CN106573937B - 作为fshr调节剂的吡唑化合物及其用途 - Google Patents

作为fshr调节剂的吡唑化合物及其用途 Download PDF

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Publication number
CN106573937B
CN106573937B CN201480081442.1A CN201480081442A CN106573937B CN 106573937 B CN106573937 B CN 106573937B CN 201480081442 A CN201480081442 A CN 201480081442A CN 106573937 B CN106573937 B CN 106573937B
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China
Prior art keywords
compound
methyl
certain embodiments
methoxy
dihydrobenzopyrano
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Expired - Fee Related
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CN201480081442.1A
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English (en)
Chinese (zh)
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CN106573937A (zh
Inventor
H.余
C.齐
P.坦派斯特
S.G.纳塔拉贾
S.S.帕尔默
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Ares Trading SA
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Ares Trading SA
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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)
  • 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)
CN201480081442.1A 2014-06-23 2014-12-22 作为fshr调节剂的吡唑化合物及其用途 Expired - Fee Related CN106573937B (zh)

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 (2)

Publication Number Publication Date
CN106573937A CN106573937A (zh) 2017-04-19
CN106573937B true CN106573937B (zh) 2022-02-11

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

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
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
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
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
AU2018392816B2 (en) * 2017-12-22 2023-04-20 HiberCell Inc. Chromenopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
JP7351851B2 (ja) 2018-05-03 2023-09-27 ジエンス ヘンルイ メデイシンカンパニー リミテッド レチノイド関連オルファン受容体ガンマ（ＲＯＲγ）のモジュレーターとしてのベンジイミダゾール誘導体およびそれらの医薬品用途
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
CA3186193A1 (en) * 2020-07-29 2022-02-03 Biao Lu Oxa-azaspiro derivative, and preparation method therefor and pharmaceutical use thereof
PE20242113A1 (es) 2021-10-14 2024-10-28 Incyte Corp Compuestos de quinolina como inhibidores de kras
EP4577206A2 (en) * 2022-08-26 2025-07-02 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
CN120693335A (zh) 2023-03-08 2025-09-23 辉凌公司 小分子fsh受体调节剂
WO2024263803A2 (en) * 2023-06-21 2024-12-26 Celmatix Inc. Novel modulators of fshr and uses thereof

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1039026A (zh) * 1988-06-20 1990-01-24 法米塔利亚·卡洛·埃巴有限责任公司 制备三环的3-氧代-丙腈衍生物的方法
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
CN102695710A (zh) * 2009-11-13 2012-09-26 默克雪兰诺有限公司 三环吡唑胺衍生物
CN105473596A (zh) * 2013-06-24 2016-04-06 默克专利有限公司 用作卵泡刺激素受体调节剂的吡唑化合物及其用途

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004505051A (ja) 2000-07-27 2004-02-19 スミスクライン　ビーチャム　コーポレーション 卵胞刺激ホルモン活性のアゴニスト
KR20050096956A (ko) * 2003-02-07 2005-10-06 다이이찌 세이야꾸 가부시기가이샤 피라졸 유도체
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
TWI461426B (zh) * 2009-05-27 2014-11-21 Merck Sharp & Dohme （二氫）咪唑並異〔５，１－ａ〕喹啉類
CN103827091B (zh) 2011-07-01 2016-05-18 默克专利有限公司 二氢吡唑、其药物组合物及其治疗生育障碍的用途
ES2899000T3 (es) 2011-07-18 2022-03-09 Merck Patent Gmbh Benzamidas
AU2013208082B2 (en) 2012-01-10 2017-07-20 Merck Patent Gmbh Benzamide derivatives as modulators of the follicle stimulating hormone
BR112014019351A8 (pt) 2012-02-08 2017-07-11 Merck Patent Gmbh Análogos de tiazolidinona deuterados como agonistas para o receptor do hormônio folículo estimulante
ES2657979T3 (es) 2013-06-24 2018-03-07 Merck Patent Gmbh Compuestos de imidazol como moduladores de FSHR y sus usos
WO2015196335A1 (en) 2014-06-23 2015-12-30 Tocopherx, Inc. Pyrazole compounds as modulators of fshr and uses thereof

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1039026A (zh) * 1988-06-20 1990-01-24 法米塔利亚·卡洛·埃巴有限责任公司 制备三环的3-氧代-丙腈衍生物的方法
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
CN102695710A (zh) * 2009-11-13 2012-09-26 默克雪兰诺有限公司 三环吡唑胺衍生物
CN105473596A (zh) * 2013-06-24 2016-04-06 默克专利有限公司 用作卵泡刺激素受体调节剂的吡唑化合物及其用途

Also Published As

Publication number Publication date
DK3157929T3 (da) 2024-02-05
RU2017101829A (ru) 2018-07-27
CA2955415A1 (en) 2015-12-30
RU2017101829A3 (OSRAM) 2018-08-30
JP2019196375A (ja) 2019-11-14
EP3157929A1 (en) 2017-04-26
WO2015196759A1 (en) 2015-12-30
WO2015196335A1 (en) 2015-12-30
RU2752173C2 (ru) 2021-07-23
KR20170033314A (ko) 2017-03-24
US20190135823A1 (en) 2019-05-09
EP3157929B1 (en) 2023-12-13
ES2972131T3 (es) 2024-06-11
JP6557331B2 (ja) 2019-08-07
EP3157929A4 (en) 2018-03-07
AU2014398875A1 (en) 2017-02-02
US20170253605A1 (en) 2017-09-07
US20220402929A1 (en) 2022-12-22
JP2021038245A (ja) 2021-03-11
MX389867B (es) 2025-03-20
AU2021204814B2 (en) 2023-07-20
JP2017524733A (ja) 2017-08-31
CN106573937A (zh) 2017-04-19
AU2020201240A1 (en) 2020-03-12
US10941152B2 (en) 2021-03-09
US10208055B2 (en) 2019-02-19
AU2014398875B2 (en) 2019-11-21
AU2021204814A1 (en) 2021-08-05
KR102416279B1 (ko) 2022-07-01
MX2017000182A (es) 2017-06-30

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