PE20180530A1 - Derivados de amidas policiclicas como inhibidores de cdk9 - Google Patents
Derivados de amidas policiclicas como inhibidores de cdk9Info
- Publication number
- PE20180530A1 PE20180530A1 PE2017002874A PE2017002874A PE20180530A1 PE 20180530 A1 PE20180530 A1 PE 20180530A1 PE 2017002874 A PE2017002874 A PE 2017002874A PE 2017002874 A PE2017002874 A PE 2017002874A PE 20180530 A1 PE20180530 A1 PE 20180530A1
- Authority
- PE
- Peru
- Prior art keywords
- pyridin
- lymphoma
- tetrahydroimidazo
- carboxamide
- chloro
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed 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
- A61K31/435—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
- A61K31/435—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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Polyesters Or Polycarbonates (AREA)
- Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
- Detergent Compositions (AREA)
Abstract
Se refiere a derivados de piridina o pirimidina de formula I, en donde: A es C(R5), N; R2 es heterocicloalquilo de 3-7 miembros, cicloalquilo de 3-7 miembros, cualquiera de ellos opcionalmente sustituido; y R4 es una de las formulas que se indica a continuacion. Estos compuestos inhiben CDK9 y pueden ser utiles en el tratamiento de enfermedades hiperproliferativas como el cancer, incluyendo trastornos hematologicos malignos como la leucemia mieloide aguda, mieloma multiple, leucemia linfocitica cronica, linfoma difuso de celulas B grandes, linfoma de Burkitt, linfoma folicular y tumores solidos como por ejemplo cancer de mama, pulmon, neuroblastoma y colon. Entre los compuestos preferidos tenemos los siguientes: (R)-N-(5-cloro-4-(5,6,7,8-tetrahidroimidazo[1,2-a]piridin-3-il)piridin-2-il)piperidin-3-carboxamida; (1S,3R)-3-acetamido de-N-(5-cloro-4-(5,6,7,8-tetrahidroimidazo[1,2-a]piridin-3-il)piridin-2-il)piperidin-3-carboxamida; entre otros.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562185852P | 2015-06-29 | 2015-06-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20180530A1 true PE20180530A1 (es) | 2018-03-19 |
Family
ID=56292699
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2017002874A PE20180530A1 (es) | 2015-06-29 | 2016-06-27 | Derivados de amidas policiclicas como inhibidores de cdk9 |
Country Status (36)
| Country | Link |
|---|---|
| US (4) | US9845331B2 (es) |
| EP (2) | EP3313838B1 (es) |
| JP (1) | JP6997627B2 (es) |
| KR (1) | KR102663113B1 (es) |
| CN (1) | CN107873028B (es) |
| AR (1) | AR105179A1 (es) |
| AU (1) | AU2016286200B2 (es) |
| BR (1) | BR122019013677B1 (es) |
| CA (1) | CA2989499C (es) |
| CL (1) | CL2017003306A1 (es) |
| CO (1) | CO2017013713A2 (es) |
| CR (2) | CR20170596A (es) |
| CY (2) | CY1122111T1 (es) |
| DK (2) | DK3313838T3 (es) |
| DO (2) | DOP2017000295A (es) |
| EA (1) | EA035383B1 (es) |
| ES (2) | ES2902148T3 (es) |
| HR (2) | HRP20211970T1 (es) |
| HU (2) | HUE057343T2 (es) |
| IL (1) | IL256393B (es) |
| LT (2) | LT3539961T (es) |
| ME (1) | ME03404B (es) |
| MX (1) | MX371034B (es) |
| NI (1) | NI201700174A (es) |
| PE (1) | PE20180530A1 (es) |
| PH (1) | PH12017502334A1 (es) |
| PL (2) | PL3313838T3 (es) |
| PT (2) | PT3539961T (es) |
| RS (2) | RS62781B1 (es) |
| SI (2) | SI3313838T1 (es) |
| SV (1) | SV2017005598A (es) |
| TN (1) | TN2017000486A1 (es) |
| TR (1) | TR201909286T4 (es) |
| TW (1) | TWI723028B (es) |
| WO (1) | WO2017001354A1 (es) |
| ZA (1) | ZA201800563B (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112020005039A2 (pt) | 2017-09-25 | 2020-09-15 | Astrazeneca Ab | combinação de um inibidor de btk e um inibidor de cdk9 para tratar câncer |
| WO2019074748A1 (en) * | 2017-10-09 | 2019-04-18 | Merck Sharp & Dohme Corp. | NOVEL SUBSTITUTED PHENYL-OXETANE AND PHENYLTETRAHYDROFURAN COMPOUNDS AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE (IDO) |
| CN108129288B (zh) * | 2017-12-27 | 2021-01-22 | 上海毕得医药科技股份有限公司 | 一种反式-3-羟基环丁基甲酸的合成方法 |
| TW202344250A (zh) | 2018-11-14 | 2023-11-16 | 瑞典商阿斯特捷利康公司 | 治療癌症之方法 |
| JP2022548568A (ja) * | 2019-09-11 | 2022-11-21 | プレリュード・セラピューティクス・インコーポレイテッド | Ｃｄｋ阻害剤及び医薬品としてのそれらの使用 |
| JP2023505850A (ja) * | 2019-12-09 | 2023-02-13 | 石薬集団中奇制薬技術（石家庄）有限公司 | サイクリン依存性キナーゼ９阻害剤としての化合物及びその用途 |
| US20230219961A1 (en) | 2020-05-12 | 2023-07-13 | Suzhou Alphama Biotechnology Co., Ltd. | Pyridine acetamide derivative serving as CDK inhibitor, and preparation method therefor and use thereof |
| JP7406008B2 (ja) * | 2020-05-12 | 2023-12-26 | 蘇州阿尓脈生物科技有限公司 | Ｃｄｋ９阻害剤としての多環式アミド系誘導体、その調製方法及び用途 |
| WO2021260578A1 (en) | 2020-06-24 | 2021-12-30 | Astrazeneca Uk Limited | Combination of antibody-drug conjugate and cdk9 inhibitor |
| WO2022028556A1 (zh) | 2020-08-07 | 2022-02-10 | 南京药石科技股份有限公司 | Cdk9抑制剂及其用途 |
| TWI809330B (zh) * | 2020-11-20 | 2023-07-21 | 大陸商勁方醫藥科技(上海)有限公司 | Cdk9抑制劑的多晶型物及其製法和用途 |
| WO2022247785A1 (zh) * | 2021-05-24 | 2022-12-01 | 石药集团中奇制药技术（石家庄）有限公司 | 一种周期蛋白依赖性激酶9抑制剂的用途 |
| CN115381824A (zh) * | 2021-05-24 | 2022-11-25 | 石药集团中奇制药技术（石家庄）有限公司 | 周期蛋白依赖性激酶9抑制剂的用途 |
| WO2023284775A1 (zh) * | 2021-07-14 | 2023-01-19 | 上海海雁医药科技有限公司 | 吡唑衍生物及其中间体和制备方法 |
| WO2023122783A2 (en) * | 2021-12-23 | 2023-06-29 | The Katholieke Universiteit Leuven | Tetrahydropyrazolopyrimidines and related analogs for inhibiting yap/taz-tead |
| KR20240025485A (ko) | 2022-08-17 | 2024-02-27 | 한국화학연구원 | Cdk2 및/또는 cdk9의 억제 또는 분해용 화합물 및 이들의 의약 용도 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008133192A1 (ja) | 2007-04-19 | 2008-11-06 | Takeda Pharmaceutical Company Limited | 縮合イミダゾール化合物およびその用途 |
| JP5379787B2 (ja) | 2007-04-24 | 2013-12-25 | インゲニウム ファーマシューティカルズ ジーエムビーエイチ | プロテインキナーゼの阻害剤 |
| US8389521B2 (en) | 2007-04-24 | 2013-03-05 | Ingenium Pharmaceuticals Gmbh | Inhibitors of protein kinases |
| JP5693951B2 (ja) | 2007-04-24 | 2015-04-01 | アストラゼネカ エービー | プロテインキナーゼの阻害剤 |
| US8507498B2 (en) | 2007-04-24 | 2013-08-13 | Ingenium Pharmaceuticals Gmbh | 4, 6-disubstituted aminopyrimidine derivatives as inhibitors of protein kinases |
| WO2008132138A1 (en) * | 2007-04-25 | 2008-11-06 | Ingenium Pharmaceuticals Gmbh | Derivatives of 4,6-disubstituted aminopyrimidines |
| KR20100090772A (ko) | 2007-10-12 | 2010-08-17 | 인게니움 파르마코이티칼스 게엠베하 | 단백질 키나제 억제제 |
| WO2011026917A1 (en) | 2009-09-04 | 2011-03-10 | Novartis Ag | Heteroaryl compounds as kinase inhibitors |
| US20110113038A1 (en) | 2009-11-12 | 2011-05-12 | International Business Machines Corporation | Search term security |
| GB201002911D0 (en) | 2010-02-19 | 2010-04-07 | Medical Res Council | Compound |
| EP2545037A1 (en) | 2010-03-10 | 2013-01-16 | Ingenium Pharmaceuticals GmbH | Inhibitors of protein kinases |
| AR081810A1 (es) | 2010-04-07 | 2012-10-24 | Bayer Cropscience Ag | Piridinilpirazoles biciclicos |
| WO2012066065A1 (en) | 2010-11-17 | 2012-05-24 | Novartis Ag | Phenyl-heteroaryl amine compounds and their uses |
| CN103339110A (zh) * | 2011-01-28 | 2013-10-02 | 诺瓦提斯公司 | 作为cdk9抑制剂的取代的杂-联芳基化合物及其用途 |
| WO2012101063A1 (en) * | 2011-01-28 | 2012-08-02 | Novartis Ag | N-acyl pyridine biaryl compounds and their uses |
| WO2012101064A1 (en) * | 2011-01-28 | 2012-08-02 | Novartis Ag | N-acyl pyrimidine biaryl compounds as protein kinase inhibitors |
| US9314026B2 (en) | 2011-10-06 | 2016-04-19 | Bayer Intellectual Property Gmbh | Heterocyclylpyri(mi)dinylpyrazole |
| EP2970268A1 (en) | 2013-03-13 | 2016-01-20 | AbbVie Inc. | Cdk9 kinase inhibitors |
| CN105189481A (zh) * | 2013-03-13 | 2015-12-23 | 艾伯维公司 | 吡啶cdk9激酶抑制剂 |
| WO2014139328A1 (en) | 2013-03-14 | 2014-09-18 | Abbvie Inc. | Pyrrolo[2,3-b]pyridine cdk9 kinase inhibitors |
| WO2014160028A1 (en) | 2013-03-14 | 2014-10-02 | Abbvie Inc. | Pyrrolopyrimindine cdk9 kinase inhibitors |
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2016
- 2016-06-27 BR BR122019013677-7A patent/BR122019013677B1/pt active IP Right Grant
- 2016-06-27 TN TNP/2017/000486A patent/TN2017000486A1/en unknown
- 2016-06-27 WO PCT/EP2016/064899 patent/WO2017001354A1/en active Application Filing
- 2016-06-27 RS RS20220005A patent/RS62781B1/sr unknown
- 2016-06-27 HU HUE19165726A patent/HUE057343T2/hu unknown
- 2016-06-27 DK DK16733459.8T patent/DK3313838T3/da active
- 2016-06-27 PE PE2017002874A patent/PE20180530A1/es unknown
- 2016-06-27 US US15/193,826 patent/US9845331B2/en active Active
- 2016-06-27 PL PL16733459T patent/PL3313838T3/pl unknown
- 2016-06-27 LT LTEP19165726.1T patent/LT3539961T/lt unknown
- 2016-06-27 RS RS20190564A patent/RS58712B1/sr unknown
- 2016-06-27 EP EP16733459.8A patent/EP3313838B1/en active Active
- 2016-06-27 PT PT191657261T patent/PT3539961T/pt unknown
- 2016-06-27 ES ES19165726T patent/ES2902148T3/es active Active
- 2016-06-27 HU HUE16733459A patent/HUE043440T2/hu unknown
- 2016-06-27 AU AU2016286200A patent/AU2016286200B2/en active Active
- 2016-06-27 SI SI201630247T patent/SI3313838T1/sl unknown
- 2016-06-27 CN CN201680029447.9A patent/CN107873028B/zh active Active
- 2016-06-27 LT LTEP16733459.8T patent/LT3313838T/lt unknown
- 2016-06-27 JP JP2017567737A patent/JP6997627B2/ja active Active
- 2016-06-27 EA EA201890094A patent/EA035383B1/ru not_active IP Right Cessation
- 2016-06-27 PL PL19165726T patent/PL3539961T3/pl unknown
- 2016-06-27 HR HRP20211970TT patent/HRP20211970T1/hr unknown
- 2016-06-27 CR CR20170596A patent/CR20170596A/es unknown
- 2016-06-27 DK DK19165726.1T patent/DK3539961T3/da active
- 2016-06-27 ME MEP-2019-138A patent/ME03404B/me unknown
- 2016-06-27 TR TR2019/09286T patent/TR201909286T4/tr unknown
- 2016-06-27 MX MX2017016244A patent/MX371034B/es active IP Right Grant
- 2016-06-27 CA CA2989499A patent/CA2989499C/en active Active
- 2016-06-27 SI SI201631427T patent/SI3539961T1/sl unknown
- 2016-06-27 EP EP19165726.1A patent/EP3539961B1/en active Active
- 2016-06-27 ES ES16733459T patent/ES2728356T3/es active Active
- 2016-06-27 PT PT16733459T patent/PT3313838T/pt unknown
- 2016-06-27 CR CR20210297A patent/CR20210297A/es unknown
- 2016-06-27 KR KR1020187002262A patent/KR102663113B1/ko active IP Right Grant
- 2016-06-28 TW TW105120362A patent/TWI723028B/zh active
- 2016-06-28 AR ARP160101956A patent/AR105179A1/es unknown
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2017
- 2017-12-06 US US15/833,277 patent/US10717746B2/en active Active
- 2017-12-12 DO DO2017000295A patent/DOP2017000295A/es unknown
- 2017-12-15 PH PH12017502334A patent/PH12017502334A1/en unknown
- 2017-12-18 IL IL256393A patent/IL256393B/en unknown
- 2017-12-20 SV SV2017005598A patent/SV2017005598A/es unknown
- 2017-12-21 CL CL2017003306A patent/CL2017003306A1/es unknown
- 2017-12-22 NI NI201700174A patent/NI201700174A/es unknown
- 2017-12-28 CO CONC2017/0013713A patent/CO2017013713A2/es unknown
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2018
- 2018-01-26 ZA ZA2018/00563A patent/ZA201800563B/en unknown
- 2018-09-25 DO DO2018000207A patent/DOP2018000207A/es unknown
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2019
- 2019-04-19 HR HRP20190748TT patent/HRP20190748T1/hr unknown
- 2019-06-19 CY CY20191100636T patent/CY1122111T1/el unknown
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2020
- 2020-07-17 US US16/931,786 patent/US11352369B2/en active Active
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2021
- 2021-12-22 CY CY20211101125T patent/CY1125066T1/el unknown
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2022
- 2022-04-27 US US17/660,935 patent/US20220340592A1/en active Pending
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