KR920019817A - 초활성 grf 유사체 - Google Patents
초활성 grf 유사체 Download PDFInfo
- Publication number
- KR920019817A KR920019817A KR1019920006975A KR920006975A KR920019817A KR 920019817 A KR920019817 A KR 920019817A KR 1019920006975 A KR1019920006975 A KR 1019920006975A KR 920006975 A KR920006975 A KR 920006975A KR 920019817 A KR920019817 A KR 920019817A
- Authority
- KR
- South Korea
- Prior art keywords
- leu
- arg
- gln
- ser
- ala
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 claims abstract 13
- 150000001413 amino acids Chemical class 0.000 claims abstract 8
- 238000000034 method Methods 0.000 claims abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 2
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 7
- -1 hydroxy, nitro, amino, acetamido Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 108090000765 processed proteins & peptides Proteins 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 150000003018 phosphorus compounds Chemical class 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
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 125000003143 4-hydroxybenzyl group Chemical group [H]C([*])([H])C1=C([H])C([H])=C(O[H])C([H])=C1[H] 0.000 claims 1
- 125000000590 4-methylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 claims 1
- LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-norleucine Chemical compound CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- UKAUYVFTDYCKQA-UHFFFAOYSA-N homoserine Chemical compound OC(=O)C(N)CCO UKAUYVFTDYCKQA-UHFFFAOYSA-N 0.000 claims 1
- 150000002596 lactones Chemical class 0.000 claims 1
- TZFLUWBMBJLZQO-UHFFFAOYSA-N n-(6,7-difluoro-5-phenyl-1h-indazol-3-yl)butanamide Chemical compound C1=C2C(NC(=O)CCC)=NNC2=C(F)C(F)=C1C1=CC=CC=C1 TZFLUWBMBJLZQO-UHFFFAOYSA-N 0.000 claims 1
- 231100000252 nontoxic Toxicity 0.000 claims 1
- 230000003000 nontoxic effect Effects 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 125000000636 p-nitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)[N+]([O-])=O 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 102000038461 Growth Hormone-Releasing Hormone Human genes 0.000 abstract 8
- 101710142969 Somatoliberin Proteins 0.000 abstract 8
- 239000000095 Growth Hormone-Releasing Hormone Substances 0.000 abstract 6
- 102000018997 Growth Hormone Human genes 0.000 abstract 2
- 108010051696 Growth Hormone Proteins 0.000 abstract 2
- 239000000122 growth hormone Substances 0.000 abstract 2
- 241000283690 Bos taurus Species 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 238000012986 modification Methods 0.000 abstract 1
- 230000004048 modification Effects 0.000 abstract 1
- 210000003205 muscle Anatomy 0.000 abstract 1
- 230000001737 promoting effect Effects 0.000 abstract 1
- 241000894007 species Species 0.000 abstract 1
- 239000013612 plasmid Substances 0.000 description 3
Classifications
-
- 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
- C07K14/575—Hormones
- C07K14/60—Growth hormone-releasing factor [GH-RF], i.e. somatoliberin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
-
- 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
- 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)
- Life Sciences & Earth Sciences (AREA)
- Endocrinology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Gastroenterology & Hepatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Zoology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Reproductive Health (AREA)
- Toxicology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Oscillators With Electromechanical Resonators (AREA)
- Measurement Of Velocity Or Position Using Acoustic Or Ultrasonic Waves (AREA)
- Steering-Linkage Mechanisms And Four-Wheel Steering (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
- Farming Of Fish And Shellfish (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Electrotherapy Devices (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 플라스미드 pHS 190의 제한부위 및 작용 지도이고,
제2도는 플라스미드 pHS 500의 제한부위 및 작용 지도이고,
제3도는 플라스미드 pHS 452의 제한부위 및 작용 지도이다.
