JP2001520662A - Lhrh−アンタゴニストの固定化及び活性安定化複合体及びその製法 - Google Patents
Lhrh−アンタゴニストの固定化及び活性安定化複合体及びその製法Info
- Publication number
- JP2001520662A JP2001520662A JP54481198A JP54481198A JP2001520662A JP 2001520662 A JP2001520662 A JP 2001520662A JP 54481198 A JP54481198 A JP 54481198A JP 54481198 A JP54481198 A JP 54481198A JP 2001520662 A JP2001520662 A JP 2001520662A
- Authority
- JP
- Japan
- Prior art keywords
- complex
- acid
- cetrorelix
- polyamino
- lhrh
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
- A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
- A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
- A61K47/645—Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Reproductive Health (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Molecular Biology (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1. LHRH−アンタゴニストとポリアミノ酸、殊にポリグルタミン酸及びポリ アスパラギン酸との新規複合体。 2. ポリアミノ酸の平均分子量が2000〜20000g/モルである、請求項 1に記載の複合体。 3. LHRHアンタゴニストとしてアンチド、アンタレリックス、アザリン、A −75998、ガニレリックス、Nal-Glu アンタゴニスト、しかし殊にはセトロレリ ックスが使用されている、請求項1及び2に記載の複合体。 4. 請求項1から3までのいずれか1項に記載のLHRHアンタゴニストとポリ アミノ酸、殊に平均分子量2000〜20000g/モルを有するポリグルタミ ン酸及びポリアスパラギン酸との複合体からなる、固定化され、かつ活性安定化 された非経口投与可能なペプチドホルモン製剤の製法において、ポリアミノ酸− ペプチドホルモン複合体を水溶液から沈殿させることを特徴とする、固定化され 、かつ活性安定化された非経口投与可能なペプチドホルモン製剤の製法。 5. 所望の制御可能なホルモン含有率を有するポリアミノ酸−ペプチドホルモン 複合体を水溶液の凍結乾燥により製造する、請求項4に記載の方法。 6. ポリマー骨格中に疎水性アミノ酸を導入するか、又は部分的なエステル化に より作用物質の放出を制御する、請求項4に記載の方法。 7. 請求項1から3までのいずれか1項に記載の化合物1種以上並びに場合によ り助剤及び骨格物質並びに安定剤を含有する、薬剤。 8. ホルモン感受性腫瘍の治療で、殊に、乳ガン、卵巣がん及び前立腺がん、良 性前立腺肥大の治療のために、受胎障害、子宮内膜症の治療のために、かつヒス テロスコピーと組み合わせて並びに試験管内受精のために使用される薬剤におい て、請求項1から3に記載の化合物を含有することを特徴とする、薬剤。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19712718.5 | 1997-03-26 | ||
DE19712718A DE19712718C2 (de) | 1997-03-26 | 1997-03-26 | Immobilisierte und aktivitätsstabilisierte Komplexe von LHRH-Antagonisten und Verfahren zu deren Herstellung |
PCT/EP1998/001398 WO1998042381A1 (de) | 1997-03-26 | 1998-03-11 | Immobilisierte und aktivitätsstabilisierte komplexe von lhrh-antagonisten und verfahren zu deren herstellung |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2001520662A true JP2001520662A (ja) | 2001-10-30 |
JP4180120B2 JP4180120B2 (ja) | 2008-11-12 |
Family
ID=7824698
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP54481198A Expired - Fee Related JP4180120B2 (ja) | 1997-03-26 | 1998-03-11 | Lhrh−アンタゴニストの固定化及び活性安定化複合体及びその製法 |
Country Status (27)
Country | Link |
---|---|
US (2) | US6022860A (ja) |
EP (1) | EP0981377B1 (ja) |
JP (1) | JP4180120B2 (ja) |
CN (1) | CN1150943C (ja) |
AR (1) | AR012186A1 (ja) |
AT (1) | ATE249245T1 (ja) |
AU (1) | AU747808B2 (ja) |
BR (1) | BR9807887B1 (ja) |
CA (1) | CA2285054C (ja) |
CZ (1) | CZ300755B6 (ja) |
DE (2) | DE19712718C2 (ja) |
DK (1) | DK0981377T3 (ja) |
ES (1) | ES2206912T3 (ja) |
HK (1) | HK1025255A1 (ja) |
HU (1) | HUP0002059A3 (ja) |
IL (1) | IL131181A (ja) |
NO (1) | NO327404B1 (ja) |
NZ (1) | NZ337343A (ja) |
PL (1) | PL190090B1 (ja) |
PT (1) | PT981377E (ja) |
RU (1) | RU2207151C2 (ja) |
SK (1) | SK284461B6 (ja) |
TR (1) | TR199902168T2 (ja) |
TW (1) | TW520288B (ja) |
UA (1) | UA69381C2 (ja) |
WO (1) | WO1998042381A1 (ja) |
ZA (1) | ZA982225B (ja) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2010110455A1 (ja) * | 2009-03-27 | 2010-09-30 | 国立大学法人 鹿児島大学 | 疎水化ポリアミノ酸からなるポリイオンコンプレックスとその用途 |
Families Citing this family (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6828415B2 (en) | 1993-02-19 | 2004-12-07 | Zentaris Gmbh | Oligopeptide lyophilisate, their preparation and use |
EP0788799A3 (en) | 1996-02-07 | 1998-10-21 | ASTA Medica Aktiengesellschaft | LHRH-Antagonists in the treatment of fertility disorders |
