TWI830713B - 作為lpa拮抗劑之三唑n-連接之胺甲醯基環己基酸 - Google Patents

作為lpa拮抗劑之三唑n-連接之胺甲醯基環己基酸 Download PDF

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TWI830713B
TWI830713B TW107145551A TW107145551A TWI830713B TW I830713 B TWI830713 B TW I830713B TW 107145551 A TW107145551 A TW 107145551A TW 107145551 A TW107145551 A TW 107145551A TW I830713 B TWI830713 B TW I830713B
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pharmaceutically acceptable
alkyl
acceptable salt
compound
lpa
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TW107145551A
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TW201927765A (zh
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琰 施
泰華 鄭
瑩 王
史俊
式微 陶
峻 李
勞倫斯 Ｊ 甘迺迪
羅伯 Ｆ 三世 卡特巴
張浩
詹姆士 R 柯德
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美商必治妥美雅史谷比公司
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    • 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
    • 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
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • 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
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    • C07C249/04—Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of oximes
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C403/00—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone
    • C07C403/04—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by halogen atoms
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    • 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
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    • 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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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
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  • Endocrinology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
TW107145551A 2017-12-19 2018-12-18 作為lpa拮抗劑之三唑n-連接之胺甲醯基環己基酸 TWI830713B (zh)

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US201762607399P 2017-12-19 2017-12-19
US62/607,399 2017-12-19

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TW201927765A TW201927765A (zh) 2019-07-16
TWI830713B true TWI830713B (zh) 2024-02-01

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US (4) US10662172B2 (enExample)
EP (2) EP3710438B1 (enExample)
JP (1) JP7274486B6 (enExample)
KR (1) KR102702229B1 (enExample)
CN (2) CN112189010A (enExample)
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KR102702231B1 (ko) 2017-12-19 2024-09-02 브리스톨-마이어스 스큅 컴퍼니 Lpa 길항제로서의 피라졸 o-연결된 카르바모일 시클로헥실 산
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CN119823001A (zh) * 2019-07-30 2025-04-15 大正制药株式会社 拮抗lpa1受体的脲化合物
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CN114787157A (zh) 2019-12-12 2022-07-22 奇斯药制品公司 作为lpa受体2抑制剂的芳族酰氨基衍生物
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JP2023505702A (ja) 2019-12-12 2023-02-10 キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ Ｌｐａ受容体２阻害剤としてのチエノピリミジン誘導体
CA3185689A1 (en) * 2020-06-03 2021-12-09 Gilead Sciences, Inc. 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
ES2991765T3 (es) 2020-07-16 2024-12-04 Chiesi Farm Spa Derivados del ácido amido ciclohexano como inhibidores del receptor de LPA
CN114456159A (zh) * 2020-11-10 2022-05-10 武汉人福创新药物研发中心有限公司 氮取代杂环噻吩类化合物及其用途
WO2022174883A1 (en) 2021-02-16 2022-08-25 Chiesi Farmaceutici S.P.A. 5-membered heterocyclyl derivatives as dual lpa receptor 1 and lpa receptor 2 inhibitors
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EP4313956A1 (en) 2021-03-24 2024-02-07 Chiesi Farmaceutici S.p.A. 8-cyclo-substituted quinazoline derivatives as lpa receptor 2 inhibitors
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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
WO2025051266A1 (zh) * 2023-09-08 2025-03-13 西藏海思科制药有限公司 杂芳环衍生物的lpar1拮抗剂及其用途
WO2025162421A1 (zh) * 2024-02-04 2025-08-07 西藏海思科制药有限公司 Lpar1拮抗剂及其用途

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