Claims (15)
- 하기 일반식(Ⅰ)의 화합물 및 그의 약학적으로 허용가능한 무독성 염 :Xl-Ala-Asp-Ala-Ile-Phe-Thr-Asn-A9-Tyr-Arg-A12-Val-Leu-Al5-Gln-Leu-Ser-Ala-Arg-A21-A22-Leu- (Ⅰ)Gln-A25-Ile-A27-A28-Arg-Y-Z-T상기식에서, A9는 Ser, Ala, Leu, Thr 또는 Asn이고, A12는 Arg 또는 Lys이며, A15는 Gly, Ala, Thr 또는 Leu이고, A21은 Arg 또는 Lys이며, A22는 Ala 또는 Leu이고, A25는 Asp 또는 Glu이며, A27는 Met, Ser, Arg, Leu 또는 노르류신이고, A28는 Ser 또는 Asn이며, Y는 없거나, 또는 1 내지 15개의 아미노산의 펩티드이고, Z는 없거나, 또는 1 내지 32개의 아미노산의 펩티드이며, T는 일반식 -COORa, -CRaO, -CONHNHRa, -CON(Ra)(Rb) 또는 CH2ORa의 카복실 말단 그룹이고, Ra 및 Rb는 독립적으로 저급알킬, 수소, Hse(락톤), HseOH 또는 HseN(Rc)(Rd)이고, Rc 및 Rd는 독립적으로 수소 또는 저급알킬이며, Xl은 일반식 의 아실그룹이고, R1은 수소, 메틸, 에틸, 하이드록시에틸, 페닐 ; 또는 할로, 저급 알킬, 저급 알콕시, 하이드록시, 니트로, 아미노, 아세트아미도, 트리플루오로메틸, -CH2-OH 또는 설프아미도에 의해 치환된 페닐 ; 또는 하나 이상의 N, O 또는 S를 함유하는 원 헤테로사이클이며, a는 0, 1, 2 또는 3이고, b는 0 또는 1이며, c는 0 또는 1이고, d는 내지 12이며, A는 없거나, 0 또는 S이고, B는 카보닐, 설포닐 및 설피닐이며, R2는 H, CH3, CH2OH, p-하이드록시벤질 또는이고, e는 0 내지 5이며, R3는 메틸, 에틸, 하이드록시에틸, 아미노, 하이드록실, 페닐 ; 또는 할로, 알킬, 알콕시, 하이드록시, 니트로, 아미노, 아세트아미도 또는 설프아미도에 의해 치환된 페닐 ; 또는 하나이상의 N, O 또는 S를 함유하는 5원 또는 6원 헤테로 사이클이다.
- 제1항에 있어서, a가 0이고, b가 1이며, B가 카보닐이고, c가 0이며, d가 0이고, A가 없는 화합물.
- 제2항에 있어서, R1이 메틸, 페닐, p-니트로페닐, p-클로로페닐, p-플루오로 페닐, p-하이드록시페닐, p-메틸페닐, N-벤질(이소니코티닐)로 이루어진 그룹에서 선택되는 화합물.
- 제3항에 있어서, R2가 H, CH3또는 CH2OH로 이루어진 그룹중에서 선택되는 화합물.
- 제3항에 있어서, R2가 H를 포함하는 화합물.
- 제1항 내지 제항중 어느 한 항에 있어서, A9가 Asn이고, A12가 Arg이며, A15가 Thr이고, A21이 Arg이며, A22가 Leu이고, A25가 Asp이며, A27이 Leu이고, A28이 Ser인 화합물.
- 제1항 내지 제6항 중 어느 한 항에 있어서, Y가 아미노산 서열 Gln-Gln-Gly-Glu-Arg-Asn-Gln-Glu-Gln-Gly-Ala-Arg-Val-Arg-Leu의 펩티드 또는 그의 작용성 유도체를 포함하는 화합물.
- 제1항 내지 제7항중 어느 한 항에 있어서, Z가 아미노산 서열 Gly-Arg-Gln-Val-Asp-Ser-Leu-Trp-Ala-Asp-Gln-Arg-Gln-Leu-Ala-Leu-Glu-Ser-Ile-Leu-Ala-Thr-Leu-Leu-Gln-Gln-His-Arg-Asn-Ser-Gln-Gly 또는 그의 작용성 유도체를 포함하는 화합물.
- 제1항 내지 제5항중 어느 한 항에 있어서, A9가 Ser이고, A12가 Arg이며, A15가 Thr이고, A21이 Arg이며, A22가 Leu이고, A25가 Asp이며, A28이 Asn인 화합물.
