JP6557331B2 - Fshrのモジュレータとしてのピラゾール化合物およびその使用 - Google Patents
Fshrのモジュレータとしてのピラゾール化合物およびその使用 Download PDFInfo
- Publication number
- JP6557331B2 JP6557331B2 JP2017519756A JP2017519756A JP6557331B2 JP 6557331 B2 JP6557331 B2 JP 6557331B2 JP 2017519756 A JP2017519756 A JP 2017519756A JP 2017519756 A JP2017519756 A JP 2017519756A JP 6557331 B2 JP6557331 B2 JP 6557331B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- methyl
- certain embodiments
- methoxy
- nitrogen
- 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.)
- Expired - Fee Related
Links
Classifications
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Reproductive Health (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019129171A Division JP2019196375A (ja) | 2014-06-23 | 2019-07-11 | Fshrのモジュレータとしてのピラゾール化合物およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017524733A JP2017524733A (ja) | 2017-08-31 |
| JP2017524733A5 JP2017524733A5 (https=) | 2018-01-18 |
| JP6557331B2 true JP6557331B2 (ja) | 2019-08-07 |
Family
ID=54936412
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017519756A Expired - Fee Related JP6557331B2 (ja) | 2014-06-23 | 2014-12-22 | Fshrのモジュレータとしてのピラゾール化合物およびその使用 |
| JP2019129171A Pending JP2019196375A (ja) | 2014-06-23 | 2019-07-11 | Fshrのモジュレータとしてのピラゾール化合物およびその使用 |
| JP2020191715A Pending JP2021038245A (ja) | 2014-06-23 | 2020-11-18 | Fshrのモジュレータとしてのピラゾール化合物およびその使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019129171A Pending JP2019196375A (ja) | 2014-06-23 | 2019-07-11 | Fshrのモジュレータとしてのピラゾール化合物およびその使用 |
| JP2020191715A Pending JP2021038245A (ja) | 2014-06-23 | 2020-11-18 | Fshrのモジュレータとしてのピラゾール化合物およびその使用 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US10208055B2 (https=) |
| EP (1) | EP3157929B1 (https=) |
| JP (3) | JP6557331B2 (https=) |
| KR (1) | KR102416279B1 (https=) |
| CN (1) | CN106573937B (https=) |
| AU (3) | AU2014398875B2 (https=) |
| CA (1) | CA2955415A1 (https=) |
| DK (1) | DK3157929T3 (https=) |
| ES (1) | ES2972131T3 (https=) |
| MX (1) | MX389867B (https=) |
| RU (1) | RU2752173C2 (https=) |
| WO (2) | WO2015196335A1 (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021038245A (ja) * | 2014-06-23 | 2021-03-11 | アレス トレーディング ソシエテ アノニム | Fshrのモジュレータとしてのピラゾール化合物およびその使用 |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| ES2971712T3 (es) * | 2017-12-22 | 2024-06-06 | Hibercell Inc | Derivados de cromenopiridina como inhibidores de la fosfatidilinositol fosfato cinasa |
| 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 |
| 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 |
| TW202214656A (zh) * | 2020-07-29 | 2022-04-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 氧氮雜環螺環衍生物、其製備方法及其醫藥用途 |
| WO2023064857A1 (en) | 2021-10-14 | 2023-04-20 | Incyte Corporation | Quinoline compounds as inhibitors of kras |
| IL319132A (en) * | 2022-08-26 | 2025-04-01 | Celmatix Inc | New FSHR modulators and their uses |
| 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 |
| 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 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| ATE363473T1 (de) * | 2001-09-19 | 2007-06-15 | Pharmacia Corp | Substituierte pyrazoloverbindungen zur behandlung von entzündungen |
| KR20050096956A (ko) | 2003-02-07 | 2005-10-06 | 다이이찌 세이야꾸 가부시기가이샤 | 피라졸 유도체 |
| US7687623B2 (en) * | 2005-05-12 | 2010-03-30 | Wyeth Llc | 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 |
| IT1393930B1 (it) * | 2009-02-25 | 2012-05-17 | Neuroscienze Pharmaness S C A R L | Composti farmaceutici |
| IT1394400B1 (it) * | 2009-02-25 | 2012-06-15 | Neuroscienze Pharmaness S C Ar L | Composizioni farmaceutiche |
