KR920004417A - 고나돌리베린 길항물질 - Google Patents
고나돌리베린 길항물질 Download PDFInfo
- Publication number
- KR920004417A KR920004417A KR1019910013368A KR910013368A KR920004417A KR 920004417 A KR920004417 A KR 920004417A KR 1019910013368 A KR1019910013368 A KR 1019910013368A KR 910013368 A KR910013368 A KR 910013368A KR 920004417 A KR920004417 A KR 920004417A
- Authority
- KR
- South Korea
- Prior art keywords
- phe
- peptide
- formula
- physiologically acceptable
- trp
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 5
- COLNVLDHVKWLRT-MRVPVSSYSA-N D-phenylalanine Chemical compound OC(=O)[C@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-MRVPVSSYSA-N 0.000 claims 4
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 3
- QIVBCDIJIAJPQS-SECBINFHSA-N D-tryptophane Chemical compound C1=CC=C2C(C[C@@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-SECBINFHSA-N 0.000 claims 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 3
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 3
- 229910052794 bromium Inorganic materials 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000000734 D-serino group Chemical group [H]N([H])[C@@]([H])(C(=O)[*])C(O[H])([H])[H] 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000001246 bromo group Chemical group Br* 0.000 claims 2
- 239000012634 fragment Substances 0.000 claims 2
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- 125000001711 D-phenylalanine group Chemical group [H]N([H])[C@@]([H])(C(=O)[*])C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 102000006771 Gonadotropins Human genes 0.000 claims 1
- 108010086677 Gonadotropins Proteins 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 230000005494 condensation Effects 0.000 claims 1
- 238000009833 condensation Methods 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 239000002622 gonadotropin Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000003755 preservative agent Substances 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 229940063296 testosterone and estrogen Drugs 0.000 claims 1
Classifications
-
- 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
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- 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
- C07K7/23—Luteinising hormone-releasing hormone [LHRH]; Related peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Endocrinology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (7)
- 일반식(I)의 펩타이드 또는 이의 생리학적으로 허용되는 염.1 2 3 4 5 6 7 8 9 10X - A - B - C - Ser - D - E - F - G - Pro - H (I)상기식에서, X는 C2-C8-알카노일이고;A는 D-Nal(2), D-Phe 또는 D-Trp(여기서 방향족 환은 브롬, 염소, 불소, 니트로, C1-C4-알킬 및 C1-C4-알콕시 중에서 선택된 동일하거나 상이한 라디칼 1 또는 2개로 임의 치환될 수 있다)이며;B는 브롬, 염소, 불소, 니트로, C1-C4-알킬 및 C1-C4-알콕시 중에서 선택된 동일하거나 상이한 라디칼 1 또는 2개로 임의 치환될 수 있는 D- Phe이고;C는 D-Pal(3), D-Phe 또는 D-Phe(여기서 D-Phe 및 D-Trp의 방향족 환은 브롬,염소, 불소, 니트로, C1-C4-알킬 및 C1-C4-알콕시 중에서 선택된 동일하거나 상이한 라디칼 1 또는 2개로 임의 치환될 수 있다)이며;D는 Tyr 또는 His이고; E는 D-Ser(R')이며;F는 Leu, Trp또는 Phe이고;G는 L-Ser(R')이며;H는 Gly-NH2, D-Ale-NH2또는 Azagly-NH2이고;R'은 글리코실 라디칼이다.
- 제1항에 있어서, X가 아세틸이고;A가 D-Nal(2)이며;B가 D-Phe(pC1)이고;C가 D-Pha(3) 또는 D-Trp이며;E가 D-Ser(R')이고;F는 Leu 이며; G가 D-Ale-NH2또는 Azagly-NH2인 일반식(I)의 펩타이드 및 이의 생리학적으로 허용되는 염
- N-말단 자유 아미노 그룹을 갖는 단편을 C-말단 자유 카복실 그룹을 갖는 단편과 축합시키고, 작용기는 보호하기 위하여 일시적으로 도입시킬 수 있는 하나 이상의 보호 그룹을 제거한 다음, 경우에 따라 상기 방법으로 수득한 펩타이드를 이의 생리학적으로 허용되는 염으로 전환시킴을 특징으로 하여, 제1항 또는 2항에서 청구된 바와 같은 일반식(I)의 펩타이드를 제조하는 방법.
- 약물로서 사용하기 위한, 제1항 또는 2항에 청구된 바와 같은 일반식(I)의 펩타이드.
- 혈장 고나도트로핀, 테스토스테론 및 에스트로겐 저하제로서, 제1항 또는 2항에 청구된 바와 같은 일반식(I)의 펩타이드의 용도.
- 제1항 또는 2항에 청구된 바와 같은 일반식(I)의 펩타이드 또는 이의 생리학적으로 허용되는 염을 함유하는 약제학적 조성물.