- 제9항에 있어서, Y가 아미노산 서열 Gln-Gln-Gly-Glu-Arg-Ans-Gln-Glu-Gln-Gly-Ala-Arg-Val-Arg-Leu- 또는 그의 작용성 유도체를 포함하는 화합물.
- 제10항에 있어서, Z가 아미노산 서열 Gly-Arg-Gln-Val-Asp-Gly-Val-Trp-Thr-Asp-Gln-Gln-Gln-Leu-Ala-Leu-Glu-Ser-Thr-Leu-Val-Ser-Leu-Leu-Gln-Glu-Arg-Asn-Ser-Gln-Gly을 포함하는 화합물.
- 제1항 내지 5항중 어느 한 항에 있어서, A9가 Ser이고, A12가 Lys이며, A15가 Gly이고, A21이 Lys이며, A22가 Leu이고, A25가 Asp이며, A25이 Met이고, A28이 Ser인 화합물.
- 제12항에 있어서, Y가 아미노산 서열 Glu-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu 또는 그의 작용성 유도체를 포함하는 화합물.
- 제13항에 있어서, Z가 없는 화합물.
- 활성 성분으로서 제1항 내지 제14항 중 어느 한 항에 청구된 GRF 유사체와 함께 하나 이상의 약학적으로 허용가능한 담체 부형제 또는 희석재를 포함하는 약학 제제.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US69209091A | 1991-04-26 | 1991-04-26 | |
| US7/692,090 | 1991-04-26 | ||
| US07/692,090 | 1991-04-26 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR920019817A true KR920019817A (ko) | 1992-11-20 |
| KR100233804B1 KR100233804B1 (ko) | 1999-12-01 |
Family
ID=24779221
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019920006975A KR100233804B1 (ko) | 1991-04-26 | 1992-04-24 | 초활성 grf 유사체 |
Country Status (24)
| Country | Link |
|---|---|
| EP (1) | EP0511003B1 (ko) |
| JP (1) | JPH05279388A (ko) |
| KR (1) | KR100233804B1 (ko) |
| CN (1) | CN1068123A (ko) |
| AT (1) | ATE178073T1 (ko) |
| AU (1) | AU1513292A (ko) |
| BR (1) | BR9201512A (ko) |
| CA (1) | CA2067304A1 (ko) |
| CZ (1) | CZ285567B6 (ko) |
| DE (1) | DE69228717T2 (ko) |
| DK (1) | DK0511003T3 (ko) |
| ES (1) | ES2129430T3 (ko) |
| FI (1) | FI921855A (ko) |
| GR (1) | GR3030459T3 (ko) |
| HU (1) | HUT64589A (ko) |
| IE (1) | IE921338A1 (ko) |
| IL (1) | IL101620A (ko) |
| MX (1) | MX9201878A (ko) |
| NO (1) | NO921595L (ko) |
| NZ (1) | NZ242459A (ko) |
| SG (1) | SG46364A1 (ko) |
| TW (1) | TW360661B (ko) |
| YU (1) | YU44292A (ko) |
| ZA (1) | ZA922746B (ko) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5453418A (en) * | 1988-03-07 | 1995-09-26 | Eli Lilly And Company | Ractopamine and growth hormone combinations |
| WO1994001451A2 (en) * | 1992-07-13 | 1994-01-20 | Bionebraska, Inc. | Method for modification of recombinant polypeptides |
| PT828758E (pt) * | 1995-05-26 | 2002-02-28 | Theratechnologies Inc | Analogos quimericos de corpo gordo-pro-grf com potencia biologica aumentada |
| EP0766966A3 (en) * | 1995-09-08 | 2001-02-28 | Eli Lilly And Company | Method of treating insulin resistance |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4628043A (en) * | 1983-04-26 | 1986-12-09 | The Salk Institute For Biological Studies | Hypothalamic GRF agonists |
| US4626523A (en) * | 1983-09-13 | 1986-12-02 | The Salk Institute For Biological Studies | GRF analogs II |
| US4528190A (en) * | 1983-10-25 | 1985-07-09 | The Salk Institute For Biological Studies | GRF Analogs IV |
| CA1271600A (en) * | 1985-01-07 | 1990-07-10 | David Howard Coy | Growth hormone-releasing peptides and method of treating mammals therewith |
