JP2003512379A5 - - Google Patents
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- Publication number
- JP2003512379A5 JP2003512379A5 JP2001531842A JP2001531842A JP2003512379A5 JP 2003512379 A5 JP2003512379 A5 JP 2003512379A5 JP 2001531842 A JP2001531842 A JP 2001531842A JP 2001531842 A JP2001531842 A JP 2001531842A JP 2003512379 A5 JP2003512379 A5 JP 2003512379A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- methyl
- alkyl
- fluorobenzyl
- aminomethyl
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 description 29
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 description 16
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 description 14
- 125000003710 aryl alkyl group Chemical group 0.000 description 14
- 125000000623 heterocyclic group Chemical group 0.000 description 14
- -1 2-pyridylethyl Chemical group 0.000 description 11
- 125000000217 alkyl group Chemical group 0.000 description 11
- 229910052739 hydrogen Inorganic materials 0.000 description 10
- 239000001257 hydrogen Substances 0.000 description 10
- 125000001072 heteroaryl group Chemical group 0.000 description 8
- 150000002431 hydrogen Chemical class 0.000 description 8
- 125000000547 substituted alkyl group Chemical group 0.000 description 8
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 8
- 229910052757 nitrogen Inorganic materials 0.000 description 7
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 6
- 125000002950 monocyclic group Chemical group 0.000 description 6
- 239000008194 pharmaceutical composition Substances 0.000 description 6
- 125000003118 aryl group Chemical group 0.000 description 5
- 125000003107 substituted aryl group Chemical group 0.000 description 5
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 4
- 125000004093 cyano group Chemical group *C#N 0.000 description 4
- 229910052736 halogen Inorganic materials 0.000 description 4
- 150000002367 halogens Chemical class 0.000 description 4
- 125000003545 alkoxy group Chemical group 0.000 description 3
- 125000003282 alkyl amino group Chemical group 0.000 description 3
- 125000004414 alkyl thio group Chemical group 0.000 description 3
- 125000004429 atom Chemical group 0.000 description 3
- 239000003163 gonadal steroid hormone Substances 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 3
- 125000006479 2-pyridyl methyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 description 2
- 239000000579 Gonadotropin-Releasing Hormone Substances 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 description 2
- 206010046798 Uterine leiomyoma Diseases 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 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 description 2
- 229940035638 gonadotropin-releasing hormone Drugs 0.000 description 2
- 201000010260 leiomyoma Diseases 0.000 description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 description 2
- 230000035935 pregnancy Effects 0.000 description 2
- 239000000651 prodrug Substances 0.000 description 2
- 229940002612 prodrug Drugs 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- VXVTZEBWTNYPSS-UHFFFAOYSA-N 3-(aminomethyl)-2-tert-butyl-4-[(2-fluorophenyl)methyl]-7-oxo-N-(3-phenylpropyl)-6H-pyrrolo[1,2-a]pyrimidine-6-carboxamide Chemical compound NCC=1C(=NC=2N(C=1CC1=C(C=CC=C1)F)C(C(C=2)=O)C(=O)NCCCC1=CC=CC=C1)C(C)(C)C VXVTZEBWTNYPSS-UHFFFAOYSA-N 0.000 description 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 description 1
