ES2721018T3 - N-Acil-(3-sustituido)-(8-metil)-5,6-dihidro-[1,2,4]triazolo[4,3-a]pirazinas como antagonistas selectivos del receptor NK-3, composición farmacéutica, métodos para su uso en trastornos mediados por el receptor de NK-3 - Google Patents
N-Acil-(3-sustituido)-(8-metil)-5,6-dihidro-[1,2,4]triazolo[4,3-a]pirazinas como antagonistas selectivos del receptor NK-3, composición farmacéutica, métodos para su uso en trastornos mediados por el receptor de NK-3 Download PDFInfo
- Publication number
- ES2721018T3 ES2721018T3 ES14713847T ES14713847T ES2721018T3 ES 2721018 T3 ES2721018 T3 ES 2721018T3 ES 14713847 T ES14713847 T ES 14713847T ES 14713847 T ES14713847 T ES 14713847T ES 2721018 T3 ES2721018 T3 ES 2721018T3
- Authority
- ES
- Spain
- Prior art keywords
- receptor
- methyl
- pyrazines
- triazolo
- dihydro
- 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.)
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Links
- 102000002003 Neurokinin-3 Receptors Human genes 0.000 title 2
- 108010040716 Neurokinin-3 Receptors Proteins 0.000 title 2
- 230000001404 mediated effect Effects 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000002464 receptor antagonist Substances 0.000 title 1
- 229940044551 receptor antagonist Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A61P15/18—Feminine contraceptives
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- A—HUMAN NECESSITIES
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- 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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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/26—Androgens
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- A—HUMAN NECESSITIES
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- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Reproductive Health (AREA)
- Dermatology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Gynecology & Obstetrics (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Otolaryngology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Pregnancy & Childbirth (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Un compuesto de Fórmula I:**Fórmula** o un solvato farmacéuticamente aceptable del mismo, en donde: R1 es H o F; R1' es H; R2 es H, F o Cl; R2' es H o F; R3 es F o Cl; R4 es metilo o trifluorometilo; X1 es S y X2 es N o X1 es CH y X2 es O; representa un enlace simple o doble dependiendo de X1 y X2; representa el enantiómero (R) o el racemato del compuesto de Fórmula I.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13161866 | 2013-03-29 | ||
| PCT/EP2014/056372 WO2014154897A1 (en) | 2013-03-29 | 2014-03-28 | NOVEL N-ACYL-(3-SUBSTITUTED)-(8-METHYL)-5,6-DIHYDRO-[1,2,4]TRIAZOLO[4,3-a]PYRAZINES AS SELECTIVE NK-3 RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITION, METHODS FOR USE IN NK-3 RECEPTOR-MEDIATED DISORDERS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2721018T3 true ES2721018T3 (es) | 2019-07-26 |
Family
ID=47997278
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES14713847T Active ES2721018T3 (es) | 2013-03-29 | 2014-03-28 | N-Acil-(3-sustituido)-(8-metil)-5,6-dihidro-[1,2,4]triazolo[4,3-a]pirazinas como antagonistas selectivos del receptor NK-3, composición farmacéutica, métodos para su uso en trastornos mediados por el receptor de NK-3 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US9840508B2 (es) |
| EP (1) | EP2989103B1 (es) |
| JP (1) | JP6275242B2 (es) |
| AU (1) | AU2014242908B2 (es) |
| CA (1) | CA2907814C (es) |