- 일반식(I)의 펩타이드 또는 이의 생리학적으로 허용되는 염을 생리학적으로 허용되는 부형제 및 경우에 따라, 다른 첨가제, 보조제 및/또는 방부제와 함께 적합한 투여형으로 전환시킴을 특징으로 하여, 제6항에 청구된 바와 같은 조성물을 제조하는 방법.※ 참고사항 : 최초출원 내용에 의하여 공개되는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4024779 | 1990-08-04 | ||
| DEP4024779.1 | 1990-08-04 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR920004417A true KR920004417A (ko) | 1992-03-27 |
| KR100191700B1 KR100191700B1 (ko) | 1999-06-15 |
Family
ID=6411646
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019910013368A KR100191700B1 (ko) | 1990-08-04 | 1991-08-02 | 고나돌리베린 길항물질 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US5434138A (ko) |
| EP (1) | EP0477499B1 (ko) |
| JP (1) | JP3164844B2 (ko) |
| KR (1) | KR100191700B1 (ko) |
| AT (1) | ATE100822T1 (ko) |
| AU (1) | AU641035B2 (ko) |
| CA (1) | CA2048407C (ko) |
| DE (1) | DE59100945D1 (ko) |
| DK (1) | DK0477499T3 (ko) |
| ES (1) | ES2062628T3 (ko) |
| IE (1) | IE65965B1 (ko) |
| IL (1) | IL99062A (ko) |
| NO (1) | NO309429B1 (ko) |
| NZ (1) | NZ239233A (ko) |
| PT (1) | PT98533B (ko) |
| TW (1) | TW205046B (ko) |
| ZA (1) | ZA916097B (ko) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5691314A (en) * | 1996-03-18 | 1997-11-25 | The Medical College Of Hampton Roads | Adjunctive therapy |
| CN1301771A (zh) * | 1999-12-27 | 2001-07-04 | 上海博德基因开发有限公司 | 一种新的多肽——人促性腺释放激素11和编码这种多肽的多核苷酸 |
| US11805833B1 (en) * | 2019-05-10 | 2023-11-07 | Julie Vahos | Flexible hair extension with form retention capability |
| WO2023101490A1 (ko) * | 2021-12-01 | 2023-06-08 | 애니젠 주식회사 | 가니렐릭스의 신규한 제조방법 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS54148722A (en) * | 1978-05-12 | 1979-11-21 | Takeda Chem Ind Ltd | Nonapeptide and its preparation |
| US5073624A (en) * | 1985-04-09 | 1991-12-17 | Administrators Of The Tulane Educational Fund | Therapeutic decapeptides |
| US4661472A (en) * | 1985-05-09 | 1987-04-28 | The Salk Institute For Biological Studies | GnRH antagonists IX |
| DE3634435A1 (de) * | 1986-10-09 | 1988-04-14 | Hoechst Ag | Analoga von gonadoliberin mit verbesserter loeslichkeit, verfahren zu deren herstellung, diese enthaltende mittel und ihre verwendung |
| US4801577A (en) * | 1987-02-05 | 1989-01-31 | Syntex (U.S.A.) Inc. | Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists |
| US5110904A (en) * | 1989-08-07 | 1992-05-05 | Abbott Laboratories | Lhrh analogs |
| GB2218102B (en) * | 1988-04-08 | 1992-09-16 | Sandoz Ltd | Calcitonin peptide derivatives |
-
1991
- 1991-07-30 DE DE91112817T patent/DE59100945D1/de not_active Expired - Fee Related
- 1991-07-30 EP EP91112817A patent/EP0477499B1/de not_active Expired - Lifetime
- 1991-07-30 ES ES91112817T patent/ES2062628T3/es not_active Expired - Lifetime
- 1991-07-30 DK DK91112817.1T patent/DK0477499T3/da active
- 1991-07-30 AT AT91112817T patent/ATE100822T1/de not_active IP Right Cessation
- 1991-08-01 PT PT98533A patent/PT98533B/pt not_active IP Right Cessation
- 1991-08-02 KR KR1019910013368A patent/KR100191700B1/ko not_active IP Right Cessation
- 1991-08-02 NO NO913020A patent/NO309429B1/no unknown
- 1991-08-02 IE IE276991A patent/IE65965B1/en not_active IP Right Cessation
- 1991-08-02 AU AU81548/91A patent/AU641035B2/en not_active Ceased
- 1991-08-02 NZ NZ239233A patent/NZ239233A/xx unknown
- 1991-08-02 CA CA002048407A patent/CA2048407C/en not_active Expired - Fee Related
- 1991-08-02 ZA ZA916097A patent/ZA916097B/xx unknown
- 1991-08-02 IL IL9906291A patent/IL99062A/en not_active IP Right Cessation
- 1991-08-05 JP JP21913991A patent/JP3164844B2/ja not_active Expired - Fee Related
- 1991-08-06 TW TW080106149A patent/TW205046B/zh active
-
1993
- 1993-11-12 US US08/151,056 patent/US5434138A/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| IL99062A (en) | 1995-07-31 |
| ATE100822T1 (de) | 1994-02-15 |
| JP3164844B2 (ja) | 2001-05-14 |
| DE59100945D1 (de) | 1994-03-10 |
| NZ239233A (en) | 1993-09-27 |
| PT98533A (pt) | 1992-06-30 |
| IE912769A1 (en) | 1992-02-12 |
| ES2062628T3 (es) | 1994-12-16 |
| DK0477499T3 (da) | 1994-05-30 |
| CA2048407A1 (en) | 1992-02-05 |
| ZA916097B (en) | 1992-04-29 |
| NO913020L (no) | 1992-02-05 |
| EP0477499A1 (de) | 1992-04-01 |
| IE65965B1 (en) | 1995-11-29 |
| IL99062A0 (en) | 1992-07-15 |
| AU8154891A (en) | 1992-02-06 |
| TW205046B (ko) | 1993-05-01 |
| PT98533B (pt) | 1999-01-29 |
| US5434138A (en) | 1995-07-18 |
| NO309429B1 (no) | 2001-01-29 |
| KR100191700B1 (ko) | 1999-06-15 |
| JPH05148299A (ja) | 1993-06-15 |
| EP0477499B1 (de) | 1994-01-26 |
| CA2048407C (en) | 2001-10-23 |
| AU641035B2 (en) | 1993-09-09 |
| NO913020D0 (no) | 1991-08-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A201 | Request for examination | ||
| E701 | Decision to grant or registration of patent right | ||
| GRNT | Written decision to grant | ||
| FPAY | Annual fee payment |
Payment date: 20011229 Year of fee payment: 4 |
|
| LAPS | Lapse due to unpaid annual fee |