BR112014021331B1 - Antagonistas do receptor do hormônio liberador de gonadotropina, composição farmacêutica compreendendo os mesmos e uso desses - Google Patents
Antagonistas do receptor do hormônio liberador de gonadotropina, composição farmacêutica compreendendo os mesmos e uso desses Download PDFInfo
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- BR112014021331B1 BR112014021331B1 BR112014021331-3A BR112014021331A BR112014021331B1 BR 112014021331 B1 BR112014021331 B1 BR 112014021331B1 BR 112014021331 A BR112014021331 A BR 112014021331A BR 112014021331 B1 BR112014021331 B1 BR 112014021331B1
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- Prior art keywords
- trifluoromethyl
- benzyl
- amino
- pyrimidine
- fluoro
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 10
- 229940127445 Gonadotropin Releasing Hormone Receptor Antagonists Drugs 0.000 title abstract 3
- 201000010099 disease Diseases 0.000 claims abstract description 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 17
- 239000003163 gonadal steroid hormone Substances 0.000 claims abstract description 14
- 206010046798 Uterine leiomyoma Diseases 0.000 claims abstract description 11
- 201000010260 leiomyoma Diseases 0.000 claims abstract description 9
- 108010086677 Gonadotropins Proteins 0.000 claims abstract description 8
- 102000006771 Gonadotropins Human genes 0.000 claims abstract description 8
- 239000002622 gonadotropin Substances 0.000 claims abstract description 8
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims abstract description 7
- 201000009273 Endometriosis Diseases 0.000 claims abstract description 6
- 208000000509 infertility Diseases 0.000 claims abstract description 6
- 230000036512 infertility Effects 0.000 claims abstract description 6
- 231100000535 infertility Toxicity 0.000 claims abstract description 6
- 208000006155 precocious puberty Diseases 0.000 claims abstract description 6
- 150000003431 steroids Chemical class 0.000 claims abstract description 6
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- 208000024827 Alzheimer disease Diseases 0.000 claims abstract description 5
- 201000000736 Amenorrhea Diseases 0.000 claims abstract description 5
- 206010001928 Amenorrhoea Diseases 0.000 claims abstract description 5
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims abstract description 5
- 206010020864 Hypertrichosis Diseases 0.000 claims abstract description 5
- 208000037093 Menstruation Disturbances Diseases 0.000 claims abstract description 5
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- -1 cyano, nitro, amino Chemical group 0.000 claims description 711
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- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims description 113
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 98
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- 125000000753 cycloalkyl group Chemical group 0.000 claims description 51
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- 239000001257 hydrogen Substances 0.000 claims description 37
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Classifications
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- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
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- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
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- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
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- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/20—Spiro-condensed systems
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| KR10-2012-0020479 | 2012-02-28 | ||
| KR20120020479 | 2012-02-28 | ||
| PCT/KR2013/001660 WO2013129879A1 (en) | 2012-02-28 | 2013-02-28 | Gonadotropin releasing hormone receptor antagonists, method for the preparation thereof and pharmaceutical composition comprising the same |