- 208000003200 Adenoma Diseases 0.000 description 1
- 206010001233 Adenoma benign Diseases 0.000 description 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 201000009273 Endometriosis Diseases 0.000 description 1
- 102000006771 Gonadotropins Human genes 0.000 description 1
- 108010086677 Gonadotropins Proteins 0.000 description 1
- 206010020112 Hirsutism Diseases 0.000 description 1
- 206010036618 Premenstrual syndrome Diseases 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 208000020221 Short stature Diseases 0.000 description 1
- 208000002495 Uterine Neoplasms Diseases 0.000 description 1
- 125000002252 acyl group Chemical group 0.000 description 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 239000002622 gonadotropin Substances 0.000 description 1
- 125000005343 heterocyclic alkyl group Chemical group 0.000 description 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 1
- 208000002551 irritable bowel syndrome Diseases 0.000 description 1
- 206010025135 lupus erythematosus Diseases 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- 230000001817 pituitary effect Effects 0.000 description 1
- 201000010065 polycystic ovary syndrome Diseases 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 208000019116 sleep disease Diseases 0.000 description 1
- 208000020685 sleep-wake disease Diseases 0.000 description 1
- 206010046766 uterine cancer Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41876899A | 1999-10-15 | 1999-10-15 | |
| US09/418,768 | 1999-10-15 | ||
| PCT/US2000/028677 WO2001029044A1 (en) | 1999-10-15 | 2000-10-16 | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2003512379A JP2003512379A (ja) | 2003-04-02 |
| JP2003512379A5 true JP2003512379A5 (https=) | 2007-11-22 |
Family
ID=23659500
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001531842A Pending JP2003512379A (ja) | 1999-10-15 | 2000-10-16 | 性腺刺激ホルモン放出ホルモンレセプターアンタゴニストおよびそれに関連する方法 |
Country Status (11)
| Country | Link |
|---|---|
| EP (1) | EP1220857B1 (https=) |
| JP (1) | JP2003512379A (https=) |
| KR (1) | KR20020045609A (https=) |
| AT (1) | ATE305008T1 (https=) |
| AU (1) | AU769855B2 (https=) |
| CA (1) | CA2386942A1 (https=) |
| DE (1) | DE60022769T2 (https=) |
| ES (1) | ES2249302T3 (https=) |
| HK (1) | HK1047437B (https=) |
| MX (1) | MXPA02003614A (https=) |
| WO (1) | WO2001029044A1 (https=) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1255738E (pt) | 2000-01-25 | 2012-06-19 | Neurocrine Biosciences Inc | Antagonistas do receptor da hormona de libertação da gonadotrofina e métodos relacionados com os mesmos |
| EP1392348B1 (en) * | 2001-04-30 | 2008-07-09 | AEterna Zentaris GmbH | Treatment of dementia and neurodegenerative diseases with intermediate doses of lhrh antagonists |
| JP2005500352A (ja) | 2001-08-02 | 2005-01-06 | ニューロクライン バイオサイエンシーズ， インコーポレイテッド | ゴナドトロピン放出ホルモンレセプター（ＧｎＲＨ）アンタゴニストとしての１，２，４−トリアジン−３，５−ジオン |
| JP2005500356A (ja) | 2001-08-02 | 2005-01-06 | ニューロクライン バイオサイエンシーズ， インコーポレイテッド | ゴナドトロピン放出ホルモンレセプターアンタゴニスト |
| WO2003011293A2 (en) | 2001-08-02 | 2003-02-13 | Neurocrine Biosciences, Inc. | Pyridinone and pyridazinone derivatives as gonadotropin-releasing hormone receptor antagonists |
| AU2002324586B2 (en) | 2001-08-02 | 2008-04-24 | Neurocrine Biosciences, Inc. | 1,3,5-triazine-2,4,6-triones, preparation and use as gonadotropin-releasing hormone receptor antagonists |
| JP2005505525A (ja) | 2001-08-02 | 2005-02-24 | ニューロクライン バイオサイエンシーズ， インコーポレイテッド | 性腺刺激ホルモン放出ホルモンレセプターアンタゴニストおよびそれに関連する方法 |
