ZA200107753B - Novel LHRH antagonists with improved solubility characteristics. - Google Patents
Novel LHRH antagonists with improved solubility characteristics. Download PDFInfo
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- ZA200107753B ZA200107753B ZA200107753A ZA200107753A ZA200107753B ZA 200107753 B ZA200107753 B ZA 200107753B ZA 200107753 A ZA200107753 A ZA 200107753A ZA 200107753 A ZA200107753 A ZA 200107753A ZA 200107753 B ZA200107753 B ZA 200107753B
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- XLXSAKCOAKORKW-UHFFFAOYSA-N gonadorelin Chemical compound C1CCC(C(=O)NCC(N)=O)N1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)CNC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 XLXSAKCOAKORKW-UHFFFAOYSA-N 0.000 description 1
- 229960001442 gonadorelin Drugs 0.000 description 1
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 description 1
- 238000005984 hydrogenation reaction Methods 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 239000012442 inert solvent Substances 0.000 description 1
- 125000003588 lysine group Chemical group [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- WOOWBQQQJXZGIE-UHFFFAOYSA-N n-ethyl-n-propan-2-ylpropan-2-amine Chemical compound CCN(C(C)C)C(C)C.CCN(C(C)C)C(C)C WOOWBQQQJXZGIE-UHFFFAOYSA-N 0.000 description 1
- FEMOMIGRRWSMCU-UHFFFAOYSA-N ninhydrin Chemical compound C1=CC=C2C(=O)C(O)(O)C(=O)C2=C1 FEMOMIGRRWSMCU-UHFFFAOYSA-N 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920002223 polystyrene Polymers 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 230000006340 racemization Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 229940043230 sarcosine Drugs 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- UGNWTBMOAKPKBL-UHFFFAOYSA-N tetrachloro-1,4-benzoquinone Chemical compound ClC1=C(Cl)C(=O)C(Cl)=C(Cl)C1=O UGNWTBMOAKPKBL-UHFFFAOYSA-N 0.000 description 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- JPZXHKDZASGCLU-LBPRGKRZSA-N β-(2-naphthyl)-alanine Chemical compound C1=CC=CC2=CC(C[C@H](N)C(O)=O)=CC=C21 JPZXHKDZASGCLU-LBPRGKRZSA-N 0.000 description 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
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/10—Peptides having 12 to 20 amino acids
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
- A61P5/04—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
-
- 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
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Endocrinology (AREA)
- Biophysics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19911771A DE19911771B4 (de) | 1999-03-17 | 1999-03-17 | LHRH-Antagonist, Verfahren zu seiner Herstellung und seiner Verwendung |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200107753B true ZA200107753B (en) | 2002-05-13 |
Family
ID=7901213
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200107753A ZA200107753B (en) | 1999-03-17 | 2001-09-19 | Novel LHRH antagonists with improved solubility characteristics. |
Country Status (33)
| Country | Link |
|---|---|
| US (3) | US6627609B1 (cs) |
| EP (1) | EP1163264B1 (cs) |
| JP (1) | JP3801867B2 (cs) |
| KR (1) | KR100569623B1 (cs) |
| CN (1) | CN1185251C (cs) |
| AR (1) | AR022970A1 (cs) |
| AT (1) | ATE277077T1 (cs) |
| AU (1) | AU759442B2 (cs) |
| BG (1) | BG65283B1 (cs) |
| BR (1) | BR0009472A (cs) |
| CA (1) | CA2381461C (cs) |
| CO (1) | CO5150192A1 (cs) |
| CZ (1) | CZ301696B6 (cs) |
| DE (2) | DE19911771B4 (cs) |
| DK (1) | DK1163264T3 (cs) |
| ES (1) | ES2225103T3 (cs) |
| HK (1) | HK1045531B (cs) |
| HU (1) | HU229672B1 (cs) |
| IL (3) | IL145484A0 (cs) |
| MX (1) | MXPA01010052A (cs) |
| NO (1) | NO327753B1 (cs) |
| NZ (1) | NZ514830A (cs) |
| PL (1) | PL200647B1 (cs) |
| PT (1) | PT1163264E (cs) |
| RU (1) | RU2227145C2 (cs) |
| SI (2) | SI1163264T1 (cs) |
| SK (1) | SK287880B6 (cs) |
| TR (1) | TR200103339T2 (cs) |
| TW (1) | TWI243179B (cs) |
