PE20181491A1 - Nuevos derivados biciclicos, un proceso para su preparacion y composiciones farmaceuticas que los contienen - Google Patents
Nuevos derivados biciclicos, un proceso para su preparacion y composiciones farmaceuticas que los contienenInfo
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- PE20181491A1 PE20181491A1 PE2017002717A PE2017002717A PE20181491A1 PE 20181491 A1 PE20181491 A1 PE 20181491A1 PE 2017002717 A PE2017002717 A PE 2017002717A PE 2017002717 A PE2017002717 A PE 2017002717A PE 20181491 A1 PE20181491 A1 PE 20181491A1
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- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
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- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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- A61K31/4355—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 oxygen as a ring hetero atom
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- 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
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- C07D209/04—Indoles; Hydrogenated indoles
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- C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
- C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
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- C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
- C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D307/81—Radicals substituted by nitrogen atoms not forming part of a nitro radical
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- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D333/56—Radicals substituted by oxygen atoms
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- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- Chemical & Material Sciences (AREA)
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- Nitrogen Condensed Heterocyclic Rings (AREA)
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
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- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Referido a compuestos derivados biciclicos de formula (I), en donde: A representa el grupo (a), en la que 1 esta unido al grupo W y 2 unido al anillo fenilo; E es un anillo furilo, tienilo o pirrolilo; X1, X3, X4 y X5 independientemente uno de otro, es un atomo de carbono o nitrogeno; X2 es C-R21 o un atomo de nitrogeno. R1 es un atomo de halogeno, un grupo alquilo(C1-C6) lineal o ramificado, un grupo alquenilo(C2-C6) lineal o ramificado, entre otros; R2, R3, R4 y R5 independientemente uno de otro, es un atomo de hidrogeno, halogeno, un grupo alquilo(C1-C6) lineal o ramificado, un grupo alquenilo(C2-C6) lineal o ramificado, entre otros, entre otros; R6 y R7 independientemente uno de otro, es un atomo de halogeno, un grupo alquilo(C1-C6) lineal o ramificado, un grupo alquinilo(C2-C6) lineal o ramificado, entre otros; W es -CH2-, -NH- o un atomo de oxigeno; R8 es un atomo de hidrogeno, alquilo(C1-C8) lineal o ramificado, un grupo arilo, entre otros; R9 es un atomo de hidrogeno, un grupo alquilo(C1-C6) lineal o ramificado, un grupo alquenilo(C2-C6), entre otros; R10 es un atomo de hidrogeno, un grupo alquilo(C1-C6) lineal o ramificado, un grupo alquenilo(C2-C6) lineal o ramificado; R14 es un atomo de hidrogeno, un grupo hidroxi o un grupo hidroxialquilo(C1-C6); n es un numero entero igual a 0 o 1. Tambien se refiere a procesos para la preparacion de estos compuestos y a composiciones farmaceuticas que comprenden estos compuestos, los cuales son utiles como agentes pro-apoptoticos, en el tratamiento de cancer y de enfermedades autoinmunes.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR1555750A FR3037959B1 (fr) | 2015-06-23 | 2015-06-23 | Nouveaux derives bicycliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20181491A1 true PE20181491A1 (es) | 2018-09-18 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2017002717A PE20181491A1 (es) | 2015-06-23 | 2016-06-22 | Nuevos derivados biciclicos, un proceso para su preparacion y composiciones farmaceuticas que los contienen |
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| FR3037956B1 (fr) * | 2015-06-23 | 2017-08-04 | Servier Lab | Nouveaux derives d'acide amine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| FR3037957B1 (fr) * | 2015-06-23 | 2019-01-25 | Les Laboratoires Servier | Nouveaux derives d'hydroxyester, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| FR3037958B1 (fr) * | 2015-06-23 | 2019-01-25 | Les Laboratoires Servier | Nouveaux derives d'hydroxy-acide, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| ES2990061T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros espirocíclicos para la degradación de proteínas diana |
| WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| ES2989988T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros heterorocíclicos para la degradación de proteínas diana |