| ES (1) | ES2721018T3 (es) |
| WO (1) | WO2014154897A1 (es) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2552920T3 (pl) | 2010-04-02 | 2017-08-31 | Ogeda Sa | Nowe wybiórcze związki antagonistów receptora NK-3, farmaceutyczne kompozycje i sposoby do zastosowania w zaburzeniach pośredniczonych przez receptory NK-3 |
| DK2763992T3 (en) | 2011-10-03 | 2016-04-25 | Euroscreen Sa | NOVEL CHIRAL N-acyl-5,6,7, (8-substituted) -tetrahydro [1,2,4] triazolo [4,3-a] pyrazines as selective NK-3 receptor antagonists, PHARMACEUTICAL COMPOSITION AND METHODS FOR THE use in the NK-3 receptor mediated diseases |
| US9604982B2 (en) | 2013-03-14 | 2017-03-28 | Janssen Pharmaceutica Nv | P2X7 modulators |
| TWI644671B (zh) | 2013-03-14 | 2018-12-21 | 比利時商健生藥品公司 | P2x7調節劑 |
| JO3509B1 (ar) | 2013-03-14 | 2020-07-05 | Janssen Pharmaceutica Nv | معدلات p2x7 |
| US9040534B2 (en) | 2013-03-14 | 2015-05-26 | Janssen Pharmaceutica Nv | [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators |
| US10183948B2 (en) | 2013-03-29 | 2019-01-22 | Ogeda Sa | N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists |
| SG11201508005XA (en) | 2013-03-29 | 2015-10-29 | Euroscreen Sa | NOVEL N-ACYL-(3-SUBSTITUTED)-(8-SUBSTITUTED)-5,6-DIHYDRO- [1,2,4]TRIAZOLO[4,3-a]PYRAZINES AS SELECTIVE NK-3 RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITION, METHODS FOR USE IN NK-3 RECEPTOR-MEDIATED DISORDERS |
| AU2015315693B2 (en) * | 2014-09-12 | 2020-01-16 | Janssen Pharmaceutica Nv | P2X7 modulating n-acyl-triazolopyrazines |
| WO2016039977A1 (en) | 2014-09-12 | 2016-03-17 | Janssen Pharmaceutica Nv | P2x7 modulators |
| WO2016046398A1 (en) | 2014-09-25 | 2016-03-31 | Euroscreen Sa | Novel chiral synthesis of n-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines |
| ES2965675T3 (es) | 2015-03-16 | 2024-04-16 | Ogeda N V | Antagonistas del receptor NK-3 para el tratamiento terapéutico o cosmético del exceso de grasa corporal |
| JP2021014404A (ja) * | 2017-10-13 | 2021-02-12 | アステラス製薬株式会社 | トリアゾロピラジン誘導体の塩及び結晶 |
| KR20210069079A (ko) | 2018-09-28 | 2021-06-10 | 얀센 파마슈티카 엔.브이. | 모노아실글리세롤 리파아제 조절제 |
| MY205440A (en) | 2018-09-28 | 2024-10-21 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| JP7644009B2 (ja) | 2018-12-21 | 2025-03-11 | オゲダ エス.エー. | 3-メチル-1,2,4-チアジアゾール-5-カルボヒドラジドまたはそのメチル-d3重水素化形態の合成 |
| CN112272670B (zh) * | 2019-04-16 | 2023-12-12 | 上海翰森生物医药科技有限公司 | 含二并环类衍生物抑制剂、其制备方法和应用 |
| JP7697934B2 (ja) | 2019-09-30 | 2025-06-24 | ヤンセン ファーマシューティカ エヌ.ベー. | 放射線標識されたmgl petリガンド |
| BR112022019077A2 (pt) | 2020-03-26 | 2022-12-27 | Janssen Pharmaceutica Nv | Moduladores da monoacilglicerol lipase |
| KR20230044443A (ko) * | 2020-07-30 | 2023-04-04 | 상하이 한서 바이오메디컬 컴퍼니 리미티드 | 질소-함유 융합된 고리 유도체 억제제, 이의 제조 방법 및 이의 용도 |
| WO2022243430A1 (en) * | 2021-05-20 | 2022-11-24 | Plus Vitech, S.L. | Treatment of acne |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000043008A1 (en) | 1999-01-25 | 2000-07-27 | Smithkline Beecham Corporation | Anti-androgens and methods for treating disease |
| CA2478389A1 (en) | 2002-03-25 | 2003-10-09 | Merck & Co., Inc. | Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| MY139563A (en) | 2002-09-04 | 2009-10-30 | Bristol Myers Squibb Co | Heterocyclic aromatic compounds useful as growth hormone secretagogues |
| AU2004277932B2 (en) | 2003-09-30 | 2009-07-16 | Merck & Co., Inc. | Phenyl pyrrolidine ether tachykinin receptor antagonists |
| DE602005008558D1 (de) | 2004-02-18 | 2008-09-11 | Astrazeneca Ab | Kondensierte heterocyclische verbindungen und deren verwendung als antagonisten des metabotropen reznkungen |
