KR970706842A - 아실화된 인슐린 동족체(Acylated Insulin Analogs) - Google Patents
아실화된 인슐린 동족체(Acylated Insulin Analogs)Info
- Publication number
- KR970706842A KR970706842A KR1019970703179A KR19970703179A KR970706842A KR 970706842 A KR970706842 A KR 970706842A KR 1019970703179 A KR1019970703179 A KR 1019970703179A KR 19970703179 A KR19970703179 A KR 19970703179A KR 970706842 A KR970706842 A KR 970706842A
- Authority
- KR
- South Korea
- Prior art keywords
- insulin
- acylated
- homologue
- lys
- seq
- Prior art date
Links
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical class N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 title claims abstract 18
- 102000004877 Insulin Human genes 0.000 claims abstract 4
- 108090001061 Insulin Proteins 0.000 claims abstract 4
- 229940125396 insulin Drugs 0.000 claims abstract 4
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims abstract 2
- 206010012601 diabetes mellitus Diseases 0.000 claims abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 239000000872 buffer Substances 0.000 claims 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims 2
- 229930195729 fatty acid Natural products 0.000 claims 2
- 239000000194 fatty acid Substances 0.000 claims 2
- 150000004665 fatty acids Chemical class 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 239000007951 isotonicity adjuster Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 239000003755 preservative agent Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 101000976075 Homo sapiens Insulin Proteins 0.000 abstract 1
- 239000004472 Lysine Substances 0.000 abstract 1
- PBGKTOXHQIOBKM-FHFVDXKLSA-N insulin (human) Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CSSC[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3C=CC(O)=CC=3)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3NC=NC=3)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(=O)N[C@@H](CC(N)=O)C(O)=O)=O)CSSC[C@@H](C(N2)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)CC=1C=CC=CC=1)C(C)C)C1=CN=CN1 PBGKTOXHQIOBKM-FHFVDXKLSA-N 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/28—Insulins
-
- 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
- C07K14/62—Insulins
-
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal 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)
- Life Sciences & Earth Sciences (AREA)
- Diabetes (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Endocrinology (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Zoology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Toxicology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
Description
Claims (13)
- 서열 동정 번호 2에 적절하에 가교결합된 서열 동정 번호 1로 나타내어지는 일아실화된 인슐린 동족체, 또는 제약학적으로 허용가능한 그의 염.
- 제1항에 있어서, 서열 동정 번호 2의 28위치에서의 Xaa가 아실화된 라이신이고, 서열 동정 번호 2의 29위치에서의 Xaa가 프롤린인 아실화된 인슐린 동족체.
- 제2항에 있어서, 아실화기가 C6-C17지방산인 아실화된 인슐린 동족체.
- 제2항에 있어서, 아실화기가 C13-C17지방산인 아실화된 인슐린 동족체.
- B28-Nε-팔미토일-LysB28ProB29-사람 인슐린.
- B28-Nε-미리스토일-LysB28ProB29-사람 인슐린.
- 제1항 내지 6항 중 어느 한 항의 인슐린 동족체를 하나 이상의 제약학적으로 허용가능한 보존제, 등장화제 또는 완충제가 함께 포함하는 비경구 제약 제제.
- 인술린 또는 인슐린 동족체와 제1항 내지 7항 중 어느 한 항의 아실화된 인슐린 동족체와의 혼합물을 포함하고, 2가지 성분의 중량비가 약 1∼99 : 99∼1인 비경구 제약 제제.
- 제8항에 있어서, 혼합물이 LysB28ProB29-사람 인슐린과 B28-Nε-아실화된-LysB28ProB29-사람 인슐린의 혼합물인 비경구 제약 제제.
- 제1항 내지 7항 중 어느 한 항의 아실화된 인슐린 동족체의 유효량을 포함하는 제약 조성물을 환자에게 투여하는 것을 포함하는, 고혈당증 환자의 치료 방법.
- 제1항 내지 7항 중 어느 한 항의 화합물, 등장화제 및 생리적으로 허용되는 완충제를 혼합하는 것을 포함하는 비경구 제약 제제의 제조 방법.
- 당뇨병 치료에서 유용한 제1항 내지 7항 중 어느 한 항에 따른 아실화된 인슐린 동족체.
