MX2015015893A - 2-fenilimidazo[1,2-a]pirimidinas como agentes formadores de imagen. - Google Patents
2-fenilimidazo[1,2-a]pirimidinas como agentes formadores de imagen.Info
- Publication number
- MX2015015893A MX2015015893A MX2015015893A MX2015015893A MX2015015893A MX 2015015893 A MX2015015893 A MX 2015015893A MX 2015015893 A MX2015015893 A MX 2015015893A MX 2015015893 A MX2015015893 A MX 2015015893A MX 2015015893 A MX2015015893 A MX 2015015893A
- Authority
- MX
- Mexico
- Prior art keywords
- lower alkyl
- halogen
- ch2ch2
- substituted
- alkyl substituted
- Prior art date
Links
- ONYRUSCZUWEZDP-UHFFFAOYSA-N 2-phenylimidazo[1,2-a]pyrimidine Chemical class N1=C2N=CC=CN2C=C1C1=CC=CC=C1 ONYRUSCZUWEZDP-UHFFFAOYSA-N 0.000 title 1
- 239000012216 imaging agent Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 11
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 125000005843 halogen group Chemical group 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- JYGFTBXVXVMTGB-UHFFFAOYSA-N indolin-2-one Chemical compound C1=CC=C2NC(=O)CC2=C1 JYGFTBXVXVMTGB-UHFFFAOYSA-N 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- XCUAIINAJCDIPM-XVFCMESISA-N N(4)-hydroxycytidine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=NO)C=C1 XCUAIINAJCDIPM-XVFCMESISA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000005605 benzo group Chemical group 0.000 abstract 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 abstract 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 abstract 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 abstract 1
- 210000004556 brain Anatomy 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- -1 di-methyl-amino Chemical group 0.000 abstract 1
- 238000003745 diagnosis Methods 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 238000003384 imaging method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000003287 optical effect Effects 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/041—Heterocyclic compounds
- A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
- A61K51/0459—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K49/00—Preparations for testing in vivo
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physics & Mathematics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Optics & Photonics (AREA)
- Psychiatry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Immunology (AREA)
- Food Science & Technology (AREA)
- Cell Biology (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Analytical Chemistry (AREA)
- Biochemistry (AREA)
- General Physics & Mathematics (AREA)
- Pathology (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención está relacionada con un compuesto con la formula general (ver Fórmula) en el que R1 es fenilo, sustituido opcionalmente por uno o dos sustituyentes, seleccionados de 3H, halógeno, alquilo inferior, dimetilamino, NHC(O)-alquilo inferior, C(O)Oalquilo inferior, alcoxi inferior, OC(3H)3, O11CH3, OCH2CH218F, alcoxi inferior sustituido por halógeno, hidroxi, alquilo inferior sustituido por hidroxi, S-alquilo inferior, o por un grupo heterociclilo; o es benzo[d] [1,3ldioxol-5-ilo, 2,3-dihidrobenzo[bl [1,4] dioxin-6-ilo, indolin-2-ona, o es heteroarilo, seleccionados de entre el grupo que consiste en