KR927003630A - 황산 에스테르기를 갖는 헥사펩티드 - Google Patents
황산 에스테르기를 갖는 헥사펩티드 Download PDFInfo
- Publication number
- KR927003630A KR927003630A KR1019920701235A KR920701235A KR927003630A KR 927003630 A KR927003630 A KR 927003630A KR 1019920701235 A KR1019920701235 A KR 1019920701235A KR 920701235 A KR920701235 A KR 920701235A KR 927003630 A KR927003630 A KR 927003630A
- Authority
- KR
- South Korea
- Prior art keywords
- compound
- formula
- pharmaceutically acceptable
- met
- acceptable salt
- Prior art date
Links
- QAOWNCQODCNURD-UHFFFAOYSA-N sulfuric acid Substances OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000006239 protecting group Chemical group 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000003295 alanine group Chemical group N[C@@H](C)C(=O)* 0.000 claims 4
- XJODGRWDFZVTKW-LURJTMIESA-N (2s)-4-methyl-2-(methylamino)pentanoic acid Chemical compound CN[C@H](C(O)=O)CC(C)C XJODGRWDFZVTKW-LURJTMIESA-N 0.000 claims 2
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims 2
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 2
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 2
- 125000000174 L-prolyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(*)=O 0.000 claims 2
- KSPIYJQBLVDRRI-WDSKDSINSA-N N-methyl-L-isoleucine Chemical compound CC[C@H](C)[C@H](NC)C(O)=O KSPIYJQBLVDRRI-WDSKDSINSA-N 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000000030 D-alanine group Chemical group [H]N([H])[C@](C([H])([H])[H])(C(=O)[*])[H] 0.000 claims 1
- QNAYBMKLOCPYGJ-UHFFFAOYSA-N D-alpha-Ala Natural products CC([NH3+])C([O-])=O QNAYBMKLOCPYGJ-UHFFFAOYSA-N 0.000 claims 1
- 125000002237 D-aspartyl group Chemical group [H]OC(=O)[C@]([H])(N([H])[H])C([H])([H])C(*)=O 0.000 claims 1
- 125000000296 D-methionine group Chemical group [H]N([H])[C@@]([H])(C(=O)[*])C([H])([H])C([H])([H])SC([H])([H])[H] 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 1
- UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
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
- C07K14/595—Gastrins; Cholecystokinins [CCK]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- 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
- C07K14/595—Gastrins; Cholecystokinins [CCK]
- C07K14/5955—Gastrins; Cholecystokinins [CCK] at least 1 amino acid in D-form
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Gastroenterology & Hepatology (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Zoology (AREA)
- Toxicology (AREA)
- Endocrinology (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Obesity (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Breeding Of Plants And Reproduction By Means Of Culturing (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Led Devices (AREA)
- Hydroponics (AREA)
- Footwear And Its Accessory, Manufacturing Method And Apparatuses (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Abstract
내용 없음
Description
황산 에스테르기를 갖는 헥사펩티드
[도면의 간단한 설명]
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (10)
- 하기 일반식(I)의 화합물 및 그의 제약상 허용되는 염.상기 식 중, M은 Met. DMet, MeMet, MetO, Ahx, DAhx, MeAhx, Leu, MeLeu, Pro, Ile, MeIle, Ala 또는 Lys이고;G는 Gly, DAla, Pro, A1la, βAla 또는 Sar이며:w는 Trp, MeTrp, Ala 또는 Nal 이고:X는Met, MeMet, MetO, Ahx, MeAhx, Leu, MeLeu, Pro, Ile, MeIle, Ala 또는 Lys이며;J는 Asp, DAsp,MeAsp, Ala 또는 Asn이고;F1은 (S)-NH (R)-NH (S)-R1N 또는 (R)-R2N이며; F1는 H, Cl, I, Br, F, NO2, NH2, R3또는 OR4이고; Z는 NH2, NHR5또는 NR5R6이며; R1, R2, R3, R5및 R6은 탄소수 1 내지 6의 알킬이고; R4는 H 또는 탄소수 1 내지 6의 알킬이다.
- 제1항에 있어서, M이 Met, Ahx, Leu, Ala 또는 Ile인 화합물.
- 제1 또는 2항에 있어서, X가 Met, Ahx, Leu 또는 Ile인 화합물.
