KR850000467A - 약학적 유용 펩티드의 제조방법 - Google Patents
약학적 유용 펩티드의 제조방법 Download PDFInfo
- Publication number
- KR850000467A KR850000467A KR1019840002863A KR840002863A KR850000467A KR 850000467 A KR850000467 A KR 850000467A KR 1019840002863 A KR1019840002863 A KR 1019840002863A KR 840002863 A KR840002863 A KR 840002863A KR 850000467 A KR850000467 A KR 850000467A
- Authority
- KR
- South Korea
- Prior art keywords
- hydrogen
- peptide
- general formula
- same
- process according
- Prior art date
Links
- 108090000765 processed proteins & peptides Proteins 0.000 title claims 10
- 238000000034 method Methods 0.000 title claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 238000004519 manufacturing process Methods 0.000 claims 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 4
- 239000003153 chemical reaction reagent Substances 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 3
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 230000002862 amidating effect Effects 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- GAZRNXIMWKZADY-UHFFFAOYSA-N 3,5-dimethylpyrazole-1-carboximidamide Chemical compound CC=1C=C(C)N(C(N)=N)N=1 GAZRNXIMWKZADY-UHFFFAOYSA-N 0.000 claims 1
- 101800001415 Bri23 peptide Proteins 0.000 claims 1
- 101800000655 C-terminal peptide Proteins 0.000 claims 1
- 102400000107 C-terminal peptide Human genes 0.000 claims 1
- 125000002038 D-arginyl group Chemical group N[C@@H](C(=O)*)CCCNC(=N)N 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- 229940059260 amidate Drugs 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 229910021529 ammonia Inorganic materials 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- NPUKDXXFDDZOKR-LLVKDONJSA-N etomidate Chemical compound CCOC(=O)C1=CN=CN1[C@H](C)C1=CC=CC=C1 NPUKDXXFDDZOKR-LLVKDONJSA-N 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- 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
- A61P11/14—Antitussive agents
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/665—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
- C07K14/70—Enkephalins
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Molecular Biology (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Toxicology (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
내용 없음.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (12)
- 시제(II)와 시제(III)을 반응시키는 것과 반응 C-말단 펩티드 카르복실산 또는 그것의 적합한 반응 유도체를 아미드화 시키는 것과 1-아미디노-3,5-디메틸피라졸 또는 화학적으로 상등한 시제를 사용하여 X2가 하기의 D-라디칼인 상응 펩티드를 아미드화시키는 것과 그 생산물을 유기펩티드 또는 그것의 염으로 적합하게 전환시키는 것을 특징으로하는 하기 일반식(I)펩티드 또는 그것의 염을 제조하는 방법.일반식(I)에서 R'은 수소, 1 또는 2탄소원자의 알킬 또는 페아미디노기, R2는 1 또는 2탄소원자의 알킬, R3는 수소 또는 카바밀, X2는 하기 구조의 D-라디칼Z1과 Z2는 동일 또는 다르게 각각 수소, 할로, 니트로, 또는 트리플루오로메틸이며 최소한 하나는 수소 이외의 것이다. m은 2,3 또는 4, n이 0,1 또는 2며 R3가 카바밀일때 n은 항상 1이다. 일반식(II)에서 R1은 일반식(I)에서와 같으며 Y1은 일반식(I)에서의 상응 N-말단부분의 라디칼서열과 동일하며, 일반식(III)에서 Y2는 상기 정의된 생산 펩티드의 남은 부분과 동일하며 그것의 상융 C-말단부분 라디칼 서열을 포함하며, 시제(II)와(III)은 적당한 곳에서 임의적으로 보호 및 또는 활성화되고 적절하게 생산물의 탈보호가 수행된다. 또한 상기 X2에서 m은 일반식(I)에서와 같고 R5는 수소 또는 아미디노기이며 R1과 R5중 최소한 하나는 수소이다.
- 제1항에 있어서, 암모니아를 펩티드 에스테르(IV)와 반응시킴을 특징으로하는, R3가 카바밀인 일반식(I)의 펩티드 또는 그것의 염의 제조방법.여기에서 R1,R2,X2,Z1과 Z2는 일반식(I)과 같고, -OR4는 적합한 치환성 알콕시, 아르알콕시 또는 아릴옥시기이다.
- 제1항에 있어서, 펩티드 카르복실산(V) 또는 그것의 반응 유도체를 아민(VI)과 반응시키는 것을 특징으로 하는 일반식(I)의 펩티드 제조방법.여기에서 R1,R2,X2,Z1,Z2와 n은 일반식(I)과 같다.
