ATE412412T1 - Derivate des 3-hydroxy-4-(cyclyl-alkylaminoalkyl)-5-phenyl-1 -pyrazols als antagonisten des gonadotropin freisetzenden hormons (gnrh) zur anwendung in de behandlung von geschlechtshormonellen erkrankungen, wie prostata-oder gebahrmutterkrebs - Google Patents
Derivate des 3-hydroxy-4-(cyclyl-alkylaminoalkyl)-5-phenyl-1 -pyrazols als antagonisten des gonadotropin freisetzenden hormons (gnrh) zur anwendung in de behandlung von geschlechtshormonellen erkrankungen, wie prostata-oder gebahrmutterkrebsInfo
- Publication number
- ATE412412T1 ATE412412T1 AT03792487T AT03792487T ATE412412T1 AT E412412 T1 ATE412412 T1 AT E412412T1 AT 03792487 T AT03792487 T AT 03792487T AT 03792487 T AT03792487 T AT 03792487T AT E412412 T1 ATE412412 T1 AT E412412T1
- Authority
- AT
- Austria
- Prior art keywords
- cyclyl
- gnrh
- alkylaminoalkyl
- pyrazole
- antagonists
- Prior art date
Links
- 239000000579 Gonadotropin-Releasing Hormone Substances 0.000 title 2
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 title 2
- XLXSAKCOAKORKW-AQJXLSMYSA-N gonadorelin Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 XLXSAKCOAKORKW-AQJXLSMYSA-N 0.000 title 2
- 229940035638 gonadotropin-releasing hormone Drugs 0.000 title 2
- 206010028980 Neoplasm Diseases 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 201000011510 cancer Diseases 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 230000003054 hormonal effect Effects 0.000 title 1
- 230000008774 maternal effect Effects 0.000 title 1
- 210000002307 prostate Anatomy 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
-
- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/18—One oxygen or sulfur atom
- C07D231/20—One oxygen atom attached in position 3 or 5
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/18—One oxygen or sulfur atom
- C07D231/20—One oxygen atom attached in position 3 or 5
- C07D231/22—One oxygen atom attached in position 3 or 5 with aryl radicals attached to ring nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02292077 | 2002-08-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE412412T1 true ATE412412T1 (de) | 2008-11-15 |
Family
ID=31896982
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT03792487T ATE412412T1 (de) | 2002-08-21 | 2003-08-19 | Derivate des 3-hydroxy-4-(cyclyl-alkylaminoalkyl)-5-phenyl-1 -pyrazols als antagonisten des gonadotropin freisetzenden hormons (gnrh) zur anwendung in de behandlung von geschlechtshormonellen erkrankungen, wie prostata-oder gebahrmutterkrebs |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US7514570B2 (de) |
| EP (1) | EP1531811B1 (de) |
| JP (1) | JP2006505528A (de) |
| AR (1) | AR041030A1 (de) |
| AT (1) | ATE412412T1 (de) |
| AU (1) | AU2003255820A1 (de) |
| DE (1) | DE60324431D1 (de) |
| ES (1) | ES2314277T3 (de) |
| TW (1) | TW200413351A (de) |
| WO (1) | WO2004017961A2 (de) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070185106A1 (en) * | 2004-02-20 | 2007-08-09 | Astrazeneca Ab | Pyrrole derivatives as gonadotropin releasing hormone (gnrh) antagonists |
| TWI350168B (en) | 2004-05-07 | 2011-10-11 | Incyte Corp | Amido compounds and their use as pharmaceuticals |
| MX2007002341A (es) | 2004-08-27 | 2007-09-25 | Esteve Labor Dr | Inhibidores del receptor sigma. |
| KR101352012B1 (ko) | 2004-08-27 | 2014-01-15 | 라보라토리오스 델 드라. 에스테브.에스.에이. | 시그마 수용체 저해제 |
| EP1829875A1 (de) | 2006-03-01 | 2007-09-05 | Laboratorios Del Dr. Esteve, S.A. | Pyrazolderivate als Inhibitoren des Sigma-Rezeptors |
| EP1829866A1 (de) | 2006-03-02 | 2007-09-05 | Laboratorios Del Dr. Esteve, S.A. | Inhibitoren von Sigmarezeptoren |