US20070185032A1 (en) * | 1996-12-11 | 2007-08-09 | Praecis Pharmaceuticals, Inc. | Pharmaceutical formulations for sustained drug delivery |
US5968895A (en) | 1996-12-11 | 1999-10-19 | Praecis Pharmaceuticals, Inc. | Pharmaceutical formulations for sustained drug delivery |
JP2002512975A (ja) * | 1998-04-23 | 2002-05-08 | アスタ メディカ アクチエンゲゼルシャフト | 受精能力障害の治療薬 |
CO5160256A1 (es) * | 1999-02-08 | 2002-05-30 | Zentaris Ag | Sales de peptidos farmaceuticamente activos para la liberacion sostenida y proceso de produccion |
DE10024451A1 (de) * | 2000-05-18 | 2001-11-29 | Asta Medica Ag | Pharmazeutische Darreichungsform für Peptide, Verfahren zu deren Herstellung und Verwendung |
AU2001289079A1 (en) | 2000-09-13 | 2002-03-26 | Praecis Pharmaceuticals Incorporated | Pharmaceutical compositions for sustained drug delivery |
US20020169125A1 (en) * | 2001-03-21 | 2002-11-14 | Cell Therapeutics, Inc. | Recombinant production of polyanionic polymers and uses thereof |
AU2002322493A1 (en) * | 2001-07-10 | 2003-01-29 | Ams Research Corporation | Surgical kit for treating prostate tissue |
US7214662B2 (en) | 2001-11-27 | 2007-05-08 | Zentaris Gmbh | Injectable solution of an LHRH antagonist |
US8093207B2 (en) * | 2005-12-09 | 2012-01-10 | Unigene Laboratories, Inc. | Fast-acting oral peptide pharmaceutical products |
WO2008083407A1 (en) | 2007-01-02 | 2008-07-10 | Aquabeam Llc | Minimally invasive methods and devices for the treatment of prostate diseases |
US9232959B2 (en) | 2007-01-02 | 2016-01-12 | Aquabeam, Llc | Multi fluid tissue resection methods and devices |
EP2259742B1 (en) | 2008-03-06 | 2020-01-01 | AquaBeam LLC | Tissue ablation and cautery with optical energy carried in fluid stream |
US9848904B2 (en) | 2009-03-06 | 2017-12-26 | Procept Biorobotics Corporation | Tissue resection and treatment with shedding pulses |
CN108606773B (zh) | 2012-02-29 | 2020-08-11 | 普罗赛普特生物机器人公司 | 自动化图像引导的组织切除和处理 |
JP6403695B2 (ja) | 2013-02-14 | 2018-10-10 | プロセプト バイオロボティクス コーポレイション | アクアアブレーションアクアビーム眼科手術方法および装置 |
JP6461971B2 (ja) | 2013-09-06 | 2019-01-30 | プロセプト バイオロボティクス コーポレイション | 飛散パルスを用いた組織切除および処置 |
BR112016031037B1 (pt) | 2014-06-30 | 2023-02-07 | Procept Biorobotics Corporation | Aparelho para ablação de tecido vascular |
CN107072591B (zh) | 2014-09-05 | 2021-10-26 | 普罗赛普特生物机器人公司 | 与靶器官图像的治疗映射结合的医师控制的组织切除 |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE257197C (ja) * | ||||
US4341767A (en) * | 1980-10-06 | 1982-07-27 | Syntex Inc. | Nonapeptide and decapeptide analogs of LHRH, useful as LHRH antagonists |
DD257197A1 (de) * | 1987-01-28 | 1988-06-08 | Univ Dresden Tech | Verfahren zur herstellung von immobilisierten, in ihrer biologischen aktivitaet stabilisierten und in ihren pharmakologischen eigenschaften modifizierten insulinpraeparationen |
US4801577A (en) * | 1987-02-05 | 1989-01-31 | Syntex (U.S.A.) Inc. | Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists |
DD269785A1 (de) * | 1988-02-08 | 1989-07-12 | Univ Dresden Tech | Verfahren zur herstellung von aktivitaetsstabilisierten und in ihren pharmakologischen eigenschaften modifizierten peptidderivaten |
DD273980B5 (de) * | 1988-07-12 | 1994-04-14 | Berlin Chemie Ag | Verfahren zur Herstellung von Insulin-Pr{paraten zur rektalen Anwendung |
DK0454044T3 (da) * | 1990-04-25 | 1996-04-22 | Hoechst Ag | Farmakologisk præparat indeholdende polyelektrolytkomplekser på mikropartikelform og mindst et virksomt stof |
DD299265A5 (de) * | 1990-09-11 | 1992-04-09 | Technische Universitaet Dresden,De | Verfahren zur herstellung von immobilisierten und aktivitaetsstabilisierten praeparaten des gonadotropin-releasing-hormons oder dessen analoga mit polyaminosaeuren |
