PE20000756A1 - Antagonistas de hormona liberadora de gonadotropina - Google Patents
Antagonistas de hormona liberadora de gonadotropinaInfo
- Publication number
- PE20000756A1 PE20000756A1 PE1999000683A PE00068399A PE20000756A1 PE 20000756 A1 PE20000756 A1 PE 20000756A1 PE 1999000683 A PE1999000683 A PE 1999000683A PE 00068399 A PE00068399 A PE 00068399A PE 20000756 A1 PE20000756 A1 PE 20000756A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- heterocycle
- members
- releasing hormone
- gonadotropin releasing
- Prior art date
Links
- 239000000579 Gonadotropin-Releasing Hormone Substances 0.000 title abstract 3
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 title abstract 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 abstract 2
- 229940035638 gonadotropin-releasing hormone Drugs 0.000 title abstract 2
- 239000005557 antagonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 abstract 1
- 108700012941 GNRH1 Proteins 0.000 abstract 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 230000003054 hormonal effect Effects 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 230000001568 sexual effect Effects 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Neurosurgery (AREA)
- Anesthesiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Steroid Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
SE REFIERE A UN COMPUESTO DERIVADO DE INDOL (I); A ES ALQUILO C1-C6, ALQUENILO C3-C6, ENTRE OTROS; RO ES H, ALQUILO C1-C6; R1 ES UN GRUPO a, b, c, ENTRE OTROS; R2 ES H, ALQUILO C1-C6, ENTRE OTROS; R2 Y A FORMAN UN ANILLO DE 5-7 MIEMBROS; R3, R4 Y R5 SON H, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; R3 Y R4 FORMAN UN ANILLO DE 3-7 MIEMBROS, HETEROCICLO; R6 ES H, ALQUILO C1-C6, ARILO, ENTRE OTROS; R7 ES H, ALQUILO C1-C6; CUANDO X ES H o HALOGENO, R7 NO SE PRESENTA; R8 ES COOR20, CONR20R21, ENTRE OTROS; R7 Y R8 FORMAN UN HETEROCICLO; R9 Y R9a SON H, ALQUILO C1-C6, ENTRE OTROS; R9 Y R9a o R10 Y R10a FORMAN UN CARBOCICLO DE 3-7 MIEMBROS, =O; R9 Y A FORMAN UN HETEROCICLO DE 3-7 MIEMBROS; R10 Y R10a SON H, ALQUILO C1-C6, ARILO, ENTRE OTROS; R9 Y R10 FORMAN UN CARBOCICLO DE 3-7 MIEMBROS, HETEROCICLO; R9 Y R2; R10 Y R2; R10 Y A FORMAN UN HETEROCICLO C3-C7; R11 Y R12 SON H, ALQUILO C1-C6, ENTRE OTROS; R20 Y R21 SON H, ALQUILO C1-C6, ENTRE OTROS; X ES N, O, SOn, CO, C(R11R12)p; Z ES O, S, NR11; m ES 0-3; n ES 0-2; p ES 0-4. TAMBIEN SE REFIERE A UNA COMPOSICION QUE COMPRENDE ADEMAS UN COMPUESTO QUE TIENE ACTIVIDAD DE HORMONA LIBERADORA DE LA HORMONA LUTEINIZANTE. EL COMPUESTO I INHIBE A LA HORMONA LIBERADORA DE GONADOTROPINA Y PUEDE SER UTIL PARA EL TRATAMIENTO DE CANCER DEPENDIENTE DE HORMONAS SEXUALES, HIPERTROFIA PROSTATICA BENIGNA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/115,497 US6200957B1 (en) | 1995-12-14 | 1998-07-14 | Antagonists of gonadotropin releasing hormone |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20000756A1 true PE20000756A1 (es) | 2000-08-30 |
Family
ID=22361786
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1999000683A PE20000756A1 (es) | 1998-07-14 | 1999-07-09 | Antagonistas de hormona liberadora de gonadotropina |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US6200957B1 (es) |