-
1992
- 1992-04-14 ZA ZA922746A patent/ZA922746B/xx unknown
- 1992-04-16 IL IL10162092A patent/IL101620A/en not_active IP Right Cessation
- 1992-04-21 CZ CS921211A patent/CZ285567B6/cs not_active IP Right Cessation
- 1992-04-23 MX MX9201878A patent/MX9201878A/es unknown
- 1992-04-23 NZ NZ242459A patent/NZ242459A/en unknown
- 1992-04-24 IE IE133892A patent/IE921338A1/en unknown
- 1992-04-24 ES ES92303717T patent/ES2129430T3/es not_active Expired - Lifetime
- 1992-04-24 FI FI921855A patent/FI921855A/fi unknown
- 1992-04-24 YU YU44292A patent/YU44292A/sh unknown
- 1992-04-24 BR BR929201512A patent/BR9201512A/pt not_active Application Discontinuation
- 1992-04-24 DE DE69228717T patent/DE69228717T2/de not_active Expired - Fee Related
- 1992-04-24 JP JP4106569A patent/JPH05279388A/ja active Pending
- 1992-04-24 EP EP92303717A patent/EP0511003B1/en not_active Expired - Lifetime
- 1992-04-24 AT AT92303717T patent/ATE178073T1/de active
- 1992-04-24 NO NO92921595A patent/NO921595L/no unknown
- 1992-04-24 SG SG1996003583A patent/SG46364A1/en unknown
- 1992-04-24 CN CN92104215A patent/CN1068123A/zh active Pending
- 1992-04-24 KR KR1019920006975A patent/KR100233804B1/ko not_active IP Right Cessation
- 1992-04-24 AU AU15132/92A patent/AU1513292A/en not_active Abandoned
- 1992-04-24 DK DK92303717T patent/DK0511003T3/da active
- 1992-04-27 HU HU9201399A patent/HUT64589A/hu unknown
- 1992-04-27 CA CA002067304A patent/CA2067304A1/en not_active Abandoned
- 1992-05-14 TW TW081103757A patent/TW360661B/zh active
-
1999
- 1999-06-09 GR GR990401532T patent/GR3030459T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP0511003B1 (en) | 1999-03-24 |
| SG46364A1 (en) | 1998-02-20 |
| CS121192A3 (en) | 1992-11-18 |
| IL101620A0 (en) | 1992-12-30 |
| CN1068123A (zh) | 1993-01-20 |
| YU44292A (sh) | 1994-06-24 |
| HUT64589A (en) | 1994-01-28 |
| FI921855A (fi) | 1992-10-27 |
| DK0511003T3 (da) | 1999-05-25 |
| CA2067304A1 (en) | 1992-10-27 |
| IL101620A (en) | 1996-08-04 |
| TW360661B (en) | 1999-06-11 |
| ES2129430T3 (es) | 1999-06-16 |
| CZ285567B6 (cs) | 1999-09-15 |
| JPH05279388A (ja) | 1993-10-26 |
| ZA922746B (en) | 1992-12-30 |
| AU1513292A (en) | 1992-10-29 |
| GR3030459T3 (en) | 1999-10-29 |
| NO921595L (no) | 1992-10-27 |
| AU690264B2 (en) | 1998-04-23 |
| BR9201512A (pt) | 1992-12-01 |
| KR100233804B1 (ko) | 1999-12-01 |
| HU9201399D0 (en) | 1992-08-28 |
| NO921595D0 (no) | 1992-04-24 |
| IE921338A1 (en) | 1992-11-04 |
| ATE178073T1 (de) | 1999-04-15 |
| NZ242459A (en) | 1993-12-23 |
| DE69228717D1 (de) | 1999-04-29 |
| AU2333495A (en) | 1995-09-14 |
| DE69228717T2 (de) | 1999-08-19 |
| FI921855A0 (fi) | 1992-04-24 |
| MX9201878A (es) | 1992-10-01 |
| EP0511003A1 (en) | 1992-10-28 |
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