tiofenilo, benzofuranilo, benzotiofenilo, pirazinilo, o benzotiazolilo; R2 es hidrógeno, alquilo inferior o alquilo inferior sustituido por halógeno; R3 es alquilo inferior, C(3H)3,11CH3, alquilo inferior sustituido por halógeno,-(CH2)2-O-alquilo inferior sustituido por halógeno o cicloalquilo; o R2 y R3 forman junto con el átomo de N al que están unidos un anillo que contiene -CH2CH2CHRCH2CH2-, -CH2CH2CH2CH2-, -CH2CH2CH2-, -CH2CH2-NR-CH2CH2-, -CH2CH2-O-CH2CH2-, -CH2CH2CHRCH2-, -CH2CHRCH2- o (ver Dibujo) R es hidrógeno, halógeno, alquilo inferior sustituido por halógeno o alcoxi inferior; o una sal de adición ácida farmacéuticamente aceptable, una mezcla racémica o su enantiómero y / o isómero óptico correspondiente de los mismos. Los compuestos son adecuados como herramientas para la obtención de imágenes, que pueden mejorar el diagnóstico mediante la identificación de pacientes potenciales con exceso de agregados de tau en el cerebro, que probablemente desarrollarán la enfermedad de Alzheimer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13168830 | 2013-05-23 | ||
| PCT/EP2014/060203 WO2014187762A1 (en) | 2013-05-23 | 2014-05-19 | 2-phenylimidazo[1,2-a]pyrimidines as imaging agents |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2015015893A true MX2015015893A (es) | 2016-03-04 |
Family
ID=48446195
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2015015893A MX2015015893A (es) | 2013-05-23 | 2014-05-19 | 2-fenilimidazo[1,2-a]pirimidinas como agentes formadores de imagen. |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US9801961B2 (es) |
| EP (1) | EP2999701B1 (es) |
| JP (1) | JP6130055B2 (es) |
| KR (1) | KR101770494B1 (es) |
| CN (1) | CN105229009B (es) |
| AR (1) | AR096371A1 (es) |
| AU (1) | AU2014270524B2 (es) |
| BR (1) | BR112015025140A2 (es) |
| CA (1) | CA2907605A1 (es) |
| DK (1) | DK2999701T3 (es) |
| ES (1) | ES2629389T3 (es) |
| HU (1) | HUE033612T2 (es) |
| MX (1) | MX2015015893A (es) |
| PL (1) | PL2999701T3 (es) |
| RU (1) | RU2665580C2 (es) |
| SG (1) | SG11201509503QA (es) |
| SI (1) | SI2999701T1 (es) |
| TW (1) | TW201500360A (es) |
| WO (1) | WO2014187762A1 (es) |
| ZA (1) | ZA201506570B (es) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107810188B (zh) | 2015-04-08 | 2020-09-22 | 拜耳作物科学股份公司 | 作为害虫防治剂和中间体产物的稠合双环杂环衍生物 |
| CN118955472A (zh) | 2015-08-07 | 2024-11-15 | 拜耳作物科学股份公司 | 作为农药的2-(杂)芳基取代的稠合杂环衍生物 |
| EP3355699B1 (en) * | 2015-09-29 | 2021-03-31 | OncoTherapy Science, Inc. | Bicyclic compound and use thereof for inhibiting suv39h2 |
| RU2018119344A (ru) | 2015-10-26 | 2019-11-28 | Байер Кропсайенс Акциенгезельшафт | Конденсированные бициклические гетероциклические производные в качестве средства для борьбы с вредителями |
| WO2017093180A1 (de) | 2015-12-01 | 2017-06-08 | Bayer Cropscience Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| CN105582168A (zh) * | 2016-01-08 | 2016-05-18 | 王明强 | 一种治疗体弱多病、元气不足、免疫力低下的中药药剂 |
| WO2017144341A1 (de) | 2016-02-23 | 2017-08-31 | Bayer Cropscience Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| WO2017174414A1 (de) | 2016-04-05 | 2017-10-12 | Bayer Cropscience Aktiengesellschaft | Naphthalin-derivate als schädlingsbekämpfungsmittel |
