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 PDFInfo
- 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
- Authority
- 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
Links
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)
- 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)
- Reproductive Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (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)
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)
| 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 |
| 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 |
| AU2019262169B2 (en) * | 2018-05-03 | 2024-05-02 | Jiangsu Hengrui Medicine Co., Ltd. | Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (RORy) 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 |
| TW202214655A (zh) * | 2020-07-09 | 2022-04-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 氧雜氮雜雙環類衍生物、其製備方法及其在醫藥上的應用 |
| US20230234962A1 (en) | 2020-07-29 | 2023-07-27 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Oxa-azaspiro derivative, and preparation method therefor and pharmaceutical use thereof |
| KR20240101561A (ko) | 2021-10-14 | 2024-07-02 | 인사이트 코포레이션 | Kras의 저해제로서의 퀴놀린 화합물 |
| JP2025527759A (ja) * | 2022-08-26 | 2025-08-22 | セルマティクス インク. | Fshrの新規なモジュレータおよびその使用 |
| 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 |
| AU2024231935A1 (en) | 2023-03-08 | 2025-07-17 | 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 |
| WO2002009706A1 (en) | 2000-07-27 | 2002-02-07 | Smithkline Beecham Corporation | Agonists of follicle stimulating hormone activity |
| BR0212617A (pt) * | 2001-09-19 | 2005-02-09 | Pharmacia Corp | Compostos de pirazolila substituìdo para o tratamento de inflamação |
| RU2332412C2 (ru) | 2003-02-07 | 2008-08-27 | Дайити Фармасьютикал Ко., Лтд. | Производные пиразола |
| 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 |
| 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 |
| CN102695710B (zh) * | 2009-11-13 | 2015-08-19 | 默克雪兰诺有限公司 | 三环吡唑胺衍生物 |
| EP2726463B1 (en) | 2011-07-01 | 2020-03-11 | Merck Patent GmbH | Dihydropyrazoles, pharmaceutical compositions thereof and their use for the treatment of fertility disorders |
| JP6162694B2 (ja) | 2011-07-18 | 2017-07-12 | 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 | ベンズアミド類 |
| WO2013106409A1 (en) | 2012-01-10 | 2013-07-18 | Merck Patent Gmbh | Benzamide derivatives as modulators of the follicle stimulating hormone |
| MX2014009416A (es) | 2012-02-08 | 2014-11-10 | Merck Patent Gmbh | Analogos de tiazolidinona deuterados como agonistas para el receptor de la hormana foliculo estimulante. |
| 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 CA CA2955415A patent/CA2955415A1/en active Pending
- 2014-12-22 MX MX2017000182A patent/MX389867B/es unknown
- 2014-12-22 WO PCT/CN2014/094459 patent/WO2015196759A1/en not_active Ceased
- 2014-12-22 AU AU2014398875A patent/AU2014398875B2/en not_active Ceased
- 2014-12-22 JP JP2017519756A patent/JP6557331B2/ja active Active
- 2014-12-22 RU RU2017101829A patent/RU2752173C2/ru active
- 2014-12-22 US US15/321,249 patent/US10208055B2/en active Active
- 2014-12-22 DK DK14896199.8T patent/DK3157929T3/da active
- 2014-12-22 KR KR1020177001959A patent/KR102416279B1/ko active Active
- 2014-12-22 CN CN201480081442.1A patent/CN106573937B/zh active Active
- 2014-12-22 EP EP14896199.8A patent/EP3157929B1/en active Active
- 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
Also Published As
| Publication number | Publication date |
|---|---|
| CN106573937A (zh) | 2017-04-19 |
| JP2019196375A (ja) | 2019-11-14 |
| DK3157929T3 (da) | 2024-02-05 |
| US20220402929A1 (en) | 2022-12-22 |
| AU2020201240A1 (en) | 2020-03-12 |
| AU2014398875A1 (en) | 2017-02-02 |
| CN106573937B (zh) | 2022-02-11 |
| US10208055B2 (en) | 2019-02-19 |
| JP2017524733A (ja) | 2017-08-31 |
| US20170253605A1 (en) | 2017-09-07 |
| MX389867B (es) | 2025-03-20 |
| RU2752173C2 (ru) | 2021-07-23 |
| JP6557331B2 (ja) | 2019-08-07 |
| KR20170033314A (ko) | 2017-03-24 |
| EP3157929A1 (en) | 2017-04-26 |
| JP2021038245A (ja) | 2021-03-11 |
| EP3157929B1 (en) | 2023-12-13 |
| WO2015196335A1 (en) | 2015-12-30 |
| US20190135823A1 (en) | 2019-05-09 |
| AU2021204814B2 (en) | 2023-07-20 |
| CA2955415A1 (en) | 2015-12-30 |
| RU2017101829A (ru) | 2018-07-27 |
| KR102416279B1 (ko) | 2022-07-01 |
| EP3157929A4 (en) | 2018-03-07 |
| WO2015196759A1 (en) | 2015-12-30 |
| RU2017101829A3 (enExample) | 2018-08-30 |
| AU2021204814A1 (en) | 2021-08-05 |
| US10941152B2 (en) | 2021-03-09 |
| AU2014398875B2 (en) | 2019-11-21 |
| MX2017000182A (es) | 2017-06-30 |
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