| GB0509405D0 (en) | 2005-05-10 | 2005-06-15 | Merck Sharp & Dohme | Therapeutic compounds |
| GB0610680D0 (en) | 2006-05-31 | 2006-07-12 | Istituto Di Ricerche D Biolog | Therapeutic compounds |
| CA2666469A1 (en) * | 2006-09-01 | 2008-03-06 | Bayer Healthcare Ag | Benzofuran and benzothiophene derivatives useful in the treatment of cancers of the central nervous system |
| US7943617B2 (en) | 2006-11-27 | 2011-05-17 | Bristol-Myers Squibb Company | Heterobicyclic compounds useful as kinase inhibitors |
| EP2090576A1 (en) * | 2008-02-01 | 2009-08-19 | Merz Pharma GmbH & Co.KGaA | 6-halo-pyrazolo[1,5-a]pyridines, a process for their preparation and their use as metabotropic glutamate receptor (mGluR) modulators |
| EP2085398A1 (en) | 2008-02-01 | 2009-08-05 | Merz Pharma GmbH & Co. KGaA | Pyrazolopyrimidines, a process for their preparation and their use as medicine |
| US20100093721A1 (en) * | 2008-10-13 | 2010-04-15 | Barbay J Kent | PHENYL AND HETEROARYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINES AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| JP5654001B2 (ja) * | 2009-04-29 | 2015-01-14 | グラクソ グループ リミテッドGlaxo Group Limited | P2X7調節因子としての5,6,7,8−テトラヒドロ[1,2,4]トリアゾロ[4,3−a]ピラジン誘導体 |
| GB0907515D0 (en) | 2009-04-30 | 2009-06-10 | Glaxo Group Ltd | Compounds |
| PL2552920T3 (pl) * | 2010-04-02 | 2017-08-31 | Ogeda Sa | Nowe wybiórcze związki antagonistów receptora NK-3, farmaceutyczne kompozycje i sposoby do zastosowania w zaburzeniach pośredniczonych przez receptory NK-3 |
| US10065960B2 (en) | 2010-04-02 | 2018-09-04 | Ogeda Sa | NK-3 receptor selective antagonist compounds, pharmaceutical composition and methods for use in NK-3 receptors mediated disorders |
| DK2763992T3 (en) | 2011-10-03 | 2016-04-25 | Euroscreen Sa | NOVEL CHIRAL N-acyl-5,6,7, (8-substituted) -tetrahydro [1,2,4] triazolo [4,3-a] pyrazines as selective NK-3 receptor antagonists, PHARMACEUTICAL COMPOSITION AND METHODS FOR THE use in the NK-3 receptor mediated diseases |
| SG11201508005XA (en) | 2013-03-29 | 2015-10-29 | Euroscreen Sa | NOVEL N-ACYL-(3-SUBSTITUTED)-(8-SUBSTITUTED)-5,6-DIHYDRO- [1,2,4]TRIAZOLO[4,3-a]PYRAZINES AS SELECTIVE NK-3 RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITION, METHODS FOR USE IN NK-3 RECEPTOR-MEDIATED DISORDERS |
-
2014
- 2014-03-28 CA CA2907814A patent/CA2907814C/en active Active
- 2014-03-28 WO PCT/EP2014/056372 patent/WO2014154897A1/en not_active Ceased
- 2014-03-28 EP EP14713847.3A patent/EP2989103B1/en active Active
- 2014-03-28 AU AU2014242908A patent/AU2014242908B2/en active Active
- 2014-03-28 US US14/777,543 patent/US9840508B2/en active Active
- 2014-03-28 ES ES14713847T patent/ES2721018T3/es active Active
- 2014-03-28 JP JP2016504707A patent/JP6275242B2/ja active Active
-
2017
- 2017-11-09 US US15/807,733 patent/US9969745B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EP2989103A1 (en) | 2016-03-02 |
| US20160289233A1 (en) | 2016-10-06 |
| WO2014154897A1 (en) | 2014-10-02 |
| JP2016516741A (ja) | 2016-06-09 |
| US9840508B2 (en) | 2017-12-12 |
| AU2014242908A1 (en) | 2015-10-22 |
| HK1218546A1 (en) | 2017-02-24 |
| CA2907814A1 (en) | 2014-10-02 |
| EP2989103B1 (en) | 2019-02-20 |
| US9969745B2 (en) | 2018-05-15 |
| AU2014242908B2 (en) | 2018-07-19 |
| US20180065972A1 (en) | 2018-03-08 |
| CA2907814C (en) | 2021-07-13 |
| JP6275242B2 (ja) | 2018-02-07 |
| AU2014242908A2 (en) | 2015-10-22 |
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