AR088760A1 - Derivados de pirrolopirimidina y purina - Google Patents
Derivados de pirrolopirimidina y purinaInfo
- Publication number
- AR088760A1 AR088760A1 ARP120103503A AR088760A1 AR 088760 A1 AR088760 A1 AR 088760A1 AR P120103503 A ARP120103503 A AR P120103503A AR 088760 A1 AR088760 A1 AR 088760A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently
- ring
- absent
- alkoxy
- Prior art date
Links
- 229940083251 peripheral vasodilators purine derivative Drugs 0.000 title abstract 2
- 150000003212 purines Chemical class 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 9
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 8
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 6
- 229910052757 nitrogen Inorganic materials 0.000 abstract 6
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical group 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 4
- -1 cyano, difluoromethyl Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 3
- 150000002431 hydrogen Chemical class 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 abstract 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- 241000124008 Mammalia Species 0.000 abstract 2
- 230000002159 abnormal effect Effects 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 230000010261 cell growth Effects 0.000 abstract 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006584 (C3-C10) heterocycloalkyl group Chemical group 0.000 abstract 1
- KDOPAZIWBAHVJB-UHFFFAOYSA-N 5h-pyrrolo[3,2-d]pyrimidine Chemical compound C1=NC=C2NC=CC2=N1 KDOPAZIWBAHVJB-UHFFFAOYSA-N 0.000 abstract 1
- 125000000172 C5-C10 aryl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000000561 purinyl group Chemical class N1=C(N=C2N=CNC2=C1)* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 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
-
- 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
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Los derivados de pirrolopirimidina y purina son útiles para tratar el crecimiento celular anormal, tal como cáncer, en mamíferos. Otras formas de realización se refieren a composiciones farmacéuticas que contienen los compuestos y a métodos para usar los compuestos y las composiciones en el tratamiento del crecimiento celular anormal en mamíferos. Reivindicación 1: Un compuesto caracterizado por la fórmula (1) en donde X es N o CR⁷; Y está ausente, o es O, S o NR⁸; Q, T, V y W son cada uno, independientemente, C o N, siempre que al menos dos de Q, T, V y W sean N y al menos uno de Q, T, V y W sea C, siempre que cuando Q y T sean N, al menos uno de R¹ y R² esté ausente y siempre que cuando T y V sean N, al menos uno de R² y R³ esté ausente; R¹ y R⁴ están cada uno, independientemente, ausentes o son hidrógeno, ciano, difluorometilo, trifluorometilo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, alcoxi C₁₋₆, -N(R⁹)(R¹⁰), cicloalquilo C₃₋₅ o heterocicloalquilo de 4 - 6 miembros, en donde alquilo C₁₋₆ se puede sustituir opcionalmente con halógeno, hidroxi, alcoxi C₁₋₆ o N(R¹¹)(R¹²); R² y R³ están cada uno, independientemente, ausentes o son hidrógeno, alquilo C₁₋₆, alquinilo C₂₋₆, alcoxi C₁₋₆, cicloalquilo C₃₋₇ o heterocicloalquilo de 3 - 7 miembros, en donde cada uno de alquilo C₁₋₆ y alcoxi C₁₋₆ en R² y R³ se sustituye, de manera independiente y opcional, con uno o más grupos R¹³, y además en donde cada uno del cicloalquilo C₃₋₇ y el heterocicloalquilo de 3 - 7 miembros en R² y R³ se sustituye, de manera independiente y opcional, con uno o más grupos R¹⁴; o R¹ y R² o R² y R³ se pueden combinar para formar un anillo de cicloalquilo C₅₋₇ o un anillo de