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| BR112014021331A2 BR112014021331A2 (https=) | 2017-06-20 |
| BR112014021331A8 BR112014021331A8 (pt) | 2017-10-10 |
| BR112014021331B1 true BR112014021331B1 (pt) | 2020-12-15 |
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| MX (1) | MX357841B (https=) |
| WO (1) | WO2013129879A1 (https=) |
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| US10005781B2 (en) | 2013-10-30 | 2018-06-26 | Shanghai Hengrui Pharmaceutical Co., Ltd. | Pyrazolopyrimidone or pyrrolotriazone derivatives, method of preparing same, and pharmaceutical applications thereof |
| JP2020528060A (ja) * | 2017-07-28 | 2020-09-17 | 江蘇恒瑞医薬股▲ふん▼有限公司 | ピリミドンヘテロアリール誘導体の製造方法およびピリミドンヘテロアリール誘導体の中間体 |
| KR101973074B1 (ko) * | 2018-11-30 | 2019-04-26 | 주식회사 티움바이오 | 퓨로피리미딘 화합물의 염 및 결정형, 및 이를 포함하는 약학적 조성물 |
| CN109651265A (zh) * | 2019-02-16 | 2019-04-19 | 安徽诺全药业有限公司 | 一种Elagolix的制备方法 |
| ES2944511T3 (es) | 2019-03-26 | 2023-06-21 | Novel Pharma Inc | Derivado de GnRH que se une a ácido graso de acción prolongada y composición farmacéutica que comprende el mismo |
| KR20210155350A (ko) | 2020-06-15 | 2021-12-22 | 한상왕 | 녹차 추출물 및 비타민 d3를 유효성분으로 포함하는 자궁근종 개선용 조성물 |
| CN115124545B (zh) * | 2022-08-31 | 2023-01-03 | 南京远淑医药科技有限公司 | 一种促性腺激素释放激素受体拮抗剂中间体的合成方法 |
| KR102738115B1 (ko) | 2024-03-25 | 2024-12-05 | 한상왕 | 자궁근종 예방, 개선 또는 치료용 약학 조성물 |
| WO2025230335A1 (ko) * | 2024-05-03 | 2025-11-06 | 주식회사 티움바이오 | 에스트로겐-의존성 질환 치료 또는 예방용 약학적 조성물 |
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| CA2163325A1 (en) * | 1994-11-21 | 1996-05-22 | Kaneyoshi Kato | Amine compounds, their production and use |
| US6156772A (en) | 1997-06-05 | 2000-12-05 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| TWI225863B (en) * | 1999-03-24 | 2005-01-01 | Takeda Chemical Industries Ltd | Thienopyrimidine compounds, their production and use |
| DE60022769T2 (de) * | 1999-10-15 | 2006-07-06 | Neurocrine Biosciences, Inc., San Diego | Gonadotropin freisetzenden hormon rezeptor antagonisten und ihre verwandten verwendungen |
| 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 |
| FR2833948B1 (fr) * | 2001-12-21 | 2004-02-06 | Sod Conseils Rech Applic | Nouveaux derives de benzimidazole et leur utilisation en tant que medicament |
| BR0312123A (pt) | 2002-06-13 | 2005-03-29 | Pfizer | Agentes de gnrh não peptìdicos, composições farmacêuticas e métodos para o seu uso |
| ES2494842T3 (es) * | 2005-07-22 | 2014-09-16 | Takeda Pharmaceutical Company Limited | Agente que previene la ovulación precoz |
| US9034850B2 (en) * | 2009-11-20 | 2015-05-19 | Sk Chemicals Co., Ltd. | Gonadotropin releasing hormone receptor antagonist, preparation method thereof and pharmaceutical composition comprising the same |
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- 2013-02-28 WO PCT/KR2013/001660 patent/WO2013129879A1/en not_active Ceased
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| CN105732649A (zh) | 2016-07-06 |
| EP2820021B1 (en) | 2016-11-30 |
| US20150166558A1 (en) | 2015-06-18 |
| AU2013226661A1 (en) | 2014-10-16 |
| CN105732649B (zh) | 2019-02-05 |
| EP2820021A4 (en) | 2015-10-21 |
| MX2014010345A (es) | 2014-11-14 |
| CN104136441A (zh) | 2014-11-05 |
| AU2013226661B2 (en) | 2017-08-31 |
| JP6209171B2 (ja) | 2017-10-04 |
| MX357841B (es) | 2018-07-26 |
| US9481684B2 (en) | 2016-11-01 |
| KR20130102002A (ko) | 2013-09-16 |
| BR112014021331A8 (pt) | 2017-10-10 |
| EP2820021A1 (en) | 2015-01-07 |
| ES2613856T3 (es) | 2017-05-26 |
| WO2013129879A1 (en) | 2013-09-06 |
| CN104136441B (zh) | 2016-09-28 |
| CA2865547C (en) | 2020-03-10 |
| KR101495260B1 (ko) | 2015-02-26 |
| BR112014021331A2 (https=) | 2017-06-20 |
| JP2015510868A (ja) | 2015-04-13 |
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