US5834520A (en) * | 1992-10-08 | 1998-11-10 | Asta-Medica Aktiengesellschaft | Container for injectable mesna solutions |
AU5605894A (en) * | 1992-11-12 | 1994-06-08 | Molecular Dynamics, Inc. | Lipophilic peptide-based carriers for targeted drug delivery using rational drug-binding design |
DE4305225A1 (de) * | 1993-02-19 | 1994-08-25 | Asta Medica Ag | Neues Herstellverfahren für Cetrorelix Lyophilisat |
US5449720A (en) * | 1993-05-24 | 1995-09-12 | Biotech Australia Pty Limited | Amplification of the VB12 uptake system using polymers |
US5502035A (en) * | 1993-08-06 | 1996-03-26 | Tap Holdings Inc. | N-terminus modified analogs of LHRH |
CA2178592C (en) * | 1993-12-09 | 2009-07-28 | Jurgen Engel | Long-acting injection suspensions and a process for their preparation |
US5821230A (en) * | 1997-04-11 | 1998-10-13 | Ferring Bv | GnRH antagonist decapeptides |
-
1997
- 1997-03-26 DE DE19712718A patent/DE19712718C2/de not_active Expired - Fee Related
-
1998
- 1998-03-11 CZ CZ0337199A patent/CZ300755B6/cs not_active IP Right Cessation
- 1998-03-11 AT AT98914877T patent/ATE249245T1/de not_active IP Right Cessation
- 1998-03-11 TR TR1999/02168T patent/TR199902168T2/xx unknown
- 1998-03-11 IL IL13118198A patent/IL131181A/en not_active IP Right Cessation
- 1998-03-11 ES ES98914877T patent/ES2206912T3/es not_active Expired - Lifetime
- 1998-03-11 PT PT98914877T patent/PT981377E/pt unknown
- 1998-03-11 JP JP54481198A patent/JP4180120B2/ja not_active Expired - Fee Related
- 1998-03-11 CA CA002285054A patent/CA2285054C/en not_active Expired - Fee Related
- 1998-03-11 DE DE59809575T patent/DE59809575D1/de not_active Expired - Fee Related
- 1998-03-11 NZ NZ337343A patent/NZ337343A/en unknown
- 1998-03-11 AU AU69207/98A patent/AU747808B2/en not_active Ceased
- 1998-03-11 DK DK98914877T patent/DK0981377T3/da active
- 1998-03-11 SK SK1316-99A patent/SK284461B6/sk not_active IP Right Cessation
- 1998-03-11 RU RU99123056/14A patent/RU2207151C2/ru active
- 1998-03-11 CN CNB988031515A patent/CN1150943C/zh not_active Expired - Fee Related
- 1998-03-11 HU HU0002059A patent/HUP0002059A3/hu unknown
- 1998-03-11 EP EP98914877A patent/EP0981377B1/de not_active Expired - Lifetime
- 1998-03-11 WO PCT/EP1998/001398 patent/WO1998042381A1/de active IP Right Grant
- 1998-03-11 BR BRPI9807887-9A patent/BR9807887B1/pt not_active IP Right Cessation
- 1998-03-11 PL PL98335830A patent/PL190090B1/pl not_active IP Right Cessation
- 1998-03-17 ZA ZA9802225A patent/ZA982225B/xx unknown
- 1998-03-23 TW TW087104303A patent/TW520288B/zh not_active IP Right Cessation
- 1998-03-26 AR ARP980101397A patent/AR012186A1/es active IP Right Grant
- 1998-03-26 US US09/048,244 patent/US6022860A/en not_active Expired - Fee Related
- 1998-11-03 UA UA99105810A patent/UA69381C2/uk unknown
-
1999
- 1999-09-24 NO NO19994665A patent/NO327404B1/no not_active IP Right Cessation
- 1999-10-22 US US09/422,990 patent/US6054555A/en not_active Expired - Fee Related
-
2000
- 2000-07-24 HK HK00104545A patent/HK1025255A1/xx not_active IP Right Cessation
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2010110455A1 (ja) * | 2009-03-27 | 2010-09-30 | 国立大学法人 鹿児島大学 | 疎水化ポリアミノ酸からなるポリイオンコンプレックスとその用途 |
JP5522486B2 (ja) * | 2009-03-27 | 2014-06-18 | 国立大学法人 鹿児島大学 | 疎水化ポリアミノ酸からなるポリイオンコンプレックスとその用途 |
US8853354B2 (en) | 2009-03-27 | 2014-10-07 | Kagoshima University | Polyion complex comprising hydrophobized polyamino acid and use of the same |
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