KR910004665A - 사이클릭 뉴로키닌 a 길항제 - Google Patents
사이클릭 뉴로키닌 a 길항제 Download PDFInfo
- Publication number
- KR910004665A KR910004665A KR1019900012226A KR900012226A KR910004665A KR 910004665 A KR910004665 A KR 910004665A KR 1019900012226 A KR1019900012226 A KR 1019900012226A KR 900012226 A KR900012226 A KR 900012226A KR 910004665 A KR910004665 A KR 910004665A
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- KR
- South Korea
- Prior art keywords
- phe
- peptide derivative
- group
- trp
- gln
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/22—Tachykinins, e.g. Eledoisins, Substance P; Related peptides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/64—Cyclic peptides containing only normal peptide links
-
- 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
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Transplantation (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
내용 없음.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 뉴로키닌 A(NKA) 수용체에서 작용제의 결합 억제에 대한 시클로(Gln-Trp-Phe-Gly-Leu-CH2NH-Leu)와 시클로(Gln-Trp-Phe-Gly-Leu-CH2NCH3-Leu)의 능력을 나타낸다,
제2도 및 제3도는 수용체로 매개된 NKA 유도 PI 전환으로 되는 길항제의 생성에 대한 시클로 (Gln-Trp-Phe-Gly-Leu-CH2NH-Leu)와 시클로 (Gln-Trp-Phe-Gly-Leu-CH2NCH3-Leu)의 능력을 나타낸다.
Claims (27)
- 하기 구조식(I)의 펩티드 유도체 또는 제약학상 허용되는 그의 염.위 식에서, A1은 Gln, gln, His, his, Asn, asn이거나 또는 식(여기서, R″는 아미노기로 치환된 C1-C5알킬기임)으로 표시되는 기이고, A2는 Trp, trp, Phe, phe, Tyr, tyr, Phg, phg, Cha, cha, Phe(4′-Cl), phe(4′-Cl), NPa, npa, Phe(4′-NO2) 또는 phe(4′-NO2)이며, A3는 Trp, trp, Phe, phe, Tyr, tyr, Phg, phg, Cha, cha, Phe(4′-Cl), phe(4′-Cl), Npa, npa, Phe(4′-NO2) 또는 phe(4′-NO2)이며, Val 또는 val이고, A4는 Gly, Ala, ala또는 β-Ala이며, B는 하기식 (a)-(g)으로 되는 군중에서 선택되는 기이고, (a), (b) -S-CH2-, (c) -O-CH2-, (d) -CH=CH-, (e), (f) -CH2-CH(OH)- 및 (g), 여기서, R은 수소 원자 또는 C1-C4알킬기이거나, 또는 페닐알킬렌기로, 단, 이 페닐알킬렌기의 알킬렌 부분은 C1-C6의 직쇄상 또는 분지상이고 페닐 부분은 치환되지 않았거나 또는 C1-4알킬, C1-4알콕시, 히드록시 또는 할로겐기로 치환되며, R1및 R2는 각기 독립적으로 이소프로필기, 이소부틸기, scc-부틸기, n-부틸기 및 2-(메틸티오)에틸기롤부터 선택된다.
- 제1항에 있어서, A1이 Gln, gln, Asn 또는 asn인 펩타이드 유도체.
- 제1항에 있어서, A2는 Trp, trp, Phe, phe, Tyr, tyr, Phg, 또는 phg인 펩타이드 유도체.
- 제1항에 있어서, A3는 Trp, trp, Phe, phe, Tyr, tyr, Phg, 또는 phg인 펩타이드 유도체.
- 제1항에 있어서 A4이 Gln, Ala 또는 ala인 펩타이드 유도체.
- 제1항에 있어서, A1이 Gln, gln, Asn 또는 asn이고, A2및 A3가 각기 Trp, trp, Phe, phe, Tyr, tyr, Cha, cha, Phg 또는 phg이며, A4이 Gly, Ala 또는 ala인 펩타이드 유도체.
- 제2항 내지 제6항 중 어느 하나의 항에 있어서, B가 -CH2NH2-인 펩타이드 유도체.
- 제2항 내지 제6항 중 어느 하나의 항에 있어서, R1이 n-부틸기인 펩타이드 유도체.
- 제2항 내지 제6항 중 어느 하나의 항에 있어서, R2가 2-메틸티오에틸기, 이소부틸기 또는 n-부틸기인 펩타이드 유도체.
- 제1항에 있어서, A1이 Gln인 펩타이드 유도체.
- 제1항에 있어서, A2는 Trp 또는 Phe인 펩타이드 유도체.