| EP3241830A1 (de) | 2016-05-04 | 2017-11-08 | Bayer CropScience Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| CN109689662B (zh) | 2016-07-19 | 2022-03-15 | 拜耳作物科学股份公司 | 作为害虫防治剂的稠合双环杂环衍生物 |
| CN115650982A (zh) | 2016-07-22 | 2023-01-31 | Ac免疫有限公司 | 用于成像tau蛋白聚集体的化合物 |
| US10865207B2 (en) | 2016-07-22 | 2020-12-15 | Ac Immune S.A. | Compounds for imaging Tau protein aggregates |
| BR112019003158B1 (pt) | 2016-08-15 | 2022-10-25 | Bayer Cropscience Aktiengesellschaft | Derivados de heterociclo bicíclico condensado, seu uso, formulação agroquímica, e método para controlar pragas animais |
| CN109963860A (zh) | 2016-09-19 | 2019-07-02 | 拜耳作物科学股份公司 | 吡唑并[1,5-a]吡啶衍生物及其作为农药的用途 |
| WO2018065288A1 (de) | 2016-10-07 | 2018-04-12 | Bayer Cropscience Aktiengesellschaft | 2-[2-phenyl-1-(sulfonylmethyl)vinyl]-imidazo[4,5-b]pyridin-derivate und verwandte verbindungen als schädlingsbekämpfungsmittel im pflanzenschutz |
| UY37556A (es) | 2017-01-10 | 2018-07-31 | Bayer Ag | Derivados heterocíclicos como pesticidas |
| EP3568395A1 (de) | 2017-01-10 | 2019-11-20 | Bayer Aktiengesellschaft | Heterocyclen-derivate als schädlingsbekämpfungsmittel |
| WO2018138050A1 (de) | 2017-01-26 | 2018-08-02 | Bayer Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| EP3615540B1 (de) | 2017-04-24 | 2022-04-27 | Bayer Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| JP6831802B2 (ja) * | 2018-01-12 | 2021-02-17 | 上海富吉医療器械有限公司Ｓｈａｎｇｈａｉ Ｃｈａｒｔｗｅｌｌ Ｍｅｄｉｃａｌ Ｉｎｓｔｒｕｍｅｎｔ Ｃｏ．， Ｌｔｄ． | 放射性核種標識化合物及びこれを含有するイメージング剤 |
| EP3305786A3 (de) | 2018-01-22 | 2018-07-25 | Bayer CropScience Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| WO2019145292A1 (en) | 2018-01-24 | 2019-08-01 | Ac Immune Sa | Azacarboline compounds for the detection of tau aggregates |
| US11306089B2 (en) | 2018-01-24 | 2022-04-19 | Life Molecular Imaging Limited | Gamma-carboline compounds for the detection of Tau aggregates |
| JP2021514949A (ja) | 2018-02-21 | 2021-06-17 | バイエル・アクチエンゲゼルシヤフト | 有害生物防除剤としての縮合二環式ヘテロ環誘導体 |
| CA3102038A1 (en) * | 2018-06-08 | 2019-12-12 | Ac Immune Sa | Novel compounds for diagnosis |
| EP3931192B1 (de) | 2019-02-26 | 2024-03-20 | Bayer Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| KR20210133240A (ko) | 2019-02-26 | 2021-11-05 | 바이엘 악티엔게젤샤프트 | 살충제로서의 융합된 비시클릭 헤테로사이클 유도체 |
| CN114890955A (zh) * | 2022-06-23 | 2022-08-12 | 江西瑞威尔生物科技有限公司 | 一种n取代吗啉类有机化合物的制备工艺 |
| US20240101563A1 (en) * | 2022-07-28 | 2024-03-28 | Ac Immune Sa | Novel compounds |
| WO2025109474A1 (en) * | 2023-11-21 | 2025-05-30 | Novartis Ag | Substituted imidazoarenes and methods of their use |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR0007447A (pt) * | 1999-11-10 | 2002-04-09 | Ortho Mcneil Pharm Inc | 2-aril-3-(heteroaril)-imidazo[1,2-a]pirimidinas substituìdas, composições farmacêuticas e métodos |
| WO2001090108A1 (en) * | 2000-05-24 | 2001-11-29 | Merck Sharp & Dohme Limited | 3-phenyl-imidazo-pyrimidine derivatives as ligands for gaba receptors |
| CA2617319A1 (en) | 2005-06-24 | 2007-01-04 | The Trustees Of The University Of Pennsylvania | Radiolabeled-pegylation of ligands for use as imaging agents |
| WO2007033080A2 (en) | 2005-09-12 | 2007-03-22 | Emory University | Alzheimer's disease imaging agents |
| WO2007034282A2 (en) * | 2005-09-19 | 2007-03-29 | Pfizer Products Inc. | Diaryl-imidazole compounds condensed with a heterocycle as c3a receptor antagonists |