| EP1829867A1 (de) | 2006-03-03 | 2007-09-05 | Laboratorios Del Dr. Esteve, S.A. | Gegenüber dem Sigmarezeptor pharmazeutisch aktive Imidazolverbindungen |
| EP2116539A1 (de) | 2008-04-25 | 2009-11-11 | Laboratorios Del. Dr. Esteve, S.A. | 1-Aryl-3-Amino-alkoxy-pyrazole als Sigma-Liganden zur Verbesserung der analgetischen Wirkung von Opioiden und zur Schwächung der Abhängigkeit davon |
| US20100061976A1 (en) * | 2008-07-24 | 2010-03-11 | Searete Llc, A Limited Liability Corporation Of The State Of Delaware | Method for treating or preventing osteoporosis by reducing follicle stimulating hormone to cyclic physiological levels in a mammalian subject |
| FR2953839A1 (fr) * | 2009-12-14 | 2011-06-17 | Sanofi Aventis | Nouveaux derives d'(heterocycle-piperidine condensee)-(piperazinyl)-1alcanone ou d'(heterocycle-pyrrolidine condensee)-(piperazinyl)-1alcanone et leur utilisation comme inhibiteurs de p75 |
| EP2353591A1 (de) | 2010-02-04 | 2011-08-10 | Laboratorios Del. Dr. Esteve, S.A. | Sigma-Liganden zur Verstärkung der analgesischen Wirkung von Opioden und Opiaten bei postoperativem Schmerz und zur Schwächung der Abhängigkeit davon |
| EP2353598A1 (de) | 2010-02-04 | 2011-08-10 | Laboratorios Del. Dr. Esteve, S.A. | Sigma-Liganden zur Anwendung in der Vorbeugung und/oder Behandlung von postoperativem Schmerz |
| EP2388005A1 (de) | 2010-05-21 | 2011-11-23 | Laboratorios Del. Dr. Esteve, S.A. | Sigma-Liganden zur Vorbeugung und/oder Behandlung von Erbrechen infolge von Chemotherapie oder Strahlentherapie |
| EP2395003A1 (de) | 2010-05-27 | 2011-12-14 | Laboratorios Del. Dr. Esteve, S.A. | Pyrazolverbindungen als Sigmarezeptor-Inhibitoren |
| EP2415471A1 (de) | 2010-08-03 | 2012-02-08 | Laboratorios Del. Dr. Esteve, S.A. | Verwendung von Sigmaliganden bei opioidinduzierter Hyperalgesie |
| EP2524694A1 (de) | 2011-05-19 | 2012-11-21 | Laboratorios Del. Dr. Esteve, S.A. | Verwendung von Sigmaliganden bei Schmerz im Zusammenhang mit Typ-2-Diabetes |
| SG11201604480PA (en) | 2013-12-17 | 2016-07-28 | Esteve Labor Dr | SEROTONIN-NOREPINEPHRINE REUPTAKE INHIBITORS (SNRIs) AND SIGMA RECEPTOR LIGANDS COMBINATIONS |
| CN104557711B (zh) * | 2014-12-26 | 2017-12-15 | 南通大学 | 含fts结构的吡唑肟类化合物的制备和应用 |
| AU2019387370A1 (en) | 2018-11-30 | 2021-06-10 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR19990072124A (ko) | 1995-12-14 | 1999-09-27 | 애쉬톤 왈레이스 티 | 고나도트로핀 방출 호르몬의 길항제 |
| PL327146A1 (en) | 1995-12-14 | 1998-11-23 | Merck & Co Inc | Antagonists of the gonadotrophin liberating hormone |
| WO1997021707A1 (en) | 1995-12-14 | 1997-06-19 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| WO1997021435A1 (en) | 1995-12-14 | 1997-06-19 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| US6200957B1 (en) | 1995-12-14 | 2001-03-13 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| JPH10287655A (ja) | 1997-04-10 | 1998-10-27 | Kaken Pharmaceut Co Ltd | ピラゾール誘導体 |
| US6514977B1 (en) * | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| EP0986385A4 (de) | 1997-06-05 | 2001-05-16 | Merck & Co Inc | Antagonisten des gonadorelins |
| AU729663B2 (en) | 1997-06-05 | 2001-02-08 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| WO1998055123A1 (en) | 1997-06-05 | 1998-12-10 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| WO1998055119A1 (en) | 1997-06-05 | 1998-12-10 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| US6156772A (en) | 1997-06-05 | 2000-12-05 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| EP0986550A1 (de) | 1997-06-05 | 2000-03-22 | Merck & Co., Inc. | Antagonisten des gonadotropin freisetzenden hormons |
| AU1197299A (en) | 1997-10-28 | 1999-05-17 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| EP1027046A4 (de) | 1997-10-28 | 2002-04-03 | Merck & Co Inc | Antagonisten des gonadotropin freisetzenden hormons |