- 제1항에 있어서, A3는 Trp 또는 Phe인 펩타이드 유도체.
- 제1항에 있어서, A4이 Gly인 펩타이드 유도체.
- 제1항에 있어서, A1이 Gln이고, A2및 A3가 각기 Trp 또는 Phe이며, A4이 Gly인 펩타이드 유도체.
- 제10항 내지 제14항 중 어느 하나의 항에 있어서, B가 -CH2NH2-인 펩타이드 유도체.
- 제10항 내지 제14항 중 어느 하나의 항에 있어서, R1이 이소부틸기인 펩타이드 유도체.
- 제10항 내지 제14항 중 어느 하나의 항에 있어서, R2가 2-메틸티오에틸기, 이소부틸기 또는 n-부틸기인 펩타이드 유도체.
- 제1항에 있어서, A1이 Gln인 펩타이드 유도체.
- 제1항에 있어서, A2는 Trp 펩타이드 유도체.
- 제1항에 있어서, A3는 Phe인 펩타이드 유도체.
- 제1항에 있어서, A4이 Gly인 펩타이드 유도체.
- 제18항 내지 제21항 중 어느 하나의 항에 있어서, B가 -CH2NH2-인 펩타이드 유도체.
- 제18항 내지 제21항 중 어느 하나의 항에 있어서, R1이 이소부틸기인 펩타이드 유도체.
- 제18항 내지 제21항 중 어느 하나의 항에 있어서, R2가 2-메틸티오에틸기, 이소부틸기 또는 n-부틸기인 펩타이드 유도체.
- 제18항 내지 제21항 중 어느 하나의 항에 있어서, B가 -CH2NH2-이고, R1이 이소부틸기이며, R2가 2-메틸티오에틸기, 이소부틸기 또는 n-부틸기인 펩타이드 유도체.
- 제1항에 있어서, A1이 Gln이고, A2는 Trp이며, A3는 Gly이고, B는 -CH2NH2-이고, R1및R2가 각기 이소부틸기인 펩타이드 유도체.
- 뉴로키닌 A의 길항 작용이 필요한 환자에게 제1항의 펩타이드 유도체를 유효량 투여하는 것으로 이루어진 뉴로키닌 A의 길항 작용의 효과를 얻는 방법,※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US39223689A | 1989-08-10 | 1989-08-10 | |
US392,236 | 1989-08-10 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR910004665A true KR910004665A (ko) | 1991-03-29 |
KR0169123B1 KR0169123B1 (ko) | 1999-01-15 |
Family
ID=23549831
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019900012226A KR0169123B1 (ko) | 1989-08-10 | 1990-08-09 | 사이클릭 뉴로키닌 a 길항제 |
Country Status (22)
Country | Link |
---|---|
US (1) | US5731286A (ko) |
EP (1) | EP0412542B1 (ko) |
JP (1) | JP2829779B2 (ko) |
KR (1) | KR0169123B1 (ko) |
CN (1) | CN1035056C (ko) |
AR (1) | AR246087A1 (ko) |
AT (1) | ATE132503T1 (ko) |
AU (1) | AU638264B2 (ko) |
CA (1) | CA2022740C (ko) |
DD (1) | DD297168A5 (ko) |
DE (1) | DE69024555T2 (ko) |
DK (1) | DK0412542T3 (ko) |
ES (1) | ES2084627T3 (ko) |
FI (1) | FI95913C (ko) |
GR (1) | GR3018984T3 (ko) |
HU (1) | HU206729B (ko) |
IE (1) | IE69382B1 (ko) |
IL (1) | IL95309A (ko) |
NO (1) | NO177715C (ko) |
NZ (1) | NZ234814A (ko) |
PT (1) | PT94952B (ko) |
ZA (1) | ZA906188B (ko) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ZA894533B (en) * | 1988-06-20 | 1990-03-28 | Merrell Dow Pharma | Neurokinin a antogonists |
DE4034829A1 (de) * | 1990-11-02 | 1992-05-07 | Merck Patent Gmbh | Cyclopeptide |
US5625060A (en) * | 1991-05-03 | 1997-04-29 | Elf Sanofi | Polycyclic amine compounds and their enantiomers, their method of preparation and pharmaceutical compositions on which they are present |
FR2676055B1 (fr) * | 1991-05-03 | 1993-09-03 | Sanofi Elf | Composes polycycliques amines et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant. |
JPH06509571A (ja) * | 1991-08-08 | 1994-10-27 | エイ・メナリニ・インダストリー・ファーマシューティケ・リウニテ・エスアールエル | タキキニン拮抗薬としての環状ヘキサペプチドの製法およびその薬学的化合物 |
US5731285A (en) * | 1992-04-15 | 1998-03-24 | A. Menatini Industrie Farmaceutiche | Tachiquinine antagonist tricyclic compounds, preparation of same and pharmaceutical compositions containing such compounds |
JP5866277B2 (ja) * | 2009-03-16 | 2016-02-17 | ザ ガバニング カウンシル オブ ザ ユニバーシティ オブ トロント | 環状アミノ酸分子およびその製造方法 |