| TWI461426B (zh) * | 2009-05-27 | 2014-11-21 | Merck Sharp & Dohme | (二氫)咪唑並異〔5,1-a〕喹啉類 |
| KR20130049766A (ko) * | 2009-11-13 | 2013-05-14 | 메르크 세로노 에스. 에이. | 트리사이클릭 피라졸 아민 유도체 |
| CA2837524C (en) | 2011-07-01 | 2019-08-20 | Merck Patent Gmbh | Dihydropyrazoles |
| EP2734517B1 (en) | 2011-07-18 | 2017-08-30 | Merck Patent GmbH | Benzamides |
| WO2013106409A1 (en) | 2012-01-10 | 2013-07-18 | Merck Patent Gmbh | Benzamide derivatives as modulators of the follicle stimulating hormone |
| EP2812320B1 (en) | 2012-02-08 | 2018-03-07 | Merck Patent GmbH | Deuterated thiazolidinone analogues as agonists for follicle stimulating hormone receptor |
| WO2014209980A1 (en) * | 2013-06-24 | 2014-12-31 | Merck Patent Gmbh | Pyrazole compounds as modulators of fshr and uses thereof |
| JP6523267B2 (ja) | 2013-06-24 | 2019-05-29 | 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の調節剤としてのイミダ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 |
-
2014
- 2014-06-23 WO PCT/CN2014/080519 patent/WO2015196335A1/en not_active Ceased
- 2014-12-22 DK DK14896199.8T patent/DK3157929T3/da active
- 2014-12-22 CA CA2955415A patent/CA2955415A1/en active Pending
- 2014-12-22 US US15/321,249 patent/US10208055B2/en active Active
- 2014-12-22 MX MX2017000182A patent/MX389867B/es unknown
- 2014-12-22 KR KR1020177001959A patent/KR102416279B1/ko not_active Expired - Fee Related
- 2014-12-22 EP EP14896199.8A patent/EP3157929B1/en active Active
- 2014-12-22 JP JP2017519756A patent/JP6557331B2/ja not_active Expired - Fee Related
- 2014-12-22 WO PCT/CN2014/094459 patent/WO2015196759A1/en not_active Ceased
- 2014-12-22 RU RU2017101829A patent/RU2752173C2/ru active
- 2014-12-22 AU AU2014398875A patent/AU2014398875B2/en not_active Ceased
- 2014-12-22 CN CN201480081442.1A patent/CN106573937B/zh not_active Expired - Fee Related
- 2014-12-22 ES ES14896199T patent/ES2972131T3/es active Active
-
2018
- 2018-12-21 US US16/229,119 patent/US10941152B2/en not_active Expired - Fee Related
-
2019
- 2019-07-11 JP JP2019129171A patent/JP2019196375A/ja active Pending
-
2020
- 2020-02-20 AU AU2020201240A patent/AU2020201240A1/en not_active Abandoned
- 2020-11-18 JP JP2020191715A patent/JP2021038245A/ja active Pending
-
2021
- 2021-01-05 US US17/141,621 patent/US20220402929A1/en not_active Abandoned
- 2021-07-09 AU AU2021204814A patent/AU2021204814B2/en not_active Ceased
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021038245A (ja) * | 2014-06-23 | 2021-03-11 | アレス トレーディング ソシエテ アノニム | Fshrのモジュレータとしてのピラゾール化合物およびその使用 |
Also Published As
| Publication number | Publication date |
|---|---|
| RU2017101829A (ru) | 2018-07-27 |
| EP3157929B1 (en) | 2023-12-13 |
| EP3157929A1 (en) | 2017-04-26 |
| KR102416279B1 (ko) | 2022-07-01 |
| AU2014398875B2 (en) | 2019-11-21 |
| WO2015196335A1 (en) | 2015-12-30 |
| RU2017101829A3 (https=) | 2018-08-30 |
| US10941152B2 (en) | 2021-03-09 |
| AU2020201240A1 (en) | 2020-03-12 |
| RU2752173C2 (ru) | 2021-07-23 |
| US20220402929A1 (en) | 2022-12-22 |
| WO2015196759A1 (en) | 2015-12-30 |
| MX2017000182A (es) | 2017-06-30 |
| KR20170033314A (ko) | 2017-03-24 |
| JP2017524733A (ja) | 2017-08-31 |
| US20170253605A1 (en) | 2017-09-07 |
| CN106573937B (zh) | 2022-02-11 |
| EP3157929A4 (en) | 2018-03-07 |
| AU2021204814A1 (en) | 2021-08-05 |
| ES2972131T3 (es) | 2024-06-11 |
| JP2019196375A (ja) | 2019-11-14 |
| CN106573937A (zh) | 2017-04-19 |
| MX389867B (es) | 2025-03-20 |
| AU2021204814B2 (en) | 2023-07-20 |
| JP2021038245A (ja) | 2021-03-11 |
| US20190135823A1 (en) | 2019-05-09 |
| CA2955415A1 (en) | 2015-12-30 |
| US10208055B2 (en) | 2019-02-19 |
| DK3157929T3 (da) | 2024-02-05 |
| AU2014398875A1 (en) | 2017-02-02 |
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