| JP4738419B2 (ja) * | 2005-11-30 | 2011-08-03 | 富士フイルムＲｉファーマ株式会社 | アミロイドの凝集及び／又は沈着に起因する疾患の診断薬及び治療薬 |
| EP2023919A4 (en) * | 2006-05-08 | 2010-12-22 | Molecular Neuroimaging Llc | COMPOUNDS AND AMYLOID PROBES FOR THERAPY AND IMAGING USES |
| US8303935B2 (en) | 2006-05-19 | 2012-11-06 | Nihon Medi-Physics Co., Ltd. | Alkoxy substituted imidazo[1,2-a]pyridines having affinity for amyloid |
| US8691187B2 (en) * | 2009-03-23 | 2014-04-08 | Eli Lilly And Company | Imaging agents for detecting neurological disorders |
| US8410117B2 (en) * | 2010-03-26 | 2013-04-02 | Hoffmann-La Roche Inc. | Imidazopyrimidine derivatives |
| EP2991983B1 (en) * | 2013-04-29 | 2017-03-01 | F. Hoffmann-La Roche AG | 2-phenyl or 2-hetaryl imidazol[1,2-a]pyridine derivatives |
-
2014
- 2014-05-19 CA CA2907605A patent/CA2907605A1/en not_active Abandoned
- 2014-05-19 CN CN201480029084.XA patent/CN105229009B/zh active Active
- 2014-05-19 SI SI201430251T patent/SI2999701T1/sl unknown
- 2014-05-19 ES ES14724757.1T patent/ES2629389T3/es active Active
- 2014-05-19 RU RU2015149528A patent/RU2665580C2/ru not_active IP Right Cessation
- 2014-05-19 JP JP2016514351A patent/JP6130055B2/ja active Active
- 2014-05-19 EP EP14724757.1A patent/EP2999701B1/en active Active
- 2014-05-19 WO PCT/EP2014/060203 patent/WO2014187762A1/en not_active Ceased
- 2014-05-19 SG SG11201509503QA patent/SG11201509503QA/en unknown
- 2014-05-19 DK DK14724757.1T patent/DK2999701T3/en active
- 2014-05-19 HU HUE14724757A patent/HUE033612T2/en unknown
- 2014-05-19 BR BR112015025140A patent/BR112015025140A2/pt not_active Application Discontinuation
- 2014-05-19 AU AU2014270524A patent/AU2014270524B2/en not_active Ceased
- 2014-05-19 MX MX2015015893A patent/MX2015015893A/es unknown
- 2014-05-19 KR KR1020157033039A patent/KR101770494B1/ko not_active Expired - Fee Related
- 2014-05-19 PL PL14724757T patent/PL2999701T3/pl unknown
- 2014-05-20 TW TW103117655A patent/TW201500360A/zh unknown
- 2014-05-21 AR ARP140102015A patent/AR096371A1/es unknown
-
2015
- 2015-09-07 ZA ZA2015/06570A patent/ZA201506570B/en unknown
- 2015-11-19 US US14/945,969 patent/US9801961B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| WO2014187762A1 (en) | 2014-11-27 |
| EP2999701A1 (en) | 2016-03-30 |
| AU2014270524A8 (en) | 2015-09-24 |
| JP6130055B2 (ja) | 2017-05-17 |
| JP2016520091A (ja) | 2016-07-11 |
| AU2014270524A1 (en) | 2015-09-17 |
| TW201500360A (zh) | 2015-01-01 |
| SI2999701T1 (sl) | 2017-08-31 |
| SG11201509503QA (en) | 2015-12-30 |
| HK1213558A1 (zh) | 2016-07-08 |
| DK2999701T3 (en) | 2017-07-10 |
| BR112015025140A2 (pt) | 2017-07-18 |
| CA2907605A1 (en) | 2014-11-27 |
| US20170128598A1 (en) | 2017-05-11 |
| AU2014270524B2 (en) | 2018-01-04 |
| EP2999701B1 (en) | 2017-04-12 |
| CN105229009B (zh) | 2017-09-29 |
| HUE033612T2 (en) | 2017-12-28 |
| RU2015149528A (ru) | 2017-06-28 |
| KR20150144796A (ko) | 2015-12-28 |
| RU2665580C2 (ru) | 2018-08-31 |
| ES2629389T3 (es) | 2017-08-09 |
| AR096371A1 (es) | 2015-12-23 |
| ZA201506570B (en) | 2017-02-22 |
| CN105229009A (zh) | 2016-01-06 |
| RU2015149528A3 (es) | 2018-03-22 |
| US9801961B2 (en) | 2017-10-31 |
| PL2999701T3 (pl) | 2017-09-29 |
| KR101770494B1 (ko) | 2017-08-22 |
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