- 실질적으로 모든 실시예에 기재된 아실화된 인슐린 동족체.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/342,931 | 1994-11-17 | ||
US08/342,931 US5693609A (en) | 1994-11-17 | 1994-11-17 | Acylated insulin analogs |
Publications (1)
Publication Number | Publication Date |
---|---|
KR970706842A true KR970706842A (ko) | 1997-12-01 |
Family
ID=23343907
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019970703179A KR970706842A (ko) | 1994-11-17 | 1995-11-14 | 아실화된 인슐린 동족체(Acylated Insulin Analogs) |
Country Status (25)
Country | Link |
---|---|
US (2) | US5693609A (ko) |
EP (1) | EP0712861B1 (ko) |
JP (1) | JPH10511644A (ko) |
KR (1) | KR970706842A (ko) |
AR (1) | AR002700A1 (ko) |
AT (1) | ATE237635T1 (ko) |
AU (1) | AU711282B2 (ko) |
BR (1) | BR9509653A (ko) |
CA (1) | CA2205060A1 (ko) |
CO (1) | CO4520284A1 (ko) |
CZ (1) | CZ145797A3 (ko) |
DE (1) | DE69530353T2 (ko) |
ES (1) | ES2194890T3 (ko) |
FI (1) | FI972031L (ko) |
HU (1) | HUT77030A (ko) |
IL (1) | IL115973A (ko) |
NO (1) | NO972169L (ko) |
NZ (1) | NZ297257A (ko) |
PL (1) | PL320644A1 (ko) |
RU (1) | RU2160118C2 (ko) |
TR (1) | TR199501420A2 (ko) |
TW (1) | TW434259B (ko) |
WO (1) | WO1996015804A1 (ko) |
YU (1) | YU71395A (ko) |
ZA (1) | ZA959679B (ko) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20190102063A (ko) * | 2017-01-05 | 2019-09-02 | 코덱시스, 인코포레이티드 | 페니실린 g 아실라아제 |
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1995
- 1995-11-14 RU RU97110125/14A patent/RU2160118C2/ru active
- 1995-11-14 CZ CZ971457A patent/CZ145797A3/cs unknown
- 1995-11-14 ZA ZA959679A patent/ZA959679B/xx unknown
- 1995-11-14 PL PL95320644A patent/PL320644A1/xx unknown
- 1995-11-14 CO CO95053589A patent/CO4520284A1/es unknown
- 1995-11-14 WO PCT/US1995/014873 patent/WO1996015804A1/en not_active Application Discontinuation
- 1995-11-14 EP EP95308166A patent/EP0712861B1/en not_active Expired - Lifetime
- 1995-11-14 NZ NZ297257A patent/NZ297257A/xx unknown
- 1995-11-14 AT AT95308166T patent/ATE237635T1/de not_active IP Right Cessation
- 1995-11-14 ES ES95308166T patent/ES2194890T3/es not_active Expired - Lifetime
- 1995-11-14 AU AU42373/96A patent/AU711282B2/en not_active Ceased
- 1995-11-14 HU HU9701890A patent/HUT77030A/hu unknown
- 1995-11-14 CA CA002205060A patent/CA2205060A1/en not_active Abandoned
- 1995-11-14 YU YU71395A patent/YU71395A/sh unknown
- 1995-11-14 KR KR1019970703179A patent/KR970706842A/ko not_active Application Discontinuation
- 1995-11-14 TR TR95/01420A patent/TR199501420A2/xx unknown
- 1995-11-14 JP JP8516964A patent/JPH10511644A/ja not_active Ceased
- 1995-11-14 DE DE69530353T patent/DE69530353T2/de not_active Expired - Fee Related
- 1995-11-14 TW TW084112035A patent/TW434259B/zh active
- 1995-11-14 AR AR10016495A patent/AR002700A1/es not_active Application Discontinuation
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1997
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JPH10511644A (ja) | 1998-11-10 |
AU4237396A (en) | 1996-06-17 |
DE69530353D1 (de) | 2003-05-22 |
NZ297257A (en) | 1999-05-28 |
EP0712861A3 (en) | 1998-03-11 |
ES2194890T3 (es) | 2003-12-01 |
IL115973A (en) | 2001-08-26 |
US5693609A (en) | 1997-12-02 |
AU711282B2 (en) | 1999-10-07 |
PL320644A1 (en) | 1997-10-13 |
DE69530353T2 (de) | 2004-02-19 |
RU2160118C2 (ru) | 2000-12-10 |
FI972031L (fi) | 1997-05-14 |
YU71395A (sh) | 1998-07-10 |
CZ145797A3 (en) | 1997-12-17 |
TW434259B (en) | 2001-05-16 |
EP0712861B1 (en) | 2003-04-16 |
CA2205060A1 (en) | 1996-05-30 |
AR002700A1 (es) | 1998-04-29 |
BR9509653A (pt) | 1997-09-16 |
WO1996015804A1 (en) | 1996-05-30 |
TR199501420A2 (tr) | 1996-06-21 |
MX9703508A (es) | 1997-07-31 |
EP0712861A2 (en) | 1996-05-22 |
US5922675A (en) | 1999-07-13 |
HUT77030A (hu) | 1998-03-02 |
NO972169D0 (no) | 1997-05-12 |
ZA959679B (en) | 1997-05-14 |
FI972031A0 (fi) | 1997-05-13 |
NO972169L (no) | 1997-05-12 |
ATE237635T1 (de) | 2003-05-15 |
IL115973A0 (en) | 1996-01-31 |
CO4520284A1 (es) | 1997-10-15 |
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