| UA (1) | UA70997C2 (cs) |
| WO (1) | WO2000055190A1 (cs) |
| YU (1) | YU68702A (cs) |
| ZA (1) | ZA200107753B (cs) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6828415B2 (en) * | 1993-02-19 | 2004-12-07 | Zentaris Gmbh | Oligopeptide lyophilisate, their preparation and use |
| US5677184A (en) * | 1994-04-19 | 1997-10-14 | Takeda Chemical Industries, Ltd. | CHO cells that express human LH-RH receptor |
| DE19911771B4 (de) * | 1999-03-17 | 2006-03-30 | Zentaris Gmbh | LHRH-Antagonist, Verfahren zu seiner Herstellung und seiner Verwendung |
| EP1268522B1 (de) | 2000-03-14 | 2008-09-17 | AEterna Zentaris GmbH | Lh-rh-antagonisten, deren herstellung und verwendung als arzneimittel |
| TR200200738T2 (tr) * | 1999-09-23 | 2002-08-21 | Zentaris Ag | Endometriyal dokunun rahim dışında çoğalması, kronik alt karın ağrısı ve fallop tüpü tıkanıklığının terapötik olarak giderilmesi. |
| US7005418B1 (en) | 1999-09-23 | 2006-02-28 | Zentaris Gmbh | Method for the therapeutic management of extrauterine proliferation of endometrial tissue, chronic pelvic pain and fallopian tube obstruction |
| DE10024451A1 (de) | 2000-05-18 | 2001-11-29 | Asta Medica Ag | Pharmazeutische Darreichungsform für Peptide, Verfahren zu deren Herstellung und Verwendung |
| HUP0400067A2 (hu) | 2001-04-30 | 2004-04-28 | Zentaris Gmbh | Dementia és neurodegeneratív betegségek kezelése közepes dózisú LHRH-antagonistával |
| SE0104462D0 (sv) * | 2001-12-29 | 2001-12-29 | Carlbiotech Ltd As | Peptide purifcation (Peptidrening) |
| ME00509B (me) * | 2002-09-27 | 2011-10-10 | Zentaris Gmbh | Oblik za terapijsku primjenu aktivnih peptida sa dugotrajnim oslobođenjem aktivnog sastojka i postupak za njihovo dobijanje |
| CN100340572C (zh) * | 2004-12-01 | 2007-10-03 | 中国人民解放军军事医学科学院毒物药物研究所 | 新的lhrh拮抗剂 |
| CN101037472B (zh) * | 2006-03-14 | 2013-03-27 | 中国人民解放军军事医学科学院毒物药物研究所 | 具有低组胺释放作用的促黄体生成素释放激素拮抗剂 |
| EP1891964A1 (en) * | 2006-08-08 | 2008-02-27 | AEterna Zentaris GmbH | Application of initial doses of LHRH analogues and maintenance doses of LHRH antagonists for the treatment of hormone-dependent cancers and corresponding pharmaceutical kits |
| CN101597321B (zh) * | 2008-06-03 | 2013-04-24 | 中国人民解放军军事医学科学院毒物药物研究所 | 长效低组胺释放副作用的lhrh拮抗剂 |
| WO2012050892A2 (en) * | 2010-09-29 | 2012-04-19 | Esperance Pharmaceuticals, Inc. | Methods for stimulating, increasing or enhancing killing of a cell that expresses luteinizing hormone releasing hormone (lhrh) receptors |
| CN102584945A (zh) * | 2012-02-09 | 2012-07-18 | 深圳翰宇药业股份有限公司 | 一种醋酸加尼瑞克的制备方法 |
| CN103524599B (zh) * | 2012-07-05 | 2016-04-20 | 中国人民解放军军事医学科学院毒物药物研究所 | 环肽lhrh拮抗剂衍生物及其药物用途 |
| CN104231055A (zh) * | 2013-06-18 | 2014-12-24 | 深圳翰宇药业股份有限公司 | 加尼瑞克前体以及由其制备醋酸加尼瑞克的方法 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4581169A (en) | 1982-12-21 | 1986-04-08 | Syntex (U.S.A.) Inc. | Nona-peptide and deca-peptide analogs of LHRH, useful as LHRH antagonists |
| EP0145032B1 (en) | 1983-08-16 | 1987-11-04 | Akzo N.V. | Lh- rh antagonists |
| US4800191A (en) * | 1987-07-17 | 1989-01-24 | Schally Andrew Victor | LHRH antagonists |
| US5140009A (en) | 1988-02-10 | 1992-08-18 | Tap Pharmaceuticals, Inc. | Octapeptide LHRH antagonists |
| US5110904A (en) * | 1989-08-07 | 1992-05-05 | Abbott Laboratories | Lhrh analogs |
| US5300492A (en) * | 1988-02-10 | 1994-04-05 | Tap Pharmaceuticals | LHRH analogs |
| EP0328090A3 (en) * | 1988-02-10 | 1990-08-16 | Abbott Laboratories | Lhrh analogs |
| CN1036343C (zh) * | 1990-11-10 | 1997-11-05 | 天津市计划生育研究所 | 新促黄体生成素释放激素拮抗类似物的制备方法 |
| DE4117507A1 (de) | 1991-05-24 | 1992-11-26 | Schering Ag | Verfahren zur herstellung von n(pfeil hoch)6(pfeil hoch)-substituierten lysin-derivaten |
| JPH08510260A (ja) * | 1993-05-20 | 1996-10-29 | バイオテック・オーストラリア・プロプライエタリー・リミテッド | Ｌｈｒｈ拮抗剤 |