- 제1항 내지 3항중 어느 한항에 있어서 R1이 아미노기인 제조방법.
- 제1항 내지 3항중 어느 한항에 있어서, X2가 D-아르기닐인 제조방법.
- 제1항 내지 5항중 어느 한항에 있어서 R2가 에틸렌인 제조방법.
- 제1,2항과 4항 내지 6항중 어느 한항에 있어서, R3가 카바밀인 제조방법.
- 제1항과 3항 내지 6항의 어느한항에 있어서 R3가 수소인 제조방법.
- 제1,3항 내지 6항과 8항의 어느 한항에 있어서 n이 1인 제조방법.
- 제1항 내지 9항중 어느 한항에 있어서 Z1과 Z2중 하나가 수소이며 다른 하나가 니트로 또는 플루오로인 제조방법.
- 제1항 내지 9항중 어느 한항에 있어서 Z1과 Z2중 하나가 수소이며 다른 하나가 4- 위치에 존재하는 제조방법.
- 제1항에 있어서, R1이 수소인 각각 상응한 일반식(I)의 펩티드를 아미드화시키는 것을 특징으로 하고, H2NC(:HN) Ty2·D-Arg·Gly·N(C2H5)·CH2 H2N(:HN)·Ty2·D-Arg · Gly·Et Phe(4NO2) · NH2와 H2NC(: HN) · Tyr · D-Arg · Gly · Et Phe(4F) ·NH2로 부터 선택된 펩티드 또는 그것의 염을 제조하는 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB838314646A GB8314646D0 (en) | 1983-05-26 | 1983-05-26 | Pharmaceutical amides |
GB8314646 | 1983-05-26 |
Publications (1)
Publication Number | Publication Date |
---|---|
KR850000467A true KR850000467A (ko) | 1985-02-27 |
Family
ID=10543432
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019840002863A KR850000467A (ko) | 1983-05-26 | 1984-05-25 | 약학적 유용 펩티드의 제조방법 |
Country Status (17)
Country | Link |
---|---|
US (1) | US4540682A (ko) |
EP (1) | EP0127154B1 (ko) |
JP (1) | JPS59231053A (ko) |
KR (1) | KR850000467A (ko) |
AT (1) | ATE57188T1 (ko) |
AU (1) | AU575324B2 (ko) |
CA (1) | CA1251898A (ko) |
DE (1) | DE3483338D1 (ko) |
DK (1) | DK258884A (ko) |
ES (2) | ES8606395A1 (ko) |
FI (1) | FI82254C (ko) |
GB (1) | GB8314646D0 (ko) |
GR (1) | GR81890B (ko) |
HU (1) | HU193569B (ko) |
IL (1) | IL71932A (ko) |
NZ (1) | NZ208283A (ko) |
ZA (1) | ZA844004B (ko) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB8622090D0 (en) * | 1986-09-12 | 1986-10-22 | Wellcome Found | Pharmacologically active compounds |
US6258550B1 (en) | 1993-04-23 | 2001-07-10 | Virginia Commonwealth University | Polypeptides that include conformation-constraining groups which flank a protein-protein interaction site |
US5928896A (en) * | 1993-04-23 | 1999-07-27 | Virginia Commonwealth University | Polypeptides that include conformation-constraining groups which flank a protein--protein interaction site |
US5952465A (en) * | 1993-04-23 | 1999-09-14 | Virginia Commonwealth University | Polypeptides that include conformation-constraining groups which flank a protein-protein interaction site |
AU6770794A (en) * | 1993-04-23 | 1994-11-21 | Herbert J. Evans | Polypeptides that include conformation-constraining groups which flank a protein-protein interaction site |
US5965698A (en) * | 1993-04-23 | 1999-10-12 | Virginia Commonwealth University | Polypeptides that include conformation-constraining groups which flank a protein--protein interaction site |
US6084066A (en) * | 1993-10-29 | 2000-07-04 | Virginia Commonwealth University | Polypetides that include conformation-constraining groups which flank a protein-protein interaction site |
US6190691B1 (en) | 1994-04-12 | 2001-02-20 | Adolor Corporation | Methods for treating inflammatory conditions |
US5962477A (en) * | 1994-04-12 | 1999-10-05 | Adolor Corporation | Screening methods for cytokine inhibitors |
US6573282B1 (en) | 1995-09-12 | 2003-06-03 | Adolor Corporation | Peripherally active anti-hyperalgesic opiates |
US5849761A (en) * | 1995-09-12 | 1998-12-15 | Regents Of The University Of California | Peripherally active anti-hyperalgesic opiates |
US6613508B1 (en) | 1996-01-23 | 2003-09-02 | Qiagen Genomics, Inc. | Methods and compositions for analyzing nucleic acid molecules utilizing sizing techniques |
