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PE20230820A1 - Derivados de biarilo como inhibidores de la interaccion proteina-proteina de yap/taz-tead - Google Patents

Derivados de biarilo como inhibidores de la interaccion proteina-proteina de yap/taz-tead

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Publication number
PE20230820A1
PE20230820A1 PE2022001962A PE2022001962A PE20230820A1 PE 20230820 A1 PE20230820 A1 PE 20230820A1 PE 2022001962 A PE2022001962 A PE 2022001962A PE 2022001962 A PE2022001962 A PE 2022001962A PE 20230820 A1 PE20230820 A1 PE 20230820A1
Authority
PE
Peru
Prior art keywords
halo
heteroatom
protein
yap
taz
Prior art date
Application number
PE2022001962A
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English (en)
Inventor
Vincent Bordas
Cara Brocklehurst
Patrick Chene
Zhongbo Fei
Pascal Furet
Vito Guagnano
Patricia Imbach-Weese
Joerg Kallen
Douget Mickael Le
Jialiang Li
Wei Li
Edwige Liliane Jeanne Lorthiois
Joseph Mckenna
Bahaa Salem
Tobias Schmelzle
Holger Sellner
Nicolas Soldermann
Markus Voegtle
Markus Wartmann
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20230820A1 publication Critical patent/PE20230820A1/es

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    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • 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
    • A61K31/40—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
    • A61K31/4025—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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/40—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/404—Indoles, e.g. pindolol
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D403/02—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
    • C07D403/04—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 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
    • C07D405/04—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
    • C07D405/10—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 carbon chain containing aromatic rings
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    • 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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    • C07D405/14—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 three or more hetero rings
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    • C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Referido a un compuesto derivado de biarilo de formula (I) o una sal farmaceuticamente aceptable del mismo, en donde W se selecciona entre O y CH-Rw; X se selecciona entre CH y N; Y se selecciona entre CH y N; Z se selecciona entre CH2, O y NH; en donde cuando Y es N, W es CH-Rw, y Z es O; A se selecciona entre: fenilo, opcionalmente sustituido con halo o haloalcoxi C1-C3; un anillo heterociclico aromatico de 5 o 6 miembros que comprende por lo menos un heteroatomo seleccionado entre N, O, y S; entre otros; Q se selecciona entre -C(R7)2-N(R8)-R1; heteroarilo parcialmente saturado de 9 o 10 miembros que comprende por lo menos un heteroatomo N; y un anillo heterociclico de 4, 5, o 6 miembros que comprende por lo menos un heteroatomo o grupo de heteroatomo seleccionado entre N, O, S, -S(=O) y -S(=O)2; R2 se selecciona entre hidrogeno y halo; R3 se selecciona entre halo, haloalquilo C1-C3 y ciano; R4 se selecciona entre H, halo; y alquilo C1-C3; R5 se selecciona entre H, alcoxi C1-C6 opcionalmente sustituido con cicloalquilo C3-C6, CO2H, SO2 alquilo C1-C3, entre otros; R6 se selecciona entre H, ciano, C(O)NHR6a, entre otros. Un compuesto seleccionado es 2-((2S,4S)-2-(aminometil)-5-cloro-2-fenil-2,3-dihidrobenzofuran-4-il)-3-fluorobenzamida. Dichos compuestos son inhibidores de la interaccion proteina-proteina de YAP/TAZ-TEAD. Tambien se refiere a una composicion farmaceutica que comprende dichos compuestos; un proceso para la preparacion de dicho compuesto y su uso en el tratamiento de cancer o tumor particularmente en el tratamiento del mesotelioma (incluido el mesotelioma pleural maligno), cancer de pancreas, sarcoma y cancer de pulmon de celulas no pequenas.
PE2022001962A 2020-03-16 2021-03-15 Derivados de biarilo como inhibidores de la interaccion proteina-proteina de yap/taz-tead PE20230820A1 (es)