| RU2074191C1 (ru) * | 1994-06-08 | 1997-02-27 | Российско-германское совместное предприятие "Константа" | Способ синтеза дез-гли 10, /d-лей 6/ lh-rh-этиламида |
| US5942493A (en) * | 1995-11-28 | 1999-08-24 | Asta Medica Aktiengesellschaft | LH-RH antagonists having improved action |
| DE19544212A1 (de) * | 1995-11-28 | 1997-06-05 | Asta Medica Ag | Neue LH-RH-Antagonisten mit verbesserter Wirkung |
| US6054432A (en) * | 1996-09-12 | 2000-04-25 | Asta Medica Aktiengesellschaft | Means for treating prostate hypertrophy and prostate cancer |
| US5968895A (en) | 1996-12-11 | 1999-10-19 | Praecis Pharmaceuticals, Inc. | Pharmaceutical formulations for sustained drug delivery |
| DE19911771B4 (de) * | 1999-03-17 | 2006-03-30 | Zentaris Gmbh | LHRH-Antagonist, Verfahren zu seiner Herstellung und seiner Verwendung |
| US6586403B1 (en) * | 2000-07-20 | 2003-07-01 | Salpep Biotechnology, Inc. | Treating allergic reactions and inflammatory responses with tri-and dipeptides |
| KR100876538B1 (ko) * | 2000-08-17 | 2008-12-31 | 아에테르나 젠타리스 게엠베하 | Ｌｈｒｈ 길항제의 염의 제조방법 |
-
1999
- 1999-03-17 DE DE19911771A patent/DE19911771B4/de not_active Expired - Fee Related
-
2000
- 2000-03-07 TW TW089104093A patent/TWI243179B/zh not_active IP Right Cessation
- 2000-03-11 NZ NZ514830A patent/NZ514830A/en not_active IP Right Cessation
- 2000-03-11 IL IL14548400A patent/IL145484A0/xx active IP Right Grant
- 2000-03-11 AT AT00910816T patent/ATE277077T1/de active
- 2000-03-11 SK SK1323-2001A patent/SK287880B6/sk not_active IP Right Cessation
- 2000-03-11 TR TR2001/03339T patent/TR200103339T2/xx unknown
- 2000-03-11 BR BR0009472-2A patent/BR0009472A/pt not_active Application Discontinuation
- 2000-03-11 CZ CZ20013318A patent/CZ301696B6/cs not_active IP Right Cessation
- 2000-03-11 HU HU0200363A patent/HU229672B1/hu unknown
- 2000-03-11 PT PT00910816T patent/PT1163264E/pt unknown
- 2000-03-11 AU AU32887/00A patent/AU759442B2/en not_active Expired
- 2000-03-11 CN CNB008067341A patent/CN1185251C/zh not_active Expired - Lifetime
- 2000-03-11 WO PCT/EP2000/002165 patent/WO2000055190A1/de not_active Ceased
- 2000-03-11 DK DK00910816T patent/DK1163264T3/da active
- 2000-03-11 ES ES00910816T patent/ES2225103T3/es not_active Expired - Lifetime
- 2000-03-11 SI SI200030505T patent/SI1163264T1/xx unknown
- 2000-03-11 EP EP00910816A patent/EP1163264B1/de not_active Expired - Lifetime
- 2000-03-11 CA CA2381461A patent/CA2381461C/en not_active Expired - Lifetime
- 2000-03-11 KR KR1020017011843A patent/KR100569623B1/ko not_active Expired - Lifetime
- 2000-03-11 RU RU2001128232/04A patent/RU2227145C2/ru active
- 2000-03-11 DE DE50007905T patent/DE50007905D1/de not_active Expired - Lifetime
- 2000-03-11 JP JP2000605616A patent/JP3801867B2/ja not_active Expired - Lifetime
- 2000-03-11 MX MXPA01010052A patent/MXPA01010052A/es active IP Right Grant
- 2000-03-11 HK HK02107028.9A patent/HK1045531B/zh not_active IP Right Cessation
- 2000-03-11 PL PL351792A patent/PL200647B1/pl unknown
- 2000-03-14 US US09/525,007 patent/US6627609B1/en not_active Expired - Lifetime
- 2000-03-16 CO CO00019239A patent/CO5150192A1/es unknown
- 2000-03-17 AR ARP000101201A patent/AR022970A1/es active IP Right Grant
- 2000-11-03 UA UA2001106842A patent/UA70997C2/uk unknown
-
2001
- 2001-03-12 SI SI200130882T patent/SI1268522T1/sl unknown
- 2001-03-12 YU YU68702A patent/YU68702A/sh unknown
- 2001-09-14 NO NO20014486A patent/NO327753B1/no not_active IP Right Cessation
- 2001-09-16 IL IL145484A patent/IL145484A/en not_active IP Right Cessation
- 2001-09-19 ZA ZA200107753A patent/ZA200107753B/en unknown
- 2001-10-11 BG BG106008A patent/BG65283B1/bg unknown
-
2002
- 2002-09-05 IL IL151647A patent/IL151647A/en not_active IP Right Cessation
-
2003
- 2003-09-29 US US10/671,573 patent/US7148195B2/en not_active Expired - Lifetime
-
2006
- 2006-07-24 US US11/459,583 patent/US7732412B2/en not_active Expired - Lifetime
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