| WO2003068769A1 (en) | 2002-02-12 | 2003-08-21 | Pfizer Inc. | Non-peptide compounds affecting the action of gonadotropin-releasing hormone (gnrh) |
| BR0312123A (pt) | 2002-06-13 | 2005-03-29 | Pfizer | Agentes de gnrh não peptìdicos, composições farmacêuticas e métodos para o seu uso |
| ATE428427T1 (de) | 2003-07-07 | 2009-05-15 | Neurocrine Biosciences Inc | Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten |
| CN100424078C (zh) | 2003-07-07 | 2008-10-08 | 纽罗克里生物科学有限公司 | 作为促性激素释放激素受体拮抗剂的嘧啶-2,4-二酮衍生物 |
| US7015226B2 (en) | 2003-07-07 | 2006-03-21 | Neurocrine Biosciences, Inc. | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
| CL2008000986A1 (es) | 2007-04-06 | 2008-10-17 | Neurocrine Biosciences Inc | COMPUESTO DERIVADO DE HETEROCICLOS DE NITROGENO, AGONISTAS DEL RECEPTOR GnRH; COMPOSICION FARMACEUTICA QUE COMPRENDE A DICHO COMPUESTO; Y USO PARA TRATAR UNA AFECCION RELACIONADA CON LAS HORMONAS SEXUALES, ENDOMETRIOSIS, DISMENORREA, ENFERMEDAD DE OV |
| PE20090044A1 (es) | 2007-04-06 | 2009-01-23 | Neurocrine Biosciences Inc | Antagonistas del receptor de la hormona liberadora de gonadotropina y procedimientos relacionados con los mismos |
| JP5637859B2 (ja) * | 2007-12-13 | 2014-12-10 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | 嚢胞性線維症膜コンダクタンスレギュレーターのモジュレーター |
| CN101987865B (zh) * | 2009-07-29 | 2014-07-30 | 中国人民解放军军事医学科学院毒物药物研究所 | 含有乙内酰脲结构的促黄体生成素释放激素拮抗剂 |
| TW201130854A (en) | 2009-12-22 | 2011-09-16 | Bayer Schering Pharma Ag | Pyridinone derivatives and pharmaceutical compositions thereof |
| WO2012175514A1 (en) | 2011-06-21 | 2012-12-27 | Bayer Intellectual Property Gmbh | Pyridinone derivatives and pharmaceutical compositions thereof |
| CN105732649B (zh) * | 2012-02-28 | 2019-02-05 | 株式会社蒂奥姆生物 | 促性腺激素释放激素受体拮抗剂、其制备方法和包含该拮抗剂的药物组合物 |
| WO2014133112A1 (ja) * | 2013-03-01 | 2014-09-04 | 国立大学法人東京大学 | オートタキシン阻害活性を有する８－置換イミダゾピリミジノン誘導体 |
| KR101973074B1 (ko) | 2018-11-30 | 2019-04-26 | 주식회사 티움바이오 | 퓨로피리미딘 화합물의 염 및 결정형, 및 이를 포함하는 약학적 조성물 |
| KR102598203B1 (ko) | 2019-11-25 | 2023-11-03 | 암젠 인크 | 델타-5 불포화효소 억제제로서의 헤테로시클릭 화합물 및 사용 방법 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6194419B1 (en) * | 1997-12-26 | 2001-02-27 | Takeda Chemical Industries, Ltd. | Nitrogen-containing heterocyclic compounds, their production and use |
| US6081508A (en) * | 1998-02-25 | 2000-06-27 | Indus River Networks, Inc. | Remote computer communication |
| WO1999051232A1 (en) * | 1998-04-02 | 1999-10-14 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
-
2000
- 2000-10-16 DE DE60022769T patent/DE60022769T2/de not_active Expired - Fee Related
- 2000-10-16 CA CA002386942A patent/CA2386942A1/en not_active Abandoned
- 2000-10-16 HK HK02109095.3A patent/HK1047437B/en not_active IP Right Cessation
- 2000-10-16 MX MXPA02003614A patent/MXPA02003614A/es active IP Right Grant
- 2000-10-16 AU AU12089/01A patent/AU769855B2/en not_active Ceased
- 2000-10-16 JP JP2001531842A patent/JP2003512379A/ja active Pending
- 2000-10-16 WO PCT/US2000/028677 patent/WO2001029044A1/en not_active Ceased
- 2000-10-16 EP EP00973591A patent/EP1220857B1/en not_active Expired - Lifetime
- 2000-10-16 KR KR1020027004773A patent/KR20020045609A/ko not_active Withdrawn
- 2000-10-16 ES ES00973591T patent/ES2249302T3/es not_active Expired - Lifetime
- 2000-10-16 AT AT00973591T patent/ATE305008T1/de not_active IP Right Cessation
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