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CN114555569B (zh) 2019-07-17 2024-10-29 祖玛珍生物科学有限公司 Nlrp3调节剂
WO2021009566A1 (en) 2019-07-17 2021-01-21 Zomagen Biosciences Ltd N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4,5,6,7-tetrahydrobenzofuran -2-sulfonamide derivatives and related compounds as nlpr3 modulators for the treatment of multiple sclerosis (ms)
JP2024530295A (ja) 2021-09-01 2024-08-16 ノバルティス アーゲー ビアリールｙａｐ／ｔａｚ－ｔｅａｄタンパク質間相互作用阻害剤の結晶形態
JP2024532374A (ja) 2021-09-01 2024-09-05 ノバルティス アーゲー Ｔｅａｄ阻害剤を含む医薬品組み合わせ物及び癌の治療のためのその使用
CN117835977A (zh) 2021-09-01 2024-04-05 诺华股份有限公司 Tead抑制剂的给药方案
EP4395828A1 (en) 2021-09-01 2024-07-10 Novartis AG Bifunctional degraders comprising a tead binder
CN118574835A (zh) 2021-12-01 2024-08-30 勃林格殷格翰国际有限公司 用于治疗癌症的环状2-氨基-3-氰基噻吩及衍生物
TW202337431A (zh) 2021-12-01 2023-10-01 德商百靈佳殷格翰國際股份有限公司 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物
US20250145608A1 (en) 2021-12-01 2025-05-08 Boehringer Ingelheim Int'l GmbH Corp. Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes
CN118613485A (zh) 2021-12-01 2024-09-06 勃林格殷格翰国际有限公司 用于治疗癌症的环状2-氨基-3-氰基噻吩及衍生物
CN119013272A (zh) 2021-12-01 2024-11-22 勃林格殷格翰国际有限公司 用于治疗癌症的环状2-氨基-3-氰基噻吩及其衍生物
US20250129096A1 (en) 2021-12-01 2025-04-24 Boehringer Ingelheim Int'l GmbH Corp. Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
JP7774326B2 (ja) * 2021-12-02 2025-11-21 上▲海▼栖臻医▲薬▼科技有限公司 芳香族化合物、その医薬組成物及びその使用
WO2023137634A1 (zh) * 2022-01-19 2023-07-27 上海奕拓医药科技有限责任公司 三并环化合物、其制备、药物组合物及应用
EP4484420A1 (en) 2022-02-21 2025-01-01 Etern Biopharma (Shanghai) Co., Ltd. Inhibitor of interaction between yap/taz and tead, preparation thereof, pharmaceutical composition thereof and use thereof
CN116813475A (zh) * 2022-06-29 2023-09-29 北京大学 一种芳环化合物的卤化合成方法
KR20240014034A (ko) * 2022-07-21 2024-01-31 주식회사 바오밥에이바이오 헤테로비시클릭 화합물 및 그를 포함하는 약제학적조성물
KR20250078472A (ko) 2022-09-29 2025-06-02 인실리코 메디신 아이피 리미티드 Tead 억제제 및 이의 사용 방법
TW202421158A (zh) 2022-11-18 2024-06-01 瑞士商諾華公司 藥物組合及其用途
WO2024176130A1 (en) 2023-02-23 2024-08-29 Novartis Ag Tead- and her2-inhibitor combinations for treating cancer
CN120769852A (zh) 2023-02-23 2025-10-10 诺华股份有限公司 联芳基yap/taz-tead蛋白-蛋白相互作用抑制剂的结晶形式
EP4669320A1 (en) 2023-02-23 2025-12-31 Novartis AG COMBINATIONS OF TEAD AND KRAS G12D INHIBITORS FOR CANCER TREATMENT
KR20240149354A (ko) * 2023-04-05 2024-10-14 주식회사 바오밥에이바이오 헤테로비시클릭 화합물 및 그를 포함하는 약제학적 조성물
CN121175302A (zh) * 2023-05-15 2025-12-19 江苏豪森药业集团有限公司 联芳基化合物、其制备方法及其医药用途
WO2024238763A2 (en) * 2023-05-16 2024-11-21 Springworks Therapeutics, Inc. Tetrahydronapthyridine and related analogs for inhibiting yap/taz-tead
WO2024246099A1 (en) 2023-05-30 2024-12-05 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2025210282A1 (en) * 2024-04-05 2025-10-09 Amphista Therapeutics Limited Compounds for targeted protein degradation
WO2025215527A2 (en) 2024-04-10 2025-10-16 Novartis Ag Pharmaceutical combinations and uses thereof
WO2025232876A1 (en) * 2024-05-10 2025-11-13 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Oxy-amide derivatives, preparation method and medical use thereof
CN119143652B (zh) * 2024-09-13 2025-11-28 山东大学 一种手性2位双取代吲哚啉化合物及其合成方法与应用

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU1856997A (en) 1996-02-02 1997-08-22 Merck & Co., Inc. Method for raising hdl cholesterol levels
CA2495943C (en) 2002-08-29 2009-07-21 Merck & Co., Inc. Indoles having anti-diabetic activity
DE102005010000A1 (de) 2005-03-04 2006-09-07 Merck Patent Gmbh Indane
TW201028414A (en) 2009-01-16 2010-08-01 Merck Sharp & Dohme Oxadiazole beta carboline derivatives as antidiabetic compounds
KR20110128913A (ko) * 2009-03-10 2011-11-30 다케다 야쿠힌 고교 가부시키가이샤 벤조푸란 유도체
US10053465B2 (en) * 2015-08-26 2018-08-21 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
EP3156404A1 (en) * 2015-10-15 2017-04-19 Inventiva New compounds inhibitors of the yap/taz-tead interaction and their use in the treatment of malignant mesothelioma
WO2019201283A1 (en) * 2018-04-20 2019-10-24 Xrad Therapeutics, Inc. Dual atm and dna-pk inhibitors for use in anti-tumor therapy
WO2019232216A1 (en) * 2018-05-31 2019-12-05 Genentech, Inc. Therapeutic compounds
EP3813826A4 (en) * 2018-06-26 2022-07-06 BioSplice Therapeutics, Inc. METHOD OF TREATMENT OF CANCER USING A CLK INHIBITOR
JP2021536445A (ja) 2018-08-29 2021-12-27 ケモセントリックス，インコーポレイティド 小型分子ｐｄ−ｌ１インヒビターによる癌治療法
TW202024023A (zh) * 2018-09-03 2020-07-01 瑞士商赫孚孟拉羅股份公司 治療性化合物及其使用方法

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