PE20130306A1 - Morfolinopirimidinas y su uso en terapia - Google Patents
Morfolinopirimidinas y su uso en terapiaInfo
- Publication number
- PE20130306A1 PE20130306A1 PE2012002373A PE2012002373A PE20130306A1 PE 20130306 A1 PE20130306 A1 PE 20130306A1 PE 2012002373 A PE2012002373 A PE 2012002373A PE 2012002373 A PE2012002373 A PE 2012002373A PE 20130306 A1 PE20130306 A1 PE 20130306A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- methylsulfonimidoyl
- methylmorpholin
- pyrimidin
- compounds
- Prior art date
Links
- 238000002560 therapeutic procedure Methods 0.000 title 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 4
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 4
- 150000001875 compounds Chemical group 0.000 abstract 3
- XIPUIGPNIDKXJU-UHFFFAOYSA-N [CH]1CC1 Chemical compound [CH]1CC1 XIPUIGPNIDKXJU-UHFFFAOYSA-N 0.000 abstract 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 abstract 2
- DUIMWXDLDBNUFD-UHFFFAOYSA-N 4-pyrimidin-2-ylmorpholine Chemical class C1COCCN1C1=NC=CC=N1 DUIMWXDLDBNUFD-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
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
- A61K31/535—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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
SE REFIERE A COMPUESTOS MORFOLINOPIRIMIDINAS DE FORMULA (I) DONDE R1 ES MORFOLIN-4-ILO O 3-METILMORFOLIN-4-ILO; R2 ES UN COMPUESTO DE FORMULA (i), (ii), ENTRE OTROS, EN DONDE R2A, R2B, R2C Y R2D SON CADA UNO H O METILO; R3 ES METILO; R4 Y R5 SON CADA UNO H, METILO O JUNTO CON EL ATOMO AL CUAL ESTAN UNIDOS FORMAN EL ANILLO A QUE ES CICLOALQUILO(C3-C6) O HETEROCICLICO DE 4 A 6 MIEMBROS; R6 ES H. SON COMPUESTOS PREFERIDOS: 4-{4-[(3R)-3-METILMORFOLIN-4-IL]-6-[((R)-S-METILSULFONIMIDOIL)METIL]PIRIMIDIN-2-IL}-1H-PIRROLO[2,3-b]PIRIDINA; 4-{4-[(3R)-3-METILMORFOLIN-4-IL]-6-[1-((S)-S-METILSULFONIMIDOIL)CICLOPROPIL]PIRIMIDIN-2-IL}-1H-PIRROLO[2,3-b]PIRIDINA; N-METIL-1-{4-[(3R)-3-METILMORFOLIN-4-IL]-6-[1-((R)-S-METILSULFONIMIDOIL)CICLOPROPIL]PIRIMIDIN-2-IL}-1H-BENZIMIDAZOL-2-AMINA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE LA QUINASA ATR SIENDO UTILES EN EL TRATAMIENTO DE CANCER
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35371310P | 2010-06-11 | 2010-06-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20130306A1 true PE20130306A1 (es) | 2013-04-05 |
Family
ID=44168987
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2012002373A PE20130306A1 (es) | 2010-06-11 | 2011-06-09 | Morfolinopirimidinas y su uso en terapia |
Country Status (38)
| Country | Link |
|---|---|
| US (5) | US8252802B2 (es) |
| EP (1) | EP2579877B1 (es) |
| JP (1) | JP5721821B2 (es) |
| KR (1) | KR101820996B1 (es) |
| CN (1) | CN103068391B (es) |
| AR (1) | AR081859A1 (es) |
| AU (1) | AU2011263491B2 (es) |
| BR (1) | BR112012031561B1 (es) |
| CA (1) | CA2800203C (es) |
| CL (1) | CL2012003503A1 (es) |
| CO (1) | CO6640270A2 (es) |
| CR (1) | CR20120628A (es) |
| CU (1) | CU24109B1 (es) |
| DK (1) | DK2579877T3 (es) |
| DO (1) | DOP2012000310A (es) |
| EA (1) | EA022087B1 (es) |
| EC (1) | ECSP12012334A (es) |
| ES (1) | ES2514325T3 (es) |
| GT (1) | GT201200334A (es) |
| HR (1) | HRP20140953T1 (es) |
| MX (1) | MX2012014477A (es) |
| MY (1) | MY158193A (es) |
| NI (1) | NI201200184A (es) |
| NZ (1) | NZ604480A (es) |
| PE (1) | PE20130306A1 (es) |
| PH (1) | PH12012502438A1 (es) |
| PL (1) | PL2579877T3 (es) |
| PT (1) | PT2579877E (es) |
