KR102416279B1 - Ｆｓｈｒ의 조절제로서의 피라졸 화합물 및 이의 용도 - Google Patents

Ｆｓｈｒ의 조절제로서의 피라졸 화합물 및 이의 용도 Download PDF

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Publication number
KR102416279B1
KR102416279B1 KR1020177001959A KR20177001959A KR102416279B1 KR 102416279 B1 KR102416279 B1 KR 102416279B1 KR 1020177001959 A KR1020177001959 A KR 1020177001959A KR 20177001959 A KR20177001959 A KR 20177001959A KR 102416279 B1 KR102416279 B1 KR 102416279B1
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compound
optionally substituted
methyl
nitrogen
sulfur
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KR20170033314A (ko
Inventor
헨리 유
창헤 퀴
폴 템페스트
셀바라즈 쥐. 나타라자
스티븐 에스. 팔머
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아레스 트레이딩 에스.아.
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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
    • C07D491/02—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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • 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
    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Reproductive Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020177001959A 2014-06-23 2014-12-22 Ｆｓｈｒ의 조절제로서의 피라졸 화합물 및 이의 용도 Expired - Fee Related KR102416279B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2014/080519 2014-06-23
PCT/CN2014/080519 WO2015196335A1 (en) 2014-06-23 2014-06-23 Pyrazole compounds as modulators of fshr and uses thereof
PCT/CN2014/094459 WO2015196759A1 (en) 2014-06-23 2014-12-22 Pyrazole compounds as modulators of fshr and uses thereof

Publications (2)

Publication Number Publication Date
KR20170033314A KR20170033314A (ko) 2017-03-24
KR102416279B1 true KR102416279B1 (ko) 2022-07-01

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Family Applications (1)

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KR1020177001959A Expired - Fee Related KR102416279B1 (ko) 2014-06-23 2014-12-22 Ｆｓｈｒ의 조절제로서의 피라졸 화합물 및 이의 용도

Country Status (12)

Country Link
US (3) US10208055B2 (enExample)
EP (1) EP3157929B1 (enExample)
JP (3) JP6557331B2 (enExample)
KR (1) KR102416279B1 (enExample)
CN (1) CN106573937B (enExample)
AU (3) AU2014398875B2 (enExample)
CA (1) CA2955415A1 (enExample)
DK (1) DK3157929T3 (enExample)
ES (1) ES2972131T3 (enExample)
MX (1) MX389867B (enExample)
RU (1) RU2752173C2 (enExample)
WO (2) WO2015196335A1 (enExample)

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WO2015196335A1 (en) 2014-06-23 2015-12-30 Tocopherx, Inc. Pyrazole compounds as modulators of fshr and uses thereof
CN106866692A (zh) * 2017-03-30 2017-06-20 毛阿龙 具有苯并1,4‑二氧杂环己二烯酮结构的fshr拮抗剂的制备方法
CN106967076A (zh) * 2017-03-30 2017-07-21 河南师范大学 一种具有6h‑二苯并吡喃结构化合物及其制备方法
CN106977523A (zh) * 2017-03-30 2017-07-25 河南师范大学 具有苯基并四氢吡咯结构的fshr拮抗剂及其制备方法
EP4335512A3 (en) * 2017-12-22 2024-06-12 HiberCell, Inc. Chromenopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
HUE062273T2 (hu) 2018-05-03 2023-10-28 Jiangsu Hengrui Pharmaceuticals Co Ltd Benzimidazolszármazékok mint a retinsavreceptor rokon árvareceptor-gamma (RORy) modulátorai és gyógyszerészeti felhasználásaik
TW202112784A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之𠳭唏并嘧啶衍生物
CN113754678B (zh) * 2020-06-02 2023-03-10 江苏恒瑞医药股份有限公司 二氢硫代色烯并吡唑类衍生物、其制备方法及其在医药上的应用
WO2022007924A1 (zh) * 2020-07-09 2022-01-13 江苏恒瑞医药股份有限公司 氧杂氮杂双环类衍生物、其制备方法及其在医药上的应用
EP4190789A1 (en) 2020-07-29 2023-06-07 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Oxa-azaspiro derivative, and preparation method therefor and pharmaceutical use thereof
KR20240101561A (ko) 2021-10-14 2024-07-02 인사이트 코포레이션 Kras의 저해제로서의 퀴놀린 화합물
WO2024044778A2 (en) * 2022-08-26 2024-02-29 Celmatix Inc. Novel modulators of fshr and uses thereof
JP2025535050A (ja) * 2022-10-05 2025-10-22 ラディオネティクス オンコロジー，インク． 卵胞刺激ホルモン受容体（ｆｓｈｒ）を標的とした治療薬およびその使用
WO2024184461A2 (en) 2023-03-08 2024-09-12 Ferring B.V. Small molecule fsh receptor modulators
WO2024263803A2 (en) * 2023-06-21 2024-12-26 Celmatix Inc. Novel modulators of fshr and uses thereof

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WO2003024936A1 (en) 2001-09-19 2003-03-27 Pharmacia Corporation Substituted pyrazolo compounds for the treatment of inflammation
WO2008035356A2 (en) 2006-09-20 2008-03-27 Glenmark Pharmaceuticals Limited Novel cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation
US20100215741A1 (en) * 2009-02-25 2010-08-26 Neuroscienze Pharmaness S.C. A.R.L. Pharmaceutical compounds
US20100216785A1 (en) 2009-02-25 2010-08-26 Neuroscienze Pharmaness S.C. A.R.L. Pharmaceutical compositions
WO2011058149A1 (en) * 2009-11-13 2011-05-19 Merck Serono S.A. Tricyclic pyrazol amine derivatives

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PL377848A1 (pl) * 2003-02-07 2006-02-20 Daiichi Pharmaceutical Co., Ltd. Pochodne pirazoli
MX2007014085A (es) * 2005-05-12 2008-02-07 Wyeth Corp Pirrolobenzodiazepinas y derivados de carboxamida heterociclica como antagonistas de receptor de hormona estimulante del foliculo.
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CN104114544A (zh) 2012-02-08 2014-10-22 默克专利有限公司 用作卵泡刺激素受体激动剂的氘化噻唑烷酮类似物
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JP6625973B2 (ja) * 2013-06-24 2019-12-25 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ Ｆｓｈｒの調節剤としてのピラゾール化合物及びその使用
WO2015196335A1 (en) * 2014-06-23 2015-12-30 Tocopherx, Inc. Pyrazole compounds as modulators of fshr and uses thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003024936A1 (en) 2001-09-19 2003-03-27 Pharmacia Corporation Substituted pyrazolo compounds for the treatment of inflammation
WO2008035356A2 (en) 2006-09-20 2008-03-27 Glenmark Pharmaceuticals Limited Novel cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation
US20100215741A1 (en) * 2009-02-25 2010-08-26 Neuroscienze Pharmaness S.C. A.R.L. Pharmaceutical compounds
US20100216785A1 (en) 2009-02-25 2010-08-26 Neuroscienze Pharmaness S.C. A.R.L. Pharmaceutical compositions
WO2011058149A1 (en) * 2009-11-13 2011-05-19 Merck Serono S.A. Tricyclic pyrazol amine derivatives

Also Published As

Publication number Publication date
WO2015196335A1 (en) 2015-12-30
US10208055B2 (en) 2019-02-19
EP3157929B1 (en) 2023-12-13
US10941152B2 (en) 2021-03-09
CN106573937A (zh) 2017-04-19
AU2014398875B2 (en) 2019-11-21
US20190135823A1 (en) 2019-05-09
CN106573937B (zh) 2022-02-11
MX2017000182A (es) 2017-06-30
AU2020201240A1 (en) 2020-03-12
MX389867B (es) 2025-03-20
EP3157929A4 (en) 2018-03-07
AU2021204814A1 (en) 2021-08-05
RU2752173C2 (ru) 2021-07-23
WO2015196759A1 (en) 2015-12-30
ES2972131T3 (es) 2024-06-11
JP6557331B2 (ja) 2019-08-07
US20170253605A1 (en) 2017-09-07
AU2021204814B2 (en) 2023-07-20
RU2017101829A3 (enExample) 2018-08-30
JP2019196375A (ja) 2019-11-14
JP2021038245A (ja) 2021-03-11
EP3157929A1 (en) 2017-04-26
KR20170033314A (ko) 2017-03-24
JP2017524733A (ja) 2017-08-31
US20220402929A1 (en) 2022-12-22
DK3157929T3 (da) 2024-02-05
AU2014398875A1 (en) 2017-02-02
CA2955415A1 (en) 2015-12-30
RU2017101829A (ru) 2018-07-27

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