- 제1 내지 3항중 어느 한 항에 있어서, F1이 (S)-NH 또는 (S)-R2N인 화합물.
- 제1 내지 4항중 어느 한 항에 있어서, Z가 NH2인 화합뭍·
- 제1항에 있어서, 일반식 (I) 의 화합이 Hpa(SO3H)-Met-Gly-Trp-Met-Asp-MePhe-NH3인 화합물 또는 그의 제약성 허용되는 염.
- 제1항에 있어서, 일반식(I)의 화합물이 T1-1 인 화합물 또는 그의 제약상 허용되는 염.
- 제1항에 정의된 일반식(I)의 화합물 또는 그의 제약상 허용되는 염을 제약상 허용되는 담체와의 혼합물로 함유하는 제약 조성물.
- 제1항에 정의된 일반식(I)의 화합물 또는 그의 제약상 허용되는 염의 비만증의 치료 또는 예방을 위한 의약 제조 용도.
- a) 하기 일반식(II)의 화합물을 황산화시키고[상기 식 중, M, G, W, X, J, Fl,, F2및 Z는 상기 정의한 바와 같고, P1은 M 또는 X가 Lys인 경우 아미노 보호기이며, Pa는 J가 Asp, D-Asp 또는 Me-Asp인 경우 카르복실 보호기이고, Pn은 F2가 NH2또는 OH인 경우 히드록실 보호기 또는 아미노 보호기이며, Pc는 Z 또는 카르복실 보호기이다], b) 하기 일반식(III)의 대응하는 화합물로부터 1개 이상의 보호기를 제거하고[상기 식 중, M, G, W, X, J, Fl, F2P1, Pa, Pn 및 Pc는 상기 정의한 바와 같고, 단, P1, Pa, Pn 및 Pc중의 적어도 하나는 보호기이다], 필요시, 생성된 일반식(I)의 화합물을 그의 제약상 허용되는 염으로 전환시키거나 또는 그 역으로 전환시키는 것으로 이루어진, 제1항에 정의된 일반식(I)의 화합물의 제조 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US44127589A | 1989-11-27 | 1989-11-27 | |
| US441,275 | 1989-11-27 | ||
| PCT/US1990/006739 WO1991008225A1 (en) | 1989-11-27 | 1990-11-16 | Hexapeptides with sulphate ester groups |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR927003630A true KR927003630A (ko) | 1992-12-18 |
Family
ID=23752246
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019920701235A KR927003630A (ko) | 1989-11-27 | 1990-11-16 | 황산 에스테르기를 갖는 헥사펩티드 |
Country Status (19)
| Country | Link |
|---|---|
| EP (1) | EP0495013B1 (ko) |
| JP (1) | JPH05500962A (ko) |
| KR (1) | KR927003630A (ko) |
| AT (1) | ATE119544T1 (ko) |
| AU (1) | AU644128B2 (ko) |
| CA (1) | CA2030720A1 (ko) |
| DE (1) | DE69017704T2 (ko) |
| DK (1) | DK0495013T3 (ko) |
| ES (1) | ES2069272T3 (ko) |
| FI (1) | FI922404A0 (ko) |
| HU (2) | HU00168A9 (ko) |
| IE (1) | IE66837B1 (ko) |
| IL (1) | IL96465A (ko) |
| LV (1) | LV11623A (ko) |
| NO (1) | NO922094L (ko) |
| NZ (1) | NZ236167A (ko) |
| PT (1) | PT95996B (ko) |
| WO (1) | WO1991008225A1 (ko) |
| ZA (1) | ZA909415B (ko) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5502164A (en) * | 1989-11-27 | 1996-03-26 | Fisons Corporation | Peptide compounds having therapeutic activity |
| IL104161A0 (en) * | 1991-12-20 | 1993-05-13 | Fisons Corp | Peptide compounds,their preparation and pharmaceutical compositions containing them |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR6915336D0 (pt) * | 1969-05-27 | 1973-03-13 | Squibb & Sons Inc | Reptidios contendo tirosina-o-sulfato |
| DD128973B1 (de) * | 1976-11-29 | 1979-11-28 | Hartmut Niedrich | Verfahren zur herstellung von peptiden,die tyrosinsulfat enthalten |
| US4217353A (en) * | 1978-05-19 | 1980-08-12 | E. I. Du Pont De Nemours And Company | Method for inducing anorexia |
| US5086042A (en) * | 1985-12-19 | 1992-02-04 | Fisons Corporation | Peptides with sulfate ester groups |
| NZ218607A (en) * | 1985-12-19 | 1989-10-27 | Pennwalt Corp | Tri-to acta-peptides with sulphate ester groups: obesity treatment |