US6312893B1 (en) | 1996-01-23 | 2001-11-06 | Qiagen Genomics, Inc. | Methods and compositions for determining the sequence of nucleic acid molecules |
US6027890A (en) * | 1996-01-23 | 2000-02-22 | Rapigene, Inc. | Methods and compositions for enhancing sensitivity in the analysis of biological-based assays |
AU6990796A (en) * | 1996-08-23 | 1998-03-06 | Sederma Sa | Synthetic peptides and their use in cosmetic or dermopharmaceutical compositions |
US20100093643A1 (en) * | 2006-08-17 | 2010-04-15 | Irina Bobrova | Cardioprotective compounds |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4178371A (en) * | 1977-12-15 | 1979-12-11 | Reckitt & Colman Products Limited | Tetrapeptide derivatives |
US4288432A (en) * | 1979-06-12 | 1981-09-08 | Richter Gedeon Vegyeszeti Gyar Rt. | Novel enkephalin analogs and process for the preparation thereof |
US4265808A (en) * | 1979-12-17 | 1981-05-05 | Eli Lilly And Company | Pharmacologically active peptides |
US4322339A (en) * | 1980-10-20 | 1982-03-30 | Eli Lilly And Company | Pharmacologically active peptides |
-
1983
- 1983-05-26 GB GB838314646A patent/GB8314646D0/en active Pending
-
1984
- 1984-05-23 US US06/613,868 patent/US4540682A/en not_active Expired - Lifetime
- 1984-05-25 EP EP84105981A patent/EP0127154B1/en not_active Expired - Lifetime
- 1984-05-25 KR KR1019840002863A patent/KR850000467A/ko not_active Application Discontinuation
- 1984-05-25 AU AU28701/84A patent/AU575324B2/en not_active Ceased
- 1984-05-25 ZA ZA844004A patent/ZA844004B/xx unknown
- 1984-05-25 HU HU842048A patent/HU193569B/hu not_active IP Right Cessation
- 1984-05-25 JP JP59106325A patent/JPS59231053A/ja active Pending
- 1984-05-25 GR GR74826A patent/GR81890B/el unknown
- 1984-05-25 DE DE8484105981T patent/DE3483338D1/de not_active Expired - Fee Related
- 1984-05-25 AT AT84105981T patent/ATE57188T1/de not_active IP Right Cessation
- 1984-05-25 ES ES532813A patent/ES8606395A1/es not_active Expired
- 1984-05-25 DK DK258884A patent/DK258884A/da not_active Application Discontinuation
- 1984-05-25 FI FI842104A patent/FI82254C/fi not_active IP Right Cessation
- 1984-05-25 CA CA000455145A patent/CA1251898A/en not_active Expired
- 1984-05-25 IL IL71932A patent/IL71932A/xx unknown
- 1984-05-25 NZ NZ208283A patent/NZ208283A/xx unknown
-
1985
- 1985-07-15 ES ES545189A patent/ES8604991A1/es not_active Expired
Also Published As
Publication number | Publication date |
---|---|
EP0127154A2 (en) | 1984-12-05 |
ATE57188T1 (de) | 1990-10-15 |
EP0127154A3 (en) | 1987-05-06 |
GB8314646D0 (en) | 1983-06-29 |
GR81890B (ko) | 1984-12-12 |
NZ208283A (en) | 1988-07-28 |
AU2870184A (en) | 1984-11-29 |
ES8606395A1 (es) | 1986-04-01 |
CA1251898A (en) | 1989-03-28 |
IL71932A (en) | 1987-10-20 |
ES8604991A1 (es) | 1986-03-01 |
DK258884D0 (da) | 1984-05-25 |
EP0127154B1 (en) | 1990-10-03 |
US4540682A (en) | 1985-09-10 |
IL71932A0 (en) | 1984-09-30 |
ES545189A0 (es) | 1986-03-01 |
FI842104A (fi) | 1984-11-27 |
HU193569B (en) | 1987-10-28 |
DE3483338D1 (de) | 1990-11-08 |
HUT34764A (en) | 1985-04-28 |
FI842104A0 (fi) | 1984-05-25 |
AU575324B2 (en) | 1988-07-28 |
FI82254B (fi) | 1990-10-31 |
ES532813A0 (es) | 1986-04-01 |
ZA844004B (en) | 1986-01-29 |
FI82254C (fi) | 1991-02-11 |
DK258884A (da) | 1984-11-27 |
JPS59231053A (ja) | 1984-12-25 |
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