WO2017079821A1 (en) | 2015-11-11 | 2017-05-18 | Encycle Therapeutics, Inc. | Fragment synthesis of cyclic peptides |
EP3939989A1 (en) | 2016-11-11 | 2022-01-19 | Zealand Pharma A/S | Cyclic peptides multimers targeting alpha 4beta 7 integrin |
EP3621980A4 (en) | 2017-05-10 | 2021-06-30 | Zealand Pharma A/S | HOMODETIC CYCLIC PEPTIDES TARGETING INTEGRIN ALPHA4 BETA7 |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4742156A (en) * | 1985-09-30 | 1988-05-03 | Mcneilab, Inc. | Peptide antagonists of neurokinin B and opthalmic solutions containing them |
US4665157A (en) * | 1985-09-30 | 1987-05-12 | Mcneilab, Inc. | Peptide antagonists of neurokinin B |
DE3711335A1 (de) * | 1987-04-03 | 1988-10-20 | Merck Patent Gmbh | Aminosaeurederivate |
GB8807246D0 (en) * | 1988-03-25 | 1988-04-27 | Merck Sharp & Dohme | Therapeutic agents |
ZA894533B (en) * | 1988-06-20 | 1990-03-28 | Merrell Dow Pharma | Neurokinin a antogonists |
FI97540C (fi) * | 1989-11-06 | 1997-01-10 | Sanofi Sa | Menetelmä terapeuttisesti käyttökelpoisten, aromaattisesti substituoitujen piperidiini- ja piperatsiinijohdannaisten valmistamiseksi |
IL99320A (en) * | 1990-09-05 | 1995-07-31 | Sanofi Sa | Arylalkylamines, their preparation and pharmaceutical preparations containing them |
FR2677361A1 (fr) * | 1991-06-04 | 1992-12-11 | Adir | Nouveaux peptides et pseudopeptides, derives de tachykinines, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
-
1990
- 1990-08-06 ZA ZA906188A patent/ZA906188B/xx unknown
- 1990-08-06 AU AU60222/90A patent/AU638264B2/en not_active Expired
- 1990-08-07 CA CA002022740A patent/CA2022740C/en not_active Expired - Lifetime
- 1990-08-07 AR AR90317547A patent/AR246087A1/es active
- 1990-08-07 IL IL9530990A patent/IL95309A/en not_active IP Right Cessation
- 1990-08-08 NZ NZ234814A patent/NZ234814A/en unknown
- 1990-08-08 FI FI903922A patent/FI95913C/fi active IP Right Grant
- 1990-08-09 DK DK90115309.8T patent/DK0412542T3/da active
- 1990-08-09 EP EP90115309A patent/EP0412542B1/en not_active Expired - Lifetime
- 1990-08-09 DE DE69024555T patent/DE69024555T2/de not_active Expired - Lifetime
- 1990-08-09 CN CN90106972A patent/CN1035056C/zh not_active Expired - Fee Related
- 1990-08-09 HU HU904952A patent/HU206729B/hu not_active IP Right Cessation
- 1990-08-09 JP JP2209390A patent/JP2829779B2/ja not_active Expired - Lifetime
- 1990-08-09 AT AT90115309T patent/ATE132503T1/de not_active IP Right Cessation
- 1990-08-09 NO NO903513A patent/NO177715C/no unknown
- 1990-08-09 KR KR1019900012226A patent/KR0169123B1/ko not_active IP Right Cessation
- 1990-08-09 ES ES90115309T patent/ES2084627T3/es not_active Expired - Lifetime
- 1990-08-09 PT PT94952A patent/PT94952B/pt not_active IP Right Cessation
- 1990-08-09 IE IE288690A patent/IE69382B1/en not_active IP Right Cessation
- 1990-08-10 DD DD90343398A patent/DD297168A5/de unknown
-
1996
- 1996-02-14 GR GR960400385T patent/GR3018984T3/el unknown
-
1997
- 1997-03-05 US US08/811,913 patent/US5731286A/en not_active Expired - Fee Related
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