CN105732649B - 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 - Google Patents

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 Download PDF

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CN105732649B
CN105732649B CN201610104516.XA CN201610104516A CN105732649B CN 105732649 B CN105732649 B CN 105732649B CN 201610104516 A CN201610104516 A CN 201610104516A CN 105732649 B CN105732649 B CN 105732649B
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trifluoromethyl
benzyl
pyrimidine
amino
fluoro
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CN105732649A (zh
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金善美
金载善
李珉姬
李素英
李峰镛
申瑛娥
朴依善
李晶娥
韩敏永
安才承
俞兑暻
金薰泽
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Tiumbio Co ltd
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Tiumbio Co ltd
SK Chemicals Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D491/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D491/02—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 two hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/527—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
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    • A61P15/18—Feminine contraceptives
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D471/02—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 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D471/12—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 in which the condensed system contains three hetero rings
    • C07D471/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D491/02—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 two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D491/02—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 two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • C07D—HETEROCYCLIC COMPOUNDS
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
CN201610104516.XA 2012-02-28 2013-02-28 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 Active CN105732649B (zh)

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KR10-2012-0020479 2012-02-28
KR20120020479 2012-02-28
CN201380011513.6A CN104136441B (zh) 2012-02-28 2013-02-28 促性腺激素释放激素受体拮抗剂、其制备方法和包含该促性腺激素释放激素受体拮抗剂的药物组合物

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CN201380011513.6A Active CN104136441B (zh) 2012-02-28 2013-02-28 促性腺激素释放激素受体拮抗剂、其制备方法和包含该促性腺激素释放激素受体拮抗剂的药物组合物

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US (1) US9481684B2 (https=)
EP (1) EP2820021B1 (https=)
JP (1) JP6209171B2 (https=)
KR (1) KR101495260B1 (https=)
CN (2) CN105732649B (https=)
AU (1) AU2013226661B2 (https=)
BR (1) BR112014021331B1 (https=)
CA (1) CA2865547C (https=)
ES (1) ES2613856T3 (https=)
MX (1) MX357841B (https=)
WO (1) WO2013129879A1 (https=)

Families Citing this family (9)

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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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US5633248A (en) * 1994-11-21 1997-05-27 Takeda Chemical Industries, Ltd. Amine compounds, their production and use
US6156772A (en) * 1997-06-05 2000-12-05 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
US20050250846A1 (en) * 2002-06-13 2005-11-10 Anderson Mark B Non-peptide GnRH agents, pharmaceutical compositions and methods for their use

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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
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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US5633248A (en) * 1994-11-21 1997-05-27 Takeda Chemical Industries, Ltd. Amine compounds, their production and use
US6156772A (en) * 1997-06-05 2000-12-05 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
US20050250846A1 (en) * 2002-06-13 2005-11-10 Anderson Mark B Non-peptide GnRH agents, pharmaceutical compositions and methods for their use

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CA2865547A1 (en) 2013-09-06
CN105732649A (zh) 2016-07-06
EP2820021B1 (en) 2016-11-30
US20150166558A1 (en) 2015-06-18
AU2013226661A1 (en) 2014-10-16
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
BR112014021331B1 (pt) 2020-12-15
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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