| EP (1) | EP1095038B1 (es) |
| JP (1) | JP2002520409A (es) |
| AT (1) | ATE248832T1 (es) |
| AU (1) | AU760030B2 (es) |
| CA (1) | CA2337407A1 (es) |
| DE (1) | DE69911023T2 (es) |
| ES (1) | ES2205855T3 (es) |
| PE (1) | PE20000756A1 (es) |
| WO (1) | WO2000004013A1 (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0022670D0 (en) | 2000-09-15 | 2000-11-01 | Astrazeneca Ab | Molecules |
| SE0100566D0 (sv) | 2001-02-20 | 2001-02-20 | Astrazeneca Ab | Compounds |
| SE0101692D0 (sv) | 2001-05-14 | 2001-05-14 | Astrazeneca Ab | Compounds |
| US7695917B2 (en) * | 2001-10-09 | 2010-04-13 | Oregon Health & Science University | Rescue of gonadotropin releasing hormone receptor mutants |
| WO2003068769A1 (en) | 2002-02-12 | 2003-08-21 | Pfizer Inc. | Non-peptide compounds affecting the action of gonadotropin-releasing hormone (gnrh) |
| AU2003233127A1 (en) | 2002-06-13 | 2003-12-31 | Pfizer Inc. | Non-peptide gnrh agents, pharmaceutical compositions and methods for their use |
| WO2004018479A1 (en) | 2002-08-21 | 2004-03-04 | Astrazeneca Ab | Thieno-pyrrole compounds as antagonists of gonadotropin releasing hormone |
| GB0219472D0 (en) | 2002-08-21 | 2002-10-02 | Astrazeneca Ab | Chemical compounds |
| DE60314158T2 (de) * | 2002-08-21 | 2008-01-31 | Astrazeneca Ab | Pyrazolderivate als gnrh-inhibitoren |
| TW200413351A (en) | 2002-08-21 | 2004-08-01 | Astrazeneca Ab | Chemical compounds |
| TW200407127A (en) | 2002-08-21 | 2004-05-16 | Astrazeneca Ab | Chemical compounds |
| US7045527B2 (en) * | 2002-09-24 | 2006-05-16 | Amgen Inc. | Piperidine derivatives |
| DE102004033902A1 (de) | 2004-07-14 | 2006-02-16 | Zentaris Gmbh | Neue Tetrahydrocarbazolderivate mit verbesserter biologischer Wirkung und verbesserter Löslichkeit als Liganden für G-Protein gekoppelte Rezeptoren (GPCR's) |
| EP2095818A1 (en) | 2008-02-29 | 2009-09-02 | AEterna Zentaris GmbH | Use of LHRH antagonists at non-castrating doses |
| WO2015007606A1 (en) * | 2013-07-15 | 2015-01-22 | Bayer Pharma Aktiengesellschaft | Spiroindoline derivatives and pharmaceutical compositions thereof |
| WO2015091315A1 (en) * | 2013-12-19 | 2015-06-25 | Bayer Pharma Aktiengesellschaft | Spiro[indolin-3,4'-piperidine] derivatives as gnrh receptor antagonists |
| WO2018002673A1 (en) | 2016-07-01 | 2018-01-04 | N4 Pharma Uk Limited | Novel formulations of angiotensin ii receptor antagonists |
| CN110709396A (zh) | 2017-04-06 | 2020-01-17 | 伊文蒂瓦公司 | Yap/taz-tead相互作用的新化合物抑制剂及其在治疗恶性间皮瘤中的用途 |
| EP3632908A1 (en) | 2018-10-02 | 2020-04-08 | Inventiva | Inhibitors of the yap/taz-tead interaction and their use in the treatment of cancer |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2181559A1 (en) | 1972-04-28 | 1973-12-07 | Aec Chimie Organique Bio | N-Phenylalkyl-N-3-indolylalkyl-alkylamines - with sedative, neuroleptic, analgesic, hypotensive, antiserotonin, adrenolytic activity |
| FR2354766A1 (fr) | 1976-06-17 | 1978-01-13 | Labaz | Derives n-aminoalkyles d'indole et procedes pour les preparer |
| ZA795239B (en) | 1978-10-12 | 1980-11-26 | Glaxo Group Ltd | Heterocyclic compounds |
| US4678784A (en) | 1984-04-11 | 1987-07-07 | Mcneilab, Inc. | Method for the treatment of LHRH diseases and conditions |
