | 1997-01-22 |
AU5080596A (en) | 1996-11-07 |
ES2183923T3 (es) | 2003-04-01 |
HU9601062D0 (en) | 1996-06-28 |
CA2174707A1 (en) | 1996-10-25 |
RU2156250C2 (ru) | 2000-09-20 |
NO309813B1 (no) | 2001-04-02 |
EP0739892A2 (de) | 1996-10-30 |
MX9601515A (es) | 1997-09-30 |
US5604247A (en) | 1997-02-18 |
NO961616L (no) | 1996-10-25 |
AU714523B2 (en) | 2000-01-06 |
TW475930B (en) | 2002-02-11 |
NO961616D0 (no) | 1996-04-23 |
CN1141921A (zh) | 1997-02-05 |
DK0739892T3 (da) | 2003-01-20 |
ATE224891T1 (de) | 2002-10-15 |
ZA963211B (en) | 1996-10-24 |
IL117989A0 (en) | 1996-08-04 |
JP3068458B2 (ja) | 2000-07-24 |
CA2174707C (en) | 2008-03-25 |
CN1063176C (zh) | 2001-03-14 |
DE59609707D1 (de) | 2002-10-31 |
NZ286422A (en) | 1998-01-26 |
IL117989A (en) | 2000-01-31 |
PT739892E (pt) | 2003-01-31 |
EP0739892B1 (de) | 2002-09-25 |
HUP9601062A3 (en) | 1998-10-28 |
AR001813A1 (es) | 1997-12-10 |
KR100416674B1 (ko) | 2004-06-11 |
BR9602025A (pt) | 1998-10-06 |
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