| EP3455219A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| UY37342A (es) | 2016-07-22 | 2018-01-31 | Servier Lab | Combinación de un inhibidor de bcl-2 y un inhibidor de mcl1, usos y composiciones farmacéuticas de éstos |
| ES2975274T3 (es) * | 2017-01-06 | 2024-07-04 | Servier Lab | Combinación de un inhibidor de MCL-1 y un compuesto de taxano, sus usos y composiciones farmacéuticas |
| UY37560A (es) | 2017-01-06 | 2018-07-31 | Servier Lab | Combinación de un inhibidor de mcl-1 y un compuesto taxano, usos y composiciones farmacéuticas de ésta |
| WO2018237026A1 (en) | 2017-06-20 | 2018-12-27 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| BR112019026959A2 (pt) | 2017-06-22 | 2020-07-07 | Les Laboratoires Servier | combinação de um inibidor de mcl-1 e um tratamento com padrão de atendimento para cânceres hematológicos, seus usos e composições farmacêuticas |
| CA3073112A1 (en) | 2017-08-15 | 2019-02-21 | Abbvie Inc. | Macrocyclic mcl-1 inhibitors and methods of use |
| CN112533598A (zh) * | 2017-08-15 | 2021-03-19 | 艾伯维公司 | 大环mcl-1抑制剂和使用方法 |
| CN111372936B (zh) * | 2017-11-23 | 2022-12-02 | 北京赛林泰医药技术有限公司 | Mcl-1选择性抑制剂及其制备和用途 |
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| AR116635A1 (es) | 2018-10-15 | 2021-05-26 | Servier Lab | Proceso para la síntesis de derivados de piperazinil-etoxi-bromofenilo y su aplicación en la producción de compuestos que los contienen |
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| KR101973074B1 (ko) * | 2018-11-30 | 2019-04-26 | 주식회사 티움바이오 | 퓨로피리미딘 화합물의 염 및 결정형, 및 이를 포함하는 약학적 조성물 |
| EP3897631A4 (en) | 2018-12-20 | 2022-11-23 | C4 Therapeutics, Inc. | TARGETED PROTEIN BREAKDOWN |
| AU2020279979A1 (en) | 2019-05-20 | 2021-11-25 | Les Laboratoires Servier | Mcl-1 inhibitor antibody-drug conjugates and methods of use |
| AR119156A1 (es) | 2019-06-17 | 2021-11-24 | Servier Lab | Combinación de un inhibidor de mcl-1 y un tratamiento estándar de atención médica para cáncer de mama, usos y composiciones farmacéuticas de la misma |
| CN114746428B (zh) * | 2019-10-03 | 2025-05-16 | 加利福尼亚技术学院 | Mcl1抑制剂及其应用 |
| US12522606B2 (en) * | 2020-01-09 | 2026-01-13 | University Of Washington | Modified pyrrolo- and pyrazolo-pyrimidines for prostate cancer therapy |
| CN117136076A (zh) | 2020-11-24 | 2023-11-28 | 诺华股份有限公司 | Mcl-1抑制剂抗体药物缀合物和使用方法 |
| WO2022216946A1 (en) * | 2021-04-07 | 2022-10-13 | California Institute Of Technology | Mcl1 inhibitors and uses thereof |
| JP2024520801A (ja) | 2021-06-11 | 2024-05-24 | ギリアード サイエンシーズ, インコーポレイテッド | Mcl-1阻害剤と抗がん剤との組み合わせ |
| TWI861509B (zh) | 2021-06-11 | 2024-11-11 | 美商基利科學股份有限公司 | Mcl-1抑制劑與抗體藥物接合物之組合 |
| IL317101A (en) | 2022-05-20 | 2025-01-01 | Novartis Ag | Antibody-drug conjugates of anticancer compounds and methods of using them |
| WO2025111450A1 (en) | 2023-11-22 | 2025-05-30 | Les Laboratoires Servier | Anti-cd74 antibody-drug conjugates and methods of use thereof |
| WO2025111431A1 (en) | 2023-11-22 | 2025-05-30 | Les Laboratoires Servier | Anti-cd7 antibody-drug conjugates and methods of use thereof |
| WO2025126157A1 (en) | 2023-12-15 | 2025-06-19 | Advesya | Anti-il-1rap binding domains and antibody-drug conjugates thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2172670T3 (es) | 1995-07-06 | 2002-10-01 | Novartis Ag | Pirrolpirimidinas y procedimientos para su preparacion. |
| EP1922321A1 (en) * | 2005-08-09 | 2008-05-21 | Eirx Therapeutics Ltd | Pyrazoloý1,5-a¨pyrimidine compounds and pharmaceutical compositions containing them |
| AR057960A1 (es) * | 2005-12-02 | 2007-12-26 | Osi Pharm Inc | Inhibidores de proteina quinasa biciclicos |
| CN102264745B (zh) * | 2008-11-10 | 2015-07-22 | 财团法人卫生研究院 | 作为酪胺酸激酶抑制剂的稠合双环及多环嘧啶化合物 |
| PE20142449A1 (es) | 2008-12-18 | 2015-01-11 | Bayer Cropscience Ag | Amidas del acido antranilico sustituidas con tetrazol como plaguicidas |
| JP2013505899A (ja) | 2009-09-28 | 2013-02-21 | チールー ファーマシューティカル カンパニー、リミテッド | チロシンキナーゼ阻害剤として有用な4−(置換アニリノ)キナゾリン誘導体 |
| CN102464667B (zh) * | 2010-11-03 | 2014-06-04 | 中国科学院上海药物研究所 | 一类五元杂环并嘧啶类化合物及其制备方法和用途 |
| MX2014005285A (es) * | 2011-11-03 | 2014-05-30 | Hoffmann La Roche | Compuestos biciclicos de piperazina. |
| AR090037A1 (es) * | 2011-11-15 | 2014-10-15 | Xention Ltd | Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio |
| FR2986002B1 (fr) | 2012-01-24 | 2014-02-21 | Servier Lab | Nouveaux derives d'indolizine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| FR3015483B1 (fr) * | 2013-12-23 | 2016-01-01 | Servier Lab | Nouveaux derives de thienopyrimidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| FR3037958B1 (fr) * | 2015-06-23 | 2019-01-25 | Les Laboratoires Servier | Nouveaux derives d'hydroxy-acide, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| FR3037956B1 (fr) * | 2015-06-23 | 2017-08-04 | Servier Lab | Nouveaux derives d'acide amine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| FR3037957B1 (fr) * | 2015-06-23 | 2019-01-25 | Les Laboratoires Servier | Nouveaux derives d'hydroxyester, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
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