| RS (1) | RS53566B1 (es) |
| SA (1) | SA111320519B1 (es) |
| SG (1) | SG185711A1 (es) |
| SI (1) | SI2579877T1 (es) |
| SM (1) | SMT201400146B (es) |
| TW (1) | TWI526208B (es) |
| UA (1) | UA109010C2 (es) |
| UY (1) | UY33440A (es) |
| WO (1) | WO2011154737A1 (es) |
| ZA (1) | ZA201300255B (es) |
Families Citing this family (54)
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| SA111320519B1 (ar) * | 2010-06-11 | 2014-07-02 | Astrazeneca Ab | مركبات بيريميدينيل للاستخدام كمثبطات atr |
| HUE044280T2 (hu) | 2014-06-17 | 2019-10-28 | Vertex Pharma | Rosszindulatú daganatok kezelése Chk1- és ATR-gátlók kombinációjával |
| TWI700283B (zh) | 2014-08-04 | 2020-08-01 | 德商拜耳製藥公司 | ２-(嗎啉-４-基)-１,７-萘啶 |
| MX395066B (es) | 2015-09-30 | 2025-03-24 | Vertex Pharma | Método para tratar cáncer usando una combinación de agentes que dañan el adn e inhibidores de proteína relacionada con ataxia telangiectasia y rad3 (atr). |
| WO2018029117A1 (en) * | 2016-08-10 | 2018-02-15 | Rheinisch-Westfälische Technische Hochschule Aachen (RWTH) | New atr inhibitors for the use in cancer therapy |
| MX394860B (es) * | 2016-09-27 | 2025-03-24 | Vertex Pharma | Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk). |
| AR110995A1 (es) | 2017-02-24 | 2019-05-22 | Bayer Ag | Combinación de inhibidores de quinasa atr con sal de radio-223 |
| JOP20190197A1 (ar) | 2017-02-24 | 2019-08-22 | Bayer Pharma AG | مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر |
| WO2018153972A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and antiandrogens |
| WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
| EP3630116B1 (en) | 2017-05-26 | 2024-05-01 | The Board Of Regents Of The University Of Texas System | Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase |
| JP7159307B2 (ja) | 2017-07-13 | 2022-10-24 | ボード オブ レジェンツ，ザ ユニバーシティ オブ テキサス システム | Ａｔｒキナーゼの複素環式阻害剤 |
| US11690911B2 (en) | 2017-08-04 | 2023-07-04 | Bayer Aktiengesellschaft | Combination of ATR kinase inhibitors and PD-1/PD-L1 inhibitors |
| EP3668839B1 (en) * | 2017-08-17 | 2023-04-12 | Board of Regents, The University of Texas System | Heterocyclic inhibitors of atr kinase |
| CA3074719A1 (en) | 2017-09-08 | 2019-03-14 | Bluevalley Pharmaceutical Llc | Substituted pyrrolopyridines as atr inhibitors |
| EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
| US11712440B2 (en) | 2017-12-08 | 2023-08-01 | Bayer Aktiengesellschaft | Predictive markers for ATR kinase inhibitors |
| GB201720989D0 (en) * | 2017-12-15 | 2018-01-31 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| LT3753937T (lt) | 2018-02-07 | 2024-02-26 | Wuxi Biocity Biopharmaceutics Co., Ltd. | Atr inhibitorius ir jo taikymas |
| WO2019178590A1 (en) | 2018-03-16 | 2019-09-19 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of atr kinase |
| SG11202011135WA (en) | 2018-05-14 | 2020-12-30 | Nuvation Bio Inc | Anti-cancer nuclear hormone receptor-targeting compounds |
| WO2020078788A1 (en) | 2018-10-16 | 2020-04-23 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds |
| KR20210097124A (ko) | 2018-10-30 | 2021-08-06 | 리페어 세라퓨틱스 인크. | 화합물, 약제 조성물, 및 화합물 제조 방법 및 atr 키나제 억제제로서의 이것들의 사용 방법 |
| MX2021007192A (es) * | 2018-12-18 | 2021-07-21 | Astrazeneca Ab | Proceso farmaceutico e intermedios. |
| MX2021013774A (es) | 2019-05-14 | 2021-12-10 | Nuvation Bio Inc | Compuestos anticancerigenos dirigidos a los receptores hormonales nucleares. |
