CN113473985A - 作为lpa拮抗剂的环戊酸 - Google Patents

作为lpa拮抗剂的环戊酸 Download PDF

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Publication number
CN113473985A
CN113473985A CN201980074355.6A CN201980074355A CN113473985A CN 113473985 A CN113473985 A CN 113473985A CN 201980074355 A CN201980074355 A CN 201980074355A CN 113473985 A CN113473985 A CN 113473985A
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Prior art keywords
independently
lpa
alkyl
substituted
compound
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CN201980074355.6A
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Chinese (zh)
Inventor
郑泰华
R·F·卡伦巴赫三世
史俊
施琰
张�浩
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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Publication of CN113473985A publication Critical patent/CN113473985A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/14—Nitrogen atoms
    • 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
    • A61K31/42—Oxazoles
    • 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero 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
    • C07D417/14—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 three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201980074355.6A 2018-09-18 2019-09-16 作为lpa拮抗剂的环戊酸 Pending CN113473985A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862732590P 2018-09-18 2018-09-18
US62/732,590 2018-09-18
PCT/US2019/051274 WO2020060915A1 (en) 2018-09-18 2019-09-16 Cyclopentyl acids as lpa antagonists

Publications (1)

Publication Number Publication Date
CN113473985A true CN113473985A (zh) 2021-10-01

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CN201980074355.6A Pending CN113473985A (zh) 2018-09-18 2019-09-16 作为lpa拮抗剂的环戊酸

Country Status (7)

Country Link
US (1) US12209072B2 (https=)
EP (1) EP3852746B1 (https=)
JP (1) JP7427658B2 (https=)
KR (1) KR102950123B1 (https=)
CN (1) CN113473985A (https=)
ES (1) ES2946657T3 (https=)
WO (1) WO2020060915A1 (https=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025051267A1 (zh) * 2023-09-08 2025-03-13 西藏海思科制药有限公司 一种lpar1拮抗剂及其用途
CN120530099A (zh) * 2023-01-19 2025-08-22 江苏恒瑞医药股份有限公司 一种三氮唑类化合物的可药用盐、晶型及其制备方法
WO2026061483A1 (zh) * 2024-09-19 2026-03-26 西藏海思科制药有限公司 一种lpar1拮抗剂及其用途

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US20220041572A1 (en) * 2018-09-18 2022-02-10 Bristol-Myers Squibb Company Cycloheptyl acids as lpa antagonists
KR102788997B1 (ko) 2018-09-18 2025-03-28 브리스톨-마이어스 스큅 컴퍼니 Lpa 길항제로서의 옥사비시클로 산
CN111434655A (zh) * 2019-01-15 2020-07-21 武汉朗来科技发展有限公司 溶血磷脂酸受体拮抗剂及其制备方法
AU2020256166A1 (en) 2019-04-02 2021-10-14 Aligos Therapeutics, Inc. Compounds targeting PRMT5
AU2020384883B2 (en) 2019-11-15 2023-11-16 Gilead Sciences, Inc. Triazole carbamate pyridyl sulfonamides as LPA receptor antagonists and uses thereof
TWI843503B (zh) 2020-06-03 2024-05-21 美商基利科學股份有限公司 Lpa受體拮抗劑及其用途
CN115867556B (zh) * 2020-06-03 2025-05-06 吉利德科学公司 Lpa受体拮抗剂及其用途
EP4196220A1 (en) * 2020-08-11 2023-06-21 Viva Star Biosciences Limited Triazole-pyridinyl substituted azacyclohexyl acetic acid compounds as lpa receptor antagonists
EP4330249A1 (en) * 2021-04-30 2024-03-06 Viva Star Biosciences (Suzhou) Co., Ltd. Novel triazole-pyridine substituted pyrrolidinyl and tetrahydro-2h-pyranyl acetic acid compounds as lpa antagonists
TWI853704B (zh) * 2021-05-11 2024-08-21 美商基利科學股份有限公司 Lpa受體拮抗劑及其用途
KR20240007233A (ko) 2021-05-13 2024-01-16 길리애드 사이언시즈, 인코포레이티드 Lpa 수용체 길항제 및 이의 용도
CA3224635A1 (en) * 2021-07-20 2023-01-26 Yunfei Li Lpa1 small molecule antagonist
WO2023107938A1 (en) 2021-12-08 2023-06-15 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
AR128613A1 (es) 2022-02-25 2024-05-29 Lhotse Bio Inc Compuestos y composiciones para el tratamiento de afecciones asociadas con la actividad del receptor de lpa

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WO2019126089A1 (en) 2017-12-19 2019-06-27 Bristol-Myers Squibb Company Cyclohexyl acid pyrazole azines as lpa antagonists
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EP3728209B1 (en) 2017-12-19 2025-12-24 Bristol-Myers Squibb Company Cyclohexyl acid isoxazole azines as lpa antagonists
CN111699180B (zh) 2017-12-19 2024-11-29 百时美施贵宝公司 作为lpa拮抗剂的吡唑n-连接的氨基甲酰基环己基酸
KR102756639B1 (ko) 2017-12-19 2025-01-16 브리스톨-마이어스 스큅 컴퍼니 Lpa 길항제로서의 시클로헥실 산 이속사졸 아졸
CN112041302B (zh) 2017-12-19 2024-11-19 百时美施贵宝公司 作为lpa拮抗剂的吡唑o-连接的氨基甲酰基环己基酸
US20220041572A1 (en) * 2018-09-18 2022-02-10 Bristol-Myers Squibb Company Cycloheptyl acids as lpa antagonists
KR102788997B1 (ko) * 2018-09-18 2025-03-28 브리스톨-마이어스 스큅 컴퍼니 Lpa 길항제로서의 옥사비시클로 산

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN120530099A (zh) * 2023-01-19 2025-08-22 江苏恒瑞医药股份有限公司 一种三氮唑类化合物的可药用盐、晶型及其制备方法
WO2025051267A1 (zh) * 2023-09-08 2025-03-13 西藏海思科制药有限公司 一种lpar1拮抗剂及其用途
WO2026061483A1 (zh) * 2024-09-19 2026-03-26 西藏海思科制药有限公司 一种lpar1拮抗剂及其用途

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WO2020060915A1 (en) 2020-03-26
ES2946657T3 (es) 2023-07-24
JP7427658B2 (ja) 2024-02-05
KR20210061383A (ko) 2021-05-27
EP3852746B1 (en) 2023-03-29
US12209072B2 (en) 2025-01-28
EP3852746A1 (en) 2021-07-28
JP2022500470A (ja) 2022-01-04
US20220041565A1 (en) 2022-02-10
KR102950123B1 (ko) 2026-04-08

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