heterocicloalquilo de 5 - 7 miembros, en donde cada uno del anillo de cicloalquilo C₅₋₇ y el anillo de heterocicloalquilo de 5 - 7 miembros se sustituye, de manera independiente y opcional, con uno o más grupos R¹³; el anillo A está ausente o es cicloalquilo C₃₋₁₀, heterocicloalquilo de 3 - 10 miembros, arilo C₅₋₁₀ o heteroarilo de 5 - 12 miembros; R⁵ y R⁵ᵃ están cada uno, independientemente, ausentes o son halógeno, ciano, hidroxi, difluorometilo, trifluorometilo, alquilo C₁₋₃, alcoxi C₁₋₃, cicloalquilo C₃₋₅ o heteroarilo de 4 - 6 miembros, en donde alquilo C₁₋₃ se sustituye opcionalmente con hidroxi, difluorometilo, trifluorometilo, alcoxi C₁₋₃ o cicloalquilo C₃₋₅; R⁶ es un compuesto del grupo de formulas (2); Z está ausente cuando el punto de unión de R⁶ en el anillo A es un átomo de nitrógeno, y Z es -NR¹⁷- cuando el anillo A está ausente o cuando el punto de unión de R⁶ en el anillo A es un átomo de carbono; R⁷ es hidrógeno, halógeno, ciano, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆ o heteroarilo de 4 - 6 miembros, en donde alquilo C₁₋₆ se puede sustituir opcionalmente con hidroxi o alcoxi C₁₋₃, y en donde el heteroarilo de 4 - 6 miembros se puede sustituir opcionalmente con alquilo C₁₋₃; R⁸ es hidrógeno o alquilo C₁₋₃; R⁹ y R¹⁰ son cada uno, independientemente, hidrógeno o alquilo C₁₋₆; o R⁹ y R¹⁰, junto con el nitrógeno al que están unidos, se pueden combinar para formar un anillo de 4 - 7 miembros, en donde R⁹ y R¹⁰ son cada uno alquilo C₁₋₃, en donde el anillo de 4 - 7 miembros se sustituye opcionalmente con uno o más grupos R¹⁴; R¹¹ y R¹² son cada uno independientemente hidrógeno o alquilo C₁₋₃; cada R¹³ es independientemente halógeno, ciano, hidroxi, alcoxi C₁₋₆, -N(R⁹)(R¹⁰), -CON(R⁹)(R¹⁰), heterocicloalquilo de 3 - 7 miembros, en donde el heterocicloalquilo de 3 - 7 miembros en R¹³ se sustituye opcionalmente con uno o más grupos R¹⁴; cada R¹⁴ es independientemente halógeno, alquilo C₁₋₃, hidroxi, alcoxi C₁₋₆, -NH₂, -NHCH₃ o N(CH₃)₂; R¹⁵ y R¹⁶ son cada uno independientemente hidrógeno o alquilo C₁₋₆, en donde alquilo C₁₋₆ de uno de R¹⁵ y R¹⁶ se sustituye opcionalmente con -N(R⁹)(R¹⁰); R¹⁷ es hidrógeno o alquilo C₁₋₃; y m es 0, 1 ó 2, siempre que cuando el anillo A esté ausente, m sea 2; o una sal de aquel aceptable desde el punto de vista farmacéutico.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161538103P | 2011-09-22 | 2011-09-22 | |
| US201261639639P | 2012-04-27 | 2012-04-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR088760A1 true AR088760A1 (es) | 2014-07-02 |
Family
ID=47116127
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120103503 AR088760A1 (es) | 2011-09-22 | 2012-09-21 | Derivados de pirrolopirimidina y purina |
Country Status (29)
| Country | Link |
|---|---|
| US (2) | US9040547B2 (es) |
| EP (1) | EP2758402B9 (es) |
| JP (1) | JP5914667B2 (es) |
| KR (1) | KR20140059246A (es) |
| CN (1) | CN103814030A (es) |
| AP (1) | AP2014007475A0 (es) |
| AR (1) | AR088760A1 (es) |
| AU (1) | AU2012311184A1 (es) |
| BR (1) | BR112014006840A2 (es) |
| CA (1) | CA2847540C (es) |
| CL (2) | CL2014002726A1 (es) |
| CO (1) | CO6910196A2 (es) |
| CR (1) | CR20140132A (es) |
| DO (1) | DOP2014000055A (es) |
| EA (1) | EA201490673A1 (es) |
| ES (1) | ES2575710T3 (es) |
| IL (1) | IL231592A0 (es) |
| MA (1) | MA35451B1 (es) |
| MD (1) | MD20140023A2 (es) |
| MX (1) | MX2014003501A (es) |
| NI (1) | NI201400023A (es) |
| PE (1) | PE20141228A1 (es) |
| PH (1) | PH12014500638A1 (es) |
| SG (1) | SG2014014450A (es) |
| TN (1) | TN2014000115A1 (es) |
| TW (1) | TWI492946B (es) |
| UA (1) | UA110259C2 (es) |
| UY (1) | UY34342A (es) |
| WO (1) | WO2013042006A1 (es) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA029131B1 (ru) | 2008-05-21 | 2018-02-28 | Ариад Фармасьютикалз, Инк. | Фосфорсодержащие производные в качестве ингибиторов киназы |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| EP2571361A4 (en) | 2010-05-19 | 2013-11-13 | Univ North Carolina | PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| BR122014012788B1 (pt) * | 2010-06-23 | 2022-04-19 | Hanmi Science Co., Ltd | Derivados de pirimidina fundidos, seus usos, e composição farmacêutica para inibição da atividade de tirosina quinase |
| CA2832504C (en) | 2011-05-04 | 2019-10-01 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| MX2014004086A (es) * | 2011-10-03 | 2014-09-22 | Univ North Carolina | Compuestos de pirrolopirimidina para el tratamiento del cancer. |
| AU2013204563B2 (en) | 2012-05-05 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| WO2013177168A1 (en) | 2012-05-22 | 2013-11-28 | The University Of North Carolina At Chapel Hill | Pyrimidine compounds for the treatment of cancer |
| US9562047B2 (en) | 2012-10-17 | 2017-02-07 | The University Of North Carolina At Chapel Hill | Pyrazolopyrimidine compounds for the treatment of cancer |
| WO2014085225A1 (en) | 2012-11-27 | 2014-06-05 | The University Of North Carolina At Chapel Hill | Pyrimidine compounds for the treatment of cancer |
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| MX2015012106A (es) * | 2013-03-14 | 2016-01-12 | Pfizer | Combinacion de un inhibidor de egfr t790m y un inhibidor de egfr para el tratamiento del cancer pulmonar de celulas no pequeñas. |
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| KR101657616B1 (ko) * | 2013-05-24 | 2016-09-19 | 주식회사유한양행 | 피리미딘 고리를 포함하는 바이사이클릭 유도체 및 그의 제조방법 |
| WO2015039612A1 (zh) * | 2013-09-18 | 2015-03-26 | 北京韩美药品有限公司 | 抑制btk和/或jak3激酶活性的化合物 |
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| EA201790189A1 (ru) | 2014-07-14 | 2017-11-30 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Способы лечения злокачественного новообразования с использованием замещенных пирролопиримидиновых соединений, композиции на их основе |
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| HK1246645A1 (zh) | 2015-03-27 | 2018-09-14 | 达纳-法伯癌症研究所股份有限公司 | 细胞周期蛋白依赖性激酶的抑制剂 |
| CN112932416A (zh) | 2015-06-04 | 2021-06-11 | 松下知识产权经营株式会社 | 生物体信息检测装置及生物体信息检测方法 |
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| WO2018155916A2 (ko) * | 2017-02-22 | 2018-08-30 | 재단법인 대구경북첨단의료산업진흥재단 | 피롤로-피리미딘 유도체 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 단백질 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물 |
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| WO2019075386A1 (en) | 2017-10-13 | 2019-04-18 | The Regents Of The University Of California | MODULATORS OF MTORC1 |
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| CN111527091B (zh) * | 2017-12-28 | 2023-03-28 | 株式会社大熊制药 | 作为激酶抑制剂的氧基-氟哌啶衍生物 |
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| EP3842435A4 (en) * | 2018-09-20 | 2022-05-11 | Hanmi Pharm. Co., Ltd. | NEW SULFONAMIDE DERIVATIVE PRESENTING A FUSED PYRIMIDINE SKELETON, HAVING AN INHIBITOR EFFECT OF EPIDERMAL GROWTH FACTOR RECEPTOR MUTATION |
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| WO2022062601A1 (zh) * | 2020-09-22 | 2022-03-31 | 江苏先声药业有限公司 | 嘧啶并吡咯类化合物 |
| CN114315838B (zh) * | 2020-09-30 | 2024-09-03 | 江苏先声药业有限公司 | 嘧啶并吡咯类化合物 |
| CN114907357A (zh) * | 2021-02-07 | 2022-08-16 | 江苏先声药业有限公司 | 嘧啶并吡咯类化合物 |
| CN118103371A (zh) * | 2021-09-18 | 2024-05-28 | 山东新时代药业有限公司 | 一种egfr抑制剂及其制备方法和用途 |
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