| CA2318957A1 (en) | 1998-02-11 | 1999-08-19 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| CA2317451A1 (en) | 1998-02-11 | 1999-08-19 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| EP1070064A1 (de) | 1998-04-02 | 2001-01-24 | Merck & Co., Inc. | Antagonisten des gonadotropin freisetzenden hormons |
| EP1067930A4 (de) | 1998-04-02 | 2002-09-18 | Merck & Co Inc | Antagonisten des gonadoliberins |
| WO1999051595A1 (en) | 1998-04-02 | 1999-10-14 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| CA2325995A1 (en) | 1998-04-02 | 1999-10-14 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| AU3210799A (en) | 1998-04-02 | 1999-10-25 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| WO1999051234A1 (en) | 1998-04-02 | 1999-10-14 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| EP1131318B1 (de) * | 1998-11-20 | 2004-03-24 | G.D. Searle LLC | Verfahren zur herstellung 5-substituierter pyrazole unter verwendung von dithietane |
| CA2367130A1 (en) | 1999-03-10 | 2000-09-14 | Merck & Co., Inc. | 6-azaindole compounds as antagonists of gonadotropin releasing hormone |
| AU3396000A (en) | 1999-03-10 | 2000-09-28 | Merck & Co., Inc. | 6-azaindole compounds as antagonists of gonadotropin releasing hormone |
| AU3868900A (en) | 1999-03-10 | 2000-09-28 | Merck & Co., Inc. | 6-azaindole compounds as antagonists of gonadotropin releasing hormone |
| WO2000053178A1 (en) | 1999-03-10 | 2000-09-14 | Merck & Co., Inc. | 6-azaindole compounds as antagonists of gonadotropin releasing hormone |
| EP1161431A4 (de) | 1999-03-10 | 2002-04-24 | Merck & Co Inc | 6-azaindol-verbindungen als antagonisten des gonadotropin-freisetzungs hormones |
| EP1165075A4 (de) | 1999-03-10 | 2002-04-10 | Merck & Co Inc | 6-azaindolverbindungen als antagonisten des gonadoliberins |
| US6583153B2 (en) | 2000-12-12 | 2003-06-24 | Ortho-Mcneil Pharmaceutical, Inc. | 7-heterocyclyl quinoline and thieno[2,3-b]yridine derivatives useful as antagonists of gonadotropin releasing hormone |
| SE0100566D0 (sv) | 2001-02-20 | 2001-02-20 | Astrazeneca Ab | Compounds |
| SE0101692D0 (sv) | 2001-05-14 | 2001-05-14 | Astrazeneca Ab | Compounds |
| KR20040083472A (ko) | 2001-12-21 | 2004-10-02 | 다이쇼 세이야꾸 가부시끼가이샤 | 피페라진 유도체 |
-
2003
- 2003-08-15 TW TW092122539A patent/TW200413351A/zh unknown
- 2003-08-19 JP JP2004530361A patent/JP2006505528A/ja active Pending
- 2003-08-19 US US10/524,977 patent/US7514570B2/en not_active Expired - Fee Related
- 2003-08-19 EP EP03792487A patent/EP1531811B1/de not_active Expired - Lifetime
- 2003-08-19 WO PCT/GB2003/003633 patent/WO2004017961A2/en not_active Ceased
- 2003-08-19 AU AU2003255820A patent/AU2003255820A1/en not_active Abandoned
- 2003-08-19 DE DE60324431T patent/DE60324431D1/de not_active Expired - Fee Related
- 2003-08-19 ES ES03792487T patent/ES2314277T3/es not_active Expired - Lifetime
- 2003-08-19 AT AT03792487T patent/ATE412412T1/de not_active IP Right Cessation
- 2003-08-21 AR ARP030103026A patent/AR041030A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| JP2006505528A (ja) | 2006-02-16 |
| DE60324431D1 (de) | 2008-12-11 |
| ES2314277T3 (es) | 2009-03-16 |
| TW200413351A (en) | 2004-08-01 |
| AU2003255820A1 (en) | 2004-03-11 |
| AU2003255820A8 (en) | 2004-03-11 |
| EP1531811A2 (de) | 2005-05-25 |
| US20060287379A1 (en) | 2006-12-21 |
| WO2004017961A2 (en) | 2004-03-04 |
| EP1531811B1 (de) | 2008-10-29 |
| AR041030A1 (es) | 2005-04-27 |
| WO2004017961A3 (en) | 2004-04-08 |
| US7514570B2 (en) | 2009-04-07 |
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| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |