CA2955415A1 - Pyrazole compounds as modulators of fshr and uses thereof - Google Patents

Pyrazole compounds as modulators of fshr and uses thereof Download PDF

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Publication number
CA2955415A1
CA2955415A1 CA2955415A CA2955415A CA2955415A1 CA 2955415 A1 CA2955415 A1 CA 2955415A1 CA 2955415 A CA2955415 A CA 2955415A CA 2955415 A CA2955415 A CA 2955415A CA 2955415 A1 CA2955415 A1 CA 2955415A1
Authority
CA
Canada
Prior art keywords
compound
ring
optionally substituted
nitrogen
sulfur
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
Application number
CA2955415A
Other languages
English (en)
French (fr)
Inventor
Henry Yu
Changhe Qi
Paul Tempest
Selvaraj G. NATARAJA
Stephen S. Palmer
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ares Trading SA
Original Assignee
Tocopherx Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Tocopherx Inc filed Critical Tocopherx Inc
Publication of CA2955415A1 publication Critical patent/CA2955415A1/en
Pending 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
    • 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
    • A61K31/42—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)
  • 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)
CA2955415A 2014-06-23 2014-12-22 Pyrazole compounds as modulators of fshr and uses thereof Pending CA2955415A1 (en)

Applications Claiming Priority (3)

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
CNPCT/CN2014/080519 2014-06-23
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
CA2955415A1 true CA2955415A1 (en) 2015-12-30

Family

ID=54936412

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2955415A Pending CA2955415A1 (en) 2014-06-23 2014-12-22 Pyrazole compounds as modulators of fshr and uses thereof

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
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
RU2020124136A (ru) * 2017-12-22 2022-01-25 Хиберселл, Инк. Производные хроменопиридина в качестве ингибиторов фосфатидилинозитолфосфаткиназы
MY208400A (en) 2018-05-03 2025-05-07 Shanghai hengrui pharmaceutical co ltd Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (ror) and pharmaceutical uses thereof
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
CN115835863B (zh) * 2020-07-09 2025-08-12 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
US20230234962A1 (en) 2020-07-29 2023-07-27 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Oxa-azaspiro derivative, and preparation method therefor and pharmaceutical use thereof
IL312114A (en) 2021-10-14 2024-06-01 Incyte Corp Quinoline compounds as Kras inhibitors
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
EP4676591A2 (en) 2023-03-08 2026-01-14 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
EP1307193A1 (en) 2000-07-27 2003-05-07 Affymax Research Institute Agonists of follicle stimulating hormone activity
ES2286275T3 (es) * 2001-09-19 2007-12-01 Pharmacia Corporation Compuestos de pirazolo sustituidos para el tratamiento de la inflamacion.
DE602004028800D1 (en) * 2003-02-07 2010-10-07 Daiichi Sankyo Co Ltd Pyrazolderivat
CA2607882A1 (en) * 2005-05-12 2006-11-23 Wyeth 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
IT1394400B1 (it) * 2009-02-25 2012-06-15 Neuroscienze Pharmaness S C Ar L Composizioni farmaceutiche
IT1393930B1 (it) * 2009-02-25 2012-05-17 Neuroscienze Pharmaness S C A R L Composti farmaceutici
TWI461426B (zh) * 2009-05-27 2014-11-21 Merck Sharp & Dohme （二氫）咪唑並異〔５，１－ａ〕喹啉類
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AU2012279416B2 (en) 2011-07-01 2017-04-06 Merck Patent Gmbh Dihydropyrazoles, pharmaceutical compositions thereof and their use for the treatment of fertility disorders
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WO2015196335A1 (en) 2014-06-23 2015-12-30 Tocopherx, Inc. Pyrazole compounds as modulators of fshr and uses thereof

Also Published As

Publication number Publication date
AU2020201240A1 (en) 2020-03-12
EP3157929A4 (en) 2018-03-07
JP2021038245A (ja) 2021-03-11
MX389867B (es) 2025-03-20
JP6557331B2 (ja) 2019-08-07
AU2021204814B2 (en) 2023-07-20
AU2014398875B2 (en) 2019-11-21
WO2015196759A1 (en) 2015-12-30
AU2021204814A1 (en) 2021-08-05
EP3157929A1 (en) 2017-04-26
RU2017101829A (ru) 2018-07-27
ES2972131T3 (es) 2024-06-11
DK3157929T3 (da) 2024-02-05
AU2014398875A1 (en) 2017-02-02
US20190135823A1 (en) 2019-05-09
KR102416279B1 (ko) 2022-07-01
US20220402929A1 (en) 2022-12-22
EP3157929B1 (en) 2023-12-13
CN106573937B (zh) 2022-02-11
JP2017524733A (ja) 2017-08-31
WO2015196335A1 (en) 2015-12-30
JP2019196375A (ja) 2019-11-14
KR20170033314A (ko) 2017-03-24
MX2017000182A (es) 2017-06-30
US20170253605A1 (en) 2017-09-07
US10208055B2 (en) 2019-02-19
US10941152B2 (en) 2021-03-09
CN106573937A (zh) 2017-04-19
RU2017101829A3 (enExample) 2018-08-30
RU2752173C2 (ru) 2021-07-23

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