| GB201908536D0 (en) * | 2019-06-13 | 2019-07-31 | Glaxosmithkline Ip Dev Ltd | Compounds |
| CN112142744A (zh) * | 2019-06-28 | 2020-12-29 | 上海瑛派药业有限公司 | 取代的稠合杂芳双环化合物作为激酶抑制剂及其应用 |
| NZ784192A (en) * | 2019-08-06 | 2025-05-30 | Wuxi Biocity Biopharmaceutics Co Ltd | Crystalline form of atr inhibitor and use thereof |
| TW202131930A (zh) | 2019-11-13 | 2021-09-01 | 美商諾維雪碧歐公司 | 抗癌核荷爾蒙受體標靶化合物 |
| CN114423760B (zh) * | 2019-11-21 | 2024-12-27 | 江苏恒瑞医药股份有限公司 | 吡唑并杂芳基类衍生物、其制备方法及其在医药上的应用 |
| CN112939966B (zh) * | 2019-12-10 | 2023-03-24 | 武汉光谷亚太医药研究院有限公司 | 嘧啶衍生物、其制备及应用 |
| WO2021143821A1 (zh) * | 2020-01-17 | 2021-07-22 | 江苏恒瑞医药股份有限公司 | 稠合杂芳基类衍生物、其制备方法及其在医药上的应用 |
| US20240150333A1 (en) * | 2020-03-20 | 2024-05-09 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Taf1 inhibitors |
| JP2023524872A (ja) | 2020-05-11 | 2023-06-13 | アストラゼネカ・アクチエボラーグ | がんの治療のためのａｔｒ阻害剤 |
| JP7418051B2 (ja) * | 2020-05-29 | 2024-01-19 | シェンチェン リンファン バイオテック カンパニー，リミティド | フルオロピロロピリジン系化合物及びその使用 |
| CN111646985A (zh) * | 2020-06-01 | 2020-09-11 | 江苏集萃分子工程研究院有限公司 | 一种含嘧啶杂环抗肿瘤药物分子azd6738的合成方法 |
| BR112022026205A2 (pt) * | 2020-06-24 | 2023-03-14 | Astrazeneca Uk Ltd | Produto farmacêutico, uso de um conjugado anticorpo anti-her2-fármaco ou um inibidor de atr na fabricação de um medicamento, e, método de tratamento do câncer |
| KR20230039675A (ko) * | 2020-07-13 | 2023-03-21 | 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 | Atr 키나제 억제제로 사용되는 피라졸로피리미딘 화합물 |
| US20230399302A1 (en) * | 2020-10-29 | 2023-12-14 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Process for the preparation of heteroaryl-substituted sulfur(vi) compounds |
| TW202304457A (zh) | 2021-03-22 | 2023-02-01 | 瑞典商阿斯特捷利康公司 | 配製物 |
| WO2022204184A1 (en) | 2021-03-23 | 2022-09-29 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| CA3213407A1 (en) | 2021-03-26 | 2022-09-29 | Astrazeneca Ab | Combination treatments for melanoma |
| WO2022235585A1 (en) | 2021-05-03 | 2022-11-10 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| IT202100021863A1 (it) * | 2021-08-13 | 2023-02-13 | Univ Degli Studi Milano | Morfolino pirimidine per l’uso nella prevenzione e/o nel trattamento di stati di ipereccitabilità neuronale |
| WO2023039573A1 (en) * | 2021-09-10 | 2023-03-16 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Compounds for targeted degradation of taf1 |
| CN116283960A (zh) * | 2021-12-21 | 2023-06-23 | 上海安诺达生物科技有限公司 | 取代的稠杂环化合物及其制备方法与应用 |
| WO2023122723A1 (en) | 2021-12-23 | 2023-06-29 | The Broad Institute, Inc. | Panels and methods for diagnosing and treating lung cancer |
| WO2023126823A1 (en) | 2021-12-28 | 2023-07-06 | Astrazeneca Uk Limited | Combination of antibody-drug conjugate and atr inhibitor |
| TW202348252A (zh) | 2022-02-16 | 2023-12-16 | 英商梅迪繆思有限公司 | 用治療性結合分子治療癌症的組合療法 |
| IL317573A (en) | 2022-06-15 | 2025-02-01 | Astrazeneca Ab | Combination therapy for cancer treatment |
| CN120435459A (zh) | 2022-12-06 | 2025-08-05 | 阿斯利康(瑞典)有限公司 | Polq抑制剂 |
| WO2024213699A1 (en) | 2023-04-14 | 2024-10-17 | Astrazeneca Ab | Combinations of kras inhibitor and atr inhibitor for the treatment of cancer |
| CN117652610A (zh) * | 2023-10-26 | 2024-03-08 | 广东省农业科学院农业生物基因研究中心 | 一种利用3-甲基吗啉-吡啶-嘧啶衍生物抑制黄曲霉毒素产生的方法 |
| WO2025181153A1 (en) | 2024-03-01 | 2025-09-04 | F. Hoffmann-La Roche Ag | Use of atr inhibitors in combination with pi3k alpha inhibitors |
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