TWI891649B - 作為cd38抑制劑之雜雙環醯胺 - Google Patents

作為cd38抑制劑之雜雙環醯胺

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Publication number
TWI891649B
TWI891649B TW109125742A TW109125742A TWI891649B TW I891649 B TWI891649 B TW I891649B TW 109125742 A TW109125742 A TW 109125742A TW 109125742 A TW109125742 A TW 109125742A TW I891649 B TWI891649 B TW I891649B
Authority
TW
Taiwan
Prior art keywords
carboxamide
pyrimidine
imidazol
alkyl
pyrrolo
Prior art date
Application number
TW109125742A
Other languages
English (en)
Chinese (zh)
Other versions
TW202120496A (zh
Inventor
羅利 Ｂ 申克爾
梅麗莎 瑪麗 瓦斯賓達
凱文 韋恩 坎茲
尼可拉斯 羅伯特 伯爾
珍妮弗 道寧
Original Assignee
德商百靈佳殷格翰國際股份有限公司
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Application filed by 德商百靈佳殷格翰國際股份有限公司 filed Critical 德商百靈佳殷格翰國際股份有限公司
Publication of TW202120496A publication Critical patent/TW202120496A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • 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
    • A61K31/41—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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/41—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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/41—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
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • C07D403/10—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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW109125742A 2019-07-31 2020-07-30 作為cd38抑制劑之雜雙環醯胺 TWI891649B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201962880923P 2019-07-31 2019-07-31
US62/880,923 2019-07-31
US201962951604P 2019-12-20 2019-12-20
US62/951,604 2019-12-20
US202063034750P 2020-06-04 2020-06-04
US63/034,750 2020-06-04

Publications (2)

Publication Number Publication Date
TW202120496A TW202120496A (zh) 2021-06-01
TWI891649B true TWI891649B (zh) 2025-08-01

Family

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Application Number Title Priority Date Filing Date
TW109125742A TWI891649B (zh) 2019-07-31 2020-07-30 作為cd38抑制劑之雜雙環醯胺

Country Status (12)

Country Link
US (4) US11535621B2 (https=)
EP (1) EP4003980A1 (https=)
JP (2) JP7721501B2 (https=)
KR (1) KR20220061958A (https=)
CN (2) CN119431323A (https=)
AU (1) AU2020321956A1 (https=)
BR (1) BR112022001291A2 (https=)
CA (1) CA3147902A1 (https=)
IL (2) IL324885A (https=)
MX (3) MX2022001019A (https=)
TW (1) TWI891649B (https=)
WO (1) WO2021021986A1 (https=)

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MX2022001019A (es) 2019-07-31 2022-02-22 Ribon Therapeutics Inc Amidas heterobiciclicas como inhibidoras del cumulo de diferenciacion 38 (cd38).
US20230025807A1 (en) * 2019-10-30 2023-01-26 Mitobridge Inc. Cd38 inhibitors
CA3195121A1 (en) * 2020-10-09 2022-04-14 Robert A. Volkmann Heteroaryl amide inhibitors of cd38
HRP20251111T1 (hr) 2021-01-29 2025-11-21 Boehringer Ingelheim International Gmbh Azakinolini kao inhibitori cd38
WO2022228496A1 (en) * 2021-04-30 2022-11-03 Nanjing Immunophage Biotech Co., Ltd Compounds and their uses as cd38 inhibitors
TW202310835A (zh) * 2021-07-12 2023-03-16 美商胞質動力學公司 Ｃｄ３８調節劑及其使用方法
CN116041344A (zh) * 2021-10-28 2023-05-02 北京望实智慧科技有限公司 双环杂芳基甲酰胺化合物作为sos1抑制剂
WO2023084206A1 (en) 2021-11-09 2023-05-19 Cerevance Ltd N-(4-aminocyclohexyl)pyrimidine-4-carboxamide derivatives as cd38 inhibitors
CN114306366B (zh) * 2021-11-30 2023-01-06 合肥康诺生物制药有限公司 含nad和cd38抑制剂的药物组合物及其用途
WO2023098699A1 (en) * 2021-12-01 2023-06-08 Nanjing Immunophage Biotech Co., Ltd Compounds and their uses as cd38 inhibitors
GB202207721D0 (en) * 2022-05-25 2022-07-06 Cerevance Ltd Novel Compounds
JP2025530999A (ja) * 2022-08-05 2025-09-19 ネクストジェン バイオサイエンス カンパニー リミテッド 低酸素症誘導因子１（ｈｉｆ－１）抑制剤又は血管内皮成長因子（ｖｅｇｆ）抑制剤としての新規化合物及びそれを含む薬学組成物
CN115825297B (zh) * 2022-11-11 2025-03-28 武汉海特生物创新医药研究有限公司 一种(s)-3-氨基哌啶-2,6-二酮盐酸盐对映异构体的检测方法
WO2024236316A1 (en) * 2023-05-18 2024-11-21 Cerevance, Inc. 3-carbonyl imidazo[1,5-a]pyridine derivatives for use as cd38 inhibitors for the treatment of cns disorders
GB202307426D0 (en) * 2023-05-18 2023-07-05 Cerevance Inc Novel compounds
WO2024254396A1 (en) * 2023-06-07 2024-12-12 Flagship Pioneering Innovations, Vi, Llc Condensed azines as inhibitors of cyclic adp ribose hydrolase
WO2026000074A1 (en) * 2024-06-25 2026-01-02 Welnx Company Inc. Use of cd38 inhibitors for reducing th2 inflammation
WO2026075971A1 (en) 2024-10-01 2026-04-09 Neolaia Inc. Combination therapy for treatment of metabolic disorders and inflamation related disorders using incretin compounds and cd38 inhibitors

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TW202120496A (zh) 2021-06-01
MX2025003445A (es) 2025-05-02
MX2025003444A (es) 2025-05-02
US20260078127A1 (en) 2026-03-19
WO2021021986A1 (en) 2021-02-04
US11535621B2 (en) 2022-12-27
AU2020321956A1 (en) 2022-03-10
US12398146B2 (en) 2025-08-26
IL289878B1 (en) 2026-01-01
JP2022542396A (ja) 2022-10-03
BR112022001291A2 (pt) 2022-06-21
JP7721501B2 (ja) 2025-08-12
US20210032251A1 (en) 2021-02-04
CA3147902A1 (en) 2021-02-04
IL289878A (en) 2022-03-01
US20240368167A1 (en) 2024-11-07
CN114423753B (zh) 2024-09-17
EP4003980A1 (en) 2022-06-01
US20230312586A1 (en) 2023-10-05
KR20220061958A (ko) 2022-05-13
US11987584B2 (en) 2024-05-21
JP2025160384A (ja) 2025-10-22
CN114423753A (zh) 2022-04-29
IL324885A (en) 2026-01-01
MX2022001019A (es) 2022-02-22
CN119431323A (zh) 2025-02-14

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