| IL84478A0 (en) * | 1986-11-18 | 1988-04-29 | Pennwalt Corp | Peptides with sulfate ester groups and their preparation |
| US4808701A (en) * | 1987-03-30 | 1989-02-28 | Hoffmann-La Roche Inc. | Cyclic peptides having appetite regulating activity |
-
1990
- 1990-11-16 KR KR1019920701235A patent/KR927003630A/ko not_active Application Discontinuation
- 1990-11-16 AU AU69644/91A patent/AU644128B2/en not_active Ceased
- 1990-11-16 WO PCT/US1990/006739 patent/WO1991008225A1/en active IP Right Grant
- 1990-11-16 DE DE69017704T patent/DE69017704T2/de not_active Expired - Fee Related
- 1990-11-16 DK DK91901058.7T patent/DK0495013T3/da active
- 1990-11-16 EP EP91901058A patent/EP0495013B1/en not_active Expired - Lifetime
- 1990-11-16 JP JP3501490A patent/JPH05500962A/ja active Pending
- 1990-11-16 AT AT91901058T patent/ATE119544T1/de not_active IP Right Cessation
- 1990-11-16 ES ES91901058T patent/ES2069272T3/es not_active Expired - Lifetime
- 1990-11-20 NZ NZ236167A patent/NZ236167A/en unknown
- 1990-11-23 ZA ZA909415A patent/ZA909415B/xx unknown
- 1990-11-23 CA CA002030720A patent/CA2030720A1/en not_active Abandoned
- 1990-11-23 IE IE423990A patent/IE66837B1/en not_active IP Right Cessation
- 1990-11-26 IL IL9646590A patent/IL96465A/en not_active IP Right Cessation
- 1990-11-26 PT PT95996A patent/PT95996B/pt not_active IP Right Cessation
-
1992
- 1992-05-26 NO NO92922094A patent/NO922094L/no unknown
- 1992-05-26 FI FI922404A patent/FI922404A0/fi not_active Application Discontinuation
-
1995
- 1995-06-07 HU HU95P/P00168P patent/HU00168A9/hu unknown
- 1995-06-12 HU HU95P/P00189P patent/HU211694A9/hu unknown
-
1996
- 1996-03-07 LV LV960068A patent/LV11623A/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| DE69017704T2 (de) | 1995-07-20 |
| NO922094L (no) | 1992-07-08 |
| AU6964491A (en) | 1991-06-26 |
| NO922094D0 (no) | 1992-05-26 |
| FI922404A (fi) | 1992-05-26 |
| ZA909415B (en) | 1991-11-27 |
| AU644128B2 (en) | 1993-12-02 |
| EP0495013A1 (en) | 1992-07-22 |
| PT95996A (pt) | 1991-09-13 |
| DK0495013T3 (da) | 1995-07-24 |
| IL96465A (en) | 1994-12-29 |
| FI922404A0 (fi) | 1992-05-26 |
| HU00168A9 (en) | 1995-07-28 |
| WO1991008225A1 (en) | 1991-06-13 |
| LV11623A (lv) | 1996-12-20 |
| JPH05500962A (ja) | 1993-02-25 |
| ES2069272T3 (es) | 1995-05-01 |
| IL96465A0 (en) | 1991-08-16 |
| DE69017704D1 (de) | 1995-04-13 |
| NZ236167A (en) | 1991-12-23 |
| EP0495013B1 (en) | 1995-03-08 |
| IE66837B1 (en) | 1996-02-07 |
| HU211694A9 (en) | 1995-12-28 |
| IE904239A1 (en) | 1991-06-05 |
| PT95996B (pt) | 1998-01-30 |
| ATE119544T1 (de) | 1995-03-15 |
| CA2030720A1 (en) | 1991-05-28 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A201 | Request for examination | ||
| N231 | Notification of change of applicant | ||
| E902 | Notification of reason for refusal | ||
| E601 | Decision to refuse application |