ES2972131T3 - Compuestos de pirazol como moduladores de FSHR y usos de los mismos - Google Patents

Compuestos de pirazol como moduladores de FSHR y usos de los mismos Download PDF

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Publication number
ES2972131T3
ES2972131T3 ES14896199T ES14896199T ES2972131T3 ES 2972131 T3 ES2972131 T3 ES 2972131T3 ES 14896199 T ES14896199 T ES 14896199T ES 14896199 T ES14896199 T ES 14896199T ES 2972131 T3 ES2972131 T3 ES 2972131T3
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ES
Spain
Prior art keywords
compound
pyrazole
methyl
methoxy
mmol
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.)
Active
Application number
ES14896199T
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English (en)
Spanish (es)
Inventor
Henry Yu
changhe Qi
Paul Tempest
Selvaraj G Nataraja
Stephen S Palmer
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Ares Trading SA
Original Assignee
Ares Trading SA
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Filing date
Publication date
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Publication of ES2972131T3 publication Critical patent/ES2972131T3/es
Active legal-status Critical Current
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Classifications

    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Reproductive Health (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
ES14896199T 2014-06-23 2014-12-22 Compuestos de pirazol como moduladores de FSHR y usos de los mismos Active ES2972131T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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 (1)

Publication Number Publication Date
ES2972131T3 true ES2972131T3 (es) 2024-06-11

Family

ID=54936412

Family Applications (1)

Application Number Title Priority Date Filing Date
ES14896199T Active ES2972131T3 (es) 2014-06-23 2014-12-22 Compuestos de pirazol como moduladores de FSHR y usos de los mismos

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)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015196335A1 (en) 2014-06-23 2015-12-30 Tocopherx, Inc. Pyrazole compounds as modulators of fshr and uses thereof
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
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
CN111936484A (zh) * 2017-12-22 2020-11-13 拉文纳制药公司 作为磷脂酰肌醇磷酸激酶抑制剂的色烯并吡啶衍生物
SMT202300212T1 (it) * 2018-05-03 2023-09-06 Shanghai hengrui pharmaceutical co ltd Derivati di benzimidazolo come modulatori del recettore gamma orfano correlato al retinoide (rory) e usi farmaceutici di essi
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
WO2022022630A1 (zh) 2020-07-29 2022-02-03 江苏恒瑞医药股份有限公司 氧杂氮杂螺环类衍生物、其制备方法及其在医药上的应用
KR20240101561A (ko) 2021-10-14 2024-07-02 인사이트 코포레이션 Kras의 저해제로서의 퀴놀린 화합물
EP4577206A2 (en) * 2022-08-26 2025-07-02 Celmatix Inc. Novel modulators of fshr and uses thereof
WO2024077006A1 (en) * 2022-10-05 2024-04-11 Radionetics Oncology, Inc. Follicle-stimulating hormone receptor (fshr) targeted therapeutics and uses thereof
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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GB8814586D0 (en) * 1988-06-20 1988-07-27 Erba Carlo Spa Tricyclic 3-oxo-propanenitrile derivatives & process for their preparation
WO2002009706A1 (en) 2000-07-27 2002-02-07 Smithkline Beecham Corporation Agonists of follicle stimulating hormone activity
CA2460939C (en) * 2001-09-19 2008-07-29 Pharmacia Corporation Substituted pyrazolyl compounds for the treatment of inflammation
RU2332412C2 (ru) 2003-02-07 2008-08-27 Дайити Фармасьютикал Ко., Лтд. Производные пиразола
EP1879898A2 (en) * 2005-05-12 2008-01-23 Wyeth a Corporation of the State of Delaware Pyrrolobenzodiazepines and heterocyclic carboxamide derivatives as follicle stimulating hormone receptor (fsh-r) antagonists
WO2008035356A2 (en) * 2006-09-20 2008-03-27 Glenmark Pharmaceuticals Limited Novel cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation
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JP6170043B2 (ja) 2011-07-01 2017-07-26 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 ジヒドロピラゾール
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Also Published As

Publication number Publication date
RU2752173C2 (ru) 2021-07-23
WO2015196759A1 (en) 2015-12-30
EP3157929A4 (en) 2018-03-07
CA2955415A1 (en) 2015-12-30
AU2021204814A1 (en) 2021-08-05
US20220402929A1 (en) 2022-12-22
AU2014398875A1 (en) 2017-02-02
MX389867B (es) 2025-03-20
KR20170033314A (ko) 2017-03-24
AU2020201240A1 (en) 2020-03-12
EP3157929A1 (en) 2017-04-26
US10208055B2 (en) 2019-02-19
JP2019196375A (ja) 2019-11-14
DK3157929T3 (da) 2024-02-05
US10941152B2 (en) 2021-03-09
JP2021038245A (ja) 2021-03-11
JP2017524733A (ja) 2017-08-31
KR102416279B1 (ko) 2022-07-01
CN106573937B (zh) 2022-02-11
CN106573937A (zh) 2017-04-19
EP3157929B1 (en) 2023-12-13
MX2017000182A (es) 2017-06-30
US20170253605A1 (en) 2017-09-07
JP6557331B2 (ja) 2019-08-07
RU2017101829A3 (enExample) 2018-08-30
RU2017101829A (ru) 2018-07-27
AU2014398875B2 (en) 2019-11-21
AU2021204814B2 (en) 2023-07-20
WO2015196335A1 (en) 2015-12-30
US20190135823A1 (en) 2019-05-09

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