| US4544663A (en) | 1984-05-07 | 1985-10-01 | Sandoz, Inc. | Indolamine derivatives as anti-fertility agents |
| DE3821148A1 (de) | 1988-06-23 | 1989-12-28 | Erwin Von Dr Angerer | Aminoalkylindole, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate |
| AU4649189A (en) | 1988-11-14 | 1990-06-12 | Upjohn Company, The | Alpha-amino-indole-3-acetic acids useful as anti-diabetic, anti-obesity and anti-atherosclerotic agents |
| US5030640A (en) | 1989-01-05 | 1991-07-09 | Merck & Co., Inc. | Novel β-adrenergic agonists and pharmaceutical compositions thereof |
| WO1990009799A1 (en) * | 1989-02-23 | 1990-09-07 | Colorado State University Research Foundation | GnRH ANALOGS FOR DESTROYING GONADOTROPHS |
| TW449600B (en) | 1994-04-19 | 2001-08-11 | Takeda Chemical Industries Ltd | Condensed-ring thiophene derivatives, their production and use |
| US5607939A (en) | 1994-04-28 | 1997-03-04 | Takeda Chemical Industries, Ltd. | Condensed heterocyclic compounds, their production and use |
| DE69528257T2 (de) | 1994-04-29 | 2003-05-15 | Takeda Chemical Industries, Ltd. | KONDENSIERTE HETEROCYCLISCHE VERBINDUNG, DEREN HERSTELLUNG UND VERWENDUNG ALS GnRH ANTAGONISTEN |
| US5780437A (en) | 1995-12-14 | 1998-07-14 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| US5756507A (en) | 1995-12-14 | 1998-05-26 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| IL124613A0 (en) | 1995-12-14 | 1998-12-06 | Merck & Co Inc | Antagonists of gonadotropin releasing hormone |
| US5849764A (en) * | 1995-12-14 | 1998-12-15 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| DE69620241T2 (de) | 1995-12-14 | 2002-10-02 | MERCK & CO., INC. (A NEW JERSEY CORP.) | Gonadotropin releasing hormon- antagonisten |
| EP1023045A2 (en) * | 1997-10-24 | 2000-08-02 | Neorx Corporation | Delivery vehicles for bioactive agents and uses thereof |
-
1998
- 1998-07-14 US US09/115,497 patent/US6200957B1/en not_active Expired - Fee Related
-
1999
- 1999-07-09 WO PCT/US1999/015581 patent/WO2000004013A1/en not_active Ceased
- 1999-07-09 DE DE69911023T patent/DE69911023T2/de not_active Expired - Fee Related
- 1999-07-09 AU AU49816/99A patent/AU760030B2/en not_active Ceased
- 1999-07-09 EP EP99933850A patent/EP1095038B1/en not_active Expired - Lifetime
- 1999-07-09 PE PE1999000683A patent/PE20000756A1/es not_active Application Discontinuation
- 1999-07-09 AT AT99933850T patent/ATE248832T1/de not_active IP Right Cessation
- 1999-07-09 CA CA002337407A patent/CA2337407A1/en not_active Abandoned
- 1999-07-09 JP JP2000560119A patent/JP2002520409A/ja not_active Withdrawn
- 1999-07-09 ES ES99933850T patent/ES2205855T3/es not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| AU760030B2 (en) | 2003-05-08 |
| US6200957B1 (en) | 2001-03-13 |
| ATE248832T1 (de) | 2003-09-15 |
| WO2000004013A1 (en) | 2000-01-27 |
| CA2337407A1 (en) | 2000-01-27 |
| ES2205855T3 (es) | 2004-05-01 |
| DE69911023T2 (de) | 2004-06-03 |
| DE69911023D1 (de) | 2003-10-09 |
| EP1095038B1 (en) | 2003-09-03 |
| EP1095038A1 (en) | 2001-05-02 |
| JP2002520409A (ja) | 2002-07-09 |